Microbiology

A Rare Case of Neurosyphilis with Calvaria Osteitis Presenting in Pregnancy

15 | Feb 14 2024

Syphilitic osteitis and neuro, otic, or ocular syphilis during pregnancy, though rare and challenging to manage due to limited data, underscore the critical need for thorough screening, prompt recognition, and tailored treatment protocols to ensure optimal outcomes for both mother and fetus. [Read the Full Post]

Utilization, reimbursement, and price trends for Hepatitis C virus medications in the US Medicaid programs: 2001-2021

24 | Feb 10 2024

The study delineates the shifting landscape of HCV treatment from conventional therapies to expensive yet effective DAA agents, emphasizing the critical role of treatment guidelines and policies in influencing market dynamics and accessibility despite persistent challenges in affordability. [Read the Full Post]

Lithium chloride treatments in free flying honey bee colonies: efficacy, brood survival, and within-colony distribution

18 | Feb 08 2024

The study demonstrates the potential effectiveness of lithium chloride as an acaricide in honey bee colonies, showing high efficacy in eradicating Varroa destructor in both broodless and brood-containing colonies without long-term adverse effects, warranting further investigation for optimizing treatment duration to achieve consistently high efficacy. [Read the Full Post]

[Effect of aqueous extract of Corni Fructus on Aβ_(25-35)-induced brain injury and neuroinflammation in mice with Alzheimer's disease]

21 | Feb 08 2024

The study explored the impact of Corni Fructus extract on Aβ_(25-35)-induced Alzheimer's disease in mice, revealing its potential to ameliorate cognitive dysfunction, reduce brain injury, and modulate inflammatory responses via specific compounds within the extract. [Read the Full Post]

Purification of thioredoxin reductase from Spirulina platensis by affinity chromatography and investigation of kinetic properties

30 | Feb 05 2024

"In this study, TrxR enzyme from Spirulina platensis was successfully purified, characterized, and found to exhibit optimal activity at pH 7.0 and 40°C, demonstrating sensitivity to various metal ions, with Se4+ enhancing activity while others displayed inhibitory effects." [Read the Full Post]

Enhancing or Quenching of a Mitochondria-Targeted AIEgens-Floxuridine Sensor by the Regulation of pH-Dependent Self-assembly, Efficient Recognition of Hg2+, and Stimulated Response of GSH

50 | Feb 03 2024

The versatile TPE-FdU fluorescent probe, exhibiting pH-responsive behavior, selective Hg2+ ion detection, and intracellular mitochondrial visualization, represents a promising advancement with diverse applications in cell imaging, environmental monitoring, and biomedical research. [Read the Full Post]

Phase II study of bemnifosbuvir in high-risk participants in a hospital setting with moderate COVID-19

14 | Jan 24 2024

The study on bemnifosbuvir for moderate COVID-19, while not meeting its primary efficacy endpoint, demonstrated well-tolerance, absence of increased mortality, and a potential for reducing viral load, suggesting a promising avenue for further exploration in managing COVID-19 progression. [Read the Full Post]

An exonuclease-resistant chain-terminating nucleotide analogue targeting the SARS-CoV-2 replicase complex

14 | Jan 24 2024

The modification of Bemnifosbuvir into the α-thiotriphosphate form, AT-9052-Sp, not only evades viral exonuclease-mediated resistance but also demonstrates a unique mechanism of immediate chain termination against SARS-CoV-2, offering a promising strategy for overcoming viral proofreading mechanisms in antiviral drug development. [Read the Full Post]

Covid-19 co-infection with Crimean Congo haemorrhagic fever (CCHF) in a CCHF endemic country: a case report

46 | Jan 22 2024

In regions where both Crimean-Congo hemorrhagic fever and severe COVID-19 coexist, differentiating between the two diseases is vital due to their overlapping clinical presentations, emphasizing the importance of accurate diagnostic testing to guide appropriate treatment strategies. [Read the Full Post]

Mitochondrial complex I inhibition by homoharringtonine: A novel strategy for suppression of chronic myeloid leukemia

23 | Jan 18 2024

The rigorous evaluation of HHT's anti-CML effects, particularly its disruption of oxidative phosphorylation via mitochondrial complex I inhibition, unveils a promising therapeutic strategy to overcome resistance associated with the BCR-ABL T315I mutation. [Read the Full Post]

Inhibition of thioredoxin-1 enhances the toxicity of glycolysis inhibitor 2-deoxyglucose by downregulating SLC1A5 expression in colorectal cancer cells

12 | Jan 17 2024

The study reveals that Trx-1 mediates resistance to 2-deoxyglucose in colorectal cancer cells by upregulating SLC1A5, suggesting that targeting Trx-1 or SLC1A5 alongside glycolysis inhibition could offer a promising strategy for improving treatment efficacy. [Read the Full Post]

Clodronic Acid has Strong Inhibitory Interactions with the Urease Enzyme of Helicobacter Pylori: Computer-aided Design and in vitro Confirmation

20 | Jan 13 2024

Clodronic acid's robust inhibition of Helicobacter pylori urease, supported by computational screening and in vitro assays, positions it as a promising candidate for repurposing into an efficient drug against H. pylori infection. [Read the Full Post]

The ELAVL3/MYCN positive feedback loop provides a therapeutic target for neuroendocrine prostate cancer

32 | Jan 11 2024

The identification of ELAVL3 as a pivotal regulator in neuroendocrine prostate cancer, its interplay with MYCN, RICTOR mRNA, and extracellular vesicles, coupled with the efficacy of pyrvinium pamoate in suppressing tumor growth and improving survival, presents a promising avenue for targeted therapies and drug repurposing strategies in this aggressive cancer. [Read the Full Post]

Repurposing Polyether Ionophores as a New-Class of Anti-SARS-Cov-2 Agents as Adjunct Therapy

29 | Jan 11 2024

The repurposing of veterinary polyether ionophores, supported by in vitro and in vivo studies, demonstrates promising potential in inhibiting SARS-CoV-2 through multi-target interactions, synergized by Zn2+ supplementation, highlighting a compelling avenue for novel therapeutic strategies against COVID-19. [Read the Full Post]

Optimized M24B Aminopeptidase Inhibitors for CARD8 Inflammasome Activation

33 | Jan 07 2024

The development of CQ80 as a selective dual inhibitor of PEPD and XPNPEP1 presents a promising avenue to selectively activate the CARD8 inflammasome, offering a potent tool for studying its biology and therapeutic potential in inflammation-related conditions. [Read the Full Post]

Evaluation of Histone Demethylase Inhibitor ML324 and Acyclovir against Cyprinid herpesvirus 3 Infection

0 | Jan 03 2024

ML324 demonstrates significant potential as an effective treatment against Cyprinid herpesvirus 3 (CyHV-3) infection in koi fish, outperforming traditional antiviral drugs like acyclovir in inhibiting virus replication both in vitro and in vivo. [Read the Full Post]

Impact of antibiotic pharmacokinetics in urine on recurrent bacteriuria following treatment of complicated urinary tract infections

28 | Dec 21 2023

The prolonged urinary clearance and dwell time of ertapenem, compared to tebipenem, in a study evaluating complicated urinary tract infections, introduced a temporal difference in bacterial repopulation, potentially confounding the assessment of efficacy and contributing to the ongoing controversy regarding the clinical relevance of bacteriuria post-antibiotic treatment. [Read the Full Post]

Structure-Based Lead Optimization of Enterovirus D68 2A Protease Inhibitors

36 | Dec 13 2023

In this study, researchers elucidated the X-ray crystal structures of EV-D68 2Apro and its C107A mutant, utilized molecular dynamics simulations to predict the binding pose of telaprevir, and optimized its structure, leading to the discovery of potent 2Apro inhibitors with improved antiviral activity against Enterovirus D68. [Read the Full Post]

Phase 1b safety and pharmacokinetics of intravenous and oral fosmanogepix in patients with acute myeloid leukaemia and neutropenia

26 | Dec 13 2023

**In this Phase 1b study, fosmanogepix, administered intravenously and orally to acute myeloid leukemia patients with neutropenia undergoing chemotherapy, demonstrated excellent tolerability, with no serious adverse events, and exhibited consistent pharmacokinetic profiles, supporting its potential as a safe and effective antifungal treatment option.** [Read the Full Post]

Conditional lethality profiling reveals anticancer mechanisms of action and drug-nutrient interactions

13 | Dec 03 2023

The study screened anticancer and non-oncology compounds in conventional and Human Plasma-Like Medium, revealing a dual mechanism of action for brivudine in folate metabolism and identifying conditional phenotypes for various drugs, offering insights into exploiting conditional lethality for therapeutic candidate discovery. [Read the Full Post]

Entropy driven cooperativity effect in multi-site drug optimization targeting SARS-CoV-2 papain-like protease

13 | Nov 28 2023

The study investigated the enhanced binding affinity between the papain-like protease (PLpro) of SARS-CoV-2 and the existing drug GRL0617, revealing that optimization of specific regions in the drug led to increased cooperativity by stabilizing key residues and reducing entropic loss, providing valuable insights for drug development strategies targeting PLpro. [Read the Full Post]

Oridonin Synergistically Enhances the Pro-Apoptotic Effect of Venetoclax on Acute Myeloid Leukemia Cells by Inhibiting AKT Signaling

32 | Nov 23 2023

**Synergistic inhibition of AKT signaling by oridonin enhances the apoptotic effects of venetoclax, offering a promising combination therapy to overcome resistance and improve outcomes in acute myeloid leukemia.** [Read the Full Post]

Segmental Zoster Paresis Accompanied by Horner's Syndrome

143 | Nov 11 2023

In this case, a 90-year-old immunocompromised woman developed right upper limb weakness and Horner's syndrome following oral therapy for zoster on the right T2 dermatome, with aggressive intravenous treatment leading to improvement in the former but persistence of the latter. [Read the Full Post]

In silico molecular study of hepatitis B virus X protein as a therapeutic target

35 | Oct 25 2023

The study identified SC75741, Punicalagin, and Ledipasvir as promising antiviral compounds with strong binding affinity for the HBx protein, suggesting their potential for targeted inhibition of HBx and further research in Hepatitis B treatment. [Read the Full Post]

Deglycosylation of SLAMF7 in breast cancers enhances phagocytosis

20 | Oct 24 2023

This study demonstrates that targeting N-glycosylation of SLAMF7 through an antibody-drug conjugate can enhance antibody affinity and phagocytosis, potentially improving the response of immunotherapeutic agents in breast cancer treatment. [Read the Full Post]

SIRT6 ameliorates LPS-induced apoptosis and tight junction injury in ARDS through the ERK1/2 pathway and autophagy

40 | Oct 21 2023

SIRT6, through its regulation of the ERK1/2 pathway and enhancement of autophagy, demonstrates a beneficial role in acute respiratory distress syndrome (ARDS) by ameliorating tight junction protein loss, inflammation, and apoptosis, suggesting its potential as a therapeutic target for ARDS. [Read the Full Post]

Novel targets and inhibitors of the Mycobacterium tuberculosis cytochrome bd oxidase to foster anti-tuberculosis drug discovery

19 | Oct 15 2023

This review provides an overview of the structural, mechanistic, and inhibitory aspects of Mycobacterium tuberculosis cytochrome bd oxidase (cyt-bd), highlighting its potential as a target for the development of novel tuberculosis treatments. [Read the Full Post]

Atypical Anti-Glomerular Basement Membrane Nephritis After the First Dose of the Severe Acute Respiratory Syndrome Coronavirus 2 mRNA Vaccine

62 | Oct 13 2023

Atypical anti-GBM nephritis, which can occur after the administration of the SARS-CoV-2 mRNA vaccine, is characterized by linear IgG deposition in the glomerular basement membrane without circulating anti-GBM antibodies or lung involvement, and its response to immunosuppressive therapy is uncertain. [Read the Full Post]

Senescent immune cells accumulation promotes brown adipose tissue dysfunction during aging

18 | Oct 11 2023

Bone marrow-derived senescent immune cells expressing S100A8 infiltrate brown adipose tissue during aging, compromising axon networks and thermogenic function, but treatment with an S100A8 inhibitor rejuvenates these functions in aged mice. [Read the Full Post]

Solithromycin inhibits IL-13-induced goblet cell hyperplasia and MUC5AC, CLCA1, and ANO1 in human bronchial epithelial cells

19 | Oct 10 2023

Solithromycin was found to attenuate IL-13-induced goblet cell hyperplasia and MUC5AC production by inhibiting the mRNA and protein expression of CLCA1 and ANO1, independent of STAT6 and ERK phosphorylation. [Read the Full Post]

Construction and Validation of Protein Expression-related Prognostic Models in Clear Cell Renal Cell Carcinoma

65 | Oct 10 2023

The study developed a prognostic evaluation model for ccRCC patients using bioinformatics methods, identified 13 independent prognostic proteins, and demonstrated their strong predictive ability for patient survival, while also identifying potential drugs for targeted therapy. [Read the Full Post]

Tamoxifen resistance induction results in the upregulation of ABCG2 expression and mitoxantrone resistance in MCF-7 breast cancer cells

75 | Oct 07 2023

The study found that prolonged exposure of ER+ MCF-7 breast cancer cells to tamoxifen led to increased expression of the ABCG2 pump, associated with TAM resistance and potential cross-resistance to mitoxantrone. [Read the Full Post]

Antibiotic Susceptibility Profile of Bacteria Causing Aerobic Vaginitis in Women in Iraq

52 | Oct 06 2023

The study revealed high rates of antimicrobial resistance among bacterial isolates from women with aerobic vaginitis, with Gram-positive bacteria showing resistance to penicillins and cephalosporins and Gram-negative bacteria displaying resistance to multiple antibiotic classes. [Read the Full Post]

Estimation of Intangible Costs for Factors Associated with Oral Antiviral Drugs for COVID-19 Treatment: A Conjoint Analysis in Japan

0 | Sep 25 2023

This study conducted a conjoint analysis to estimate the intangible costs of factors associated with oral antiviral drugs for COVID-19 among the Japanese population, revealing preferences regarding the company, formulation, size, frequency of administration, infectiousness duration, and out-of-pocket expenses. [Read the Full Post]

Upgrading nirmatrelvir to inhibit SARS-CoV-2 Mpro via DeepFrag and free energy calculations

22 | Sep 25 2023

The hybrid approach combining machine learning and free energy simulations proposed six modified compounds derived from nirmatrelvir, which exhibited enhanced electrostatic interaction free energy with SARS-CoV-2 Mpro and potentially reduced toxicity compared to the original inhibitor. [Read the Full Post]

Orthogonal dual reporter-based gain-of-signal assay for probing SARS-CoV-2 3CL protease activity in living cells: inhibitor identification and mutation investigation

28 | Sep 22 2023

The researchers developed a dual reporter-based assay that measures the activity of the main protease of SARS-CoV-2, overcoming limitations of previous assays and identifying potential inhibitors while assessing the susceptibility of circulating variants. [Read the Full Post]

Semi-quantification and Potency Verification of the HIV Protease Inhibitor Based on the Matrix-Capsid Protein Immobilized Nickel (II)/NTA-Tol/Graphene Oxide/SPCE Electrochemical Biosensor

38 | Sep 15 2023

The study proposes a low-cost electrochemical biosensor platform for the semi-quantification and verification of HIV protease inhibitors, offering a potential solution to expedite the discovery and development of new HIV drugs. [Read the Full Post]

Estimation of Intangible Costs for Factors Associated with Oral Antiviral Drugs for COVID-19 Treatment: A Conjoint Analysis in Japan

24 | Sep 13 2023

This study conducted a conjoint analysis to estimate the intangible costs associated with factors of oral antiviral drugs for COVID-19 in Japan, revealing preferences such as a higher intangible cost for drugs developed by foreign companies and a lower cost for smaller sizes and tablets compared to larger sizes and capsules, respectively. [Read the Full Post]

ACSS2-mediated NF-κB activation promotes alkaliptosis in human pancreatic cancer cells

75 | Aug 13 2023

ACSS2, an enzyme involved in acetyl-coenzyme A production and histone acetylation, has been identified as a positive regulator of alkaliptosis in human pancreatic ductal adenocarcinoma cells, potentially offering new therapeutic strategies for PDAC treatment. [Read the Full Post]

C-C motif chemokine receptor 2 inhibition reduces liver fibrosis by restoring the immune cell landscape

37 | Aug 08 2023

Cenicriviroc (CVC) treatment and CCR2 deletion alleviate liver fibrosis by restoring the immune cell landscape, inhibiting the hepatic accumulation of inflammatory macrophages and neutrophils, and suppressing profibrotic gene transcription through inactivation of the CCR2-STAT1/NFκB/ERK signaling pathways. [Read the Full Post]

Tropifexor plus cenicriviroc combination versus monotherapy in non-alcoholic steatohepatitis: Results from the Phase 2b TANDEM study

57 | Aug 08 2023

The combination therapy of tropifexor (TXR) and cenicriviroc (CVC) did not show significant additional efficacy compared to respective monotherapies in terms of alanine aminotransferase (ALT) levels, body weight, or histological endpoints in the treatment of non-alcoholic steatohepatitis (NASH) in a phase 2b study. [Read the Full Post]

pH-sensitive smart indicators based on cellulose and different natural pigments for tracing kimchi ripening stages

166 | Jul 27 2023

The study found that cellulose-based pH-sensitive indicators loaded with natural pigments showed more pronounced color changes in response to lactic acid and pH variations, with alkalized indicators being particularly effective for monitoring the fermentation process of acidic foods such as kimchi. [Read the Full Post]

5-FU mediated depletion of myeloid suppressor cells enhances T-cell infiltration and anti-tumor response in immunotherapy-resistant lung tumor

137 | Jul 19 2023

Depletion of MDSCs using low-dose 5-fluorouracil (5-FU) chemotherapy showed significant anti-tumor effects by increasing the infiltration of CD8+ cytotoxic T-cells in a cold tumor model of Lewis Lung Carcinoma (LLC). [Read the Full Post]

The pattern of histone H3 epigenetic posttranslational modifications is regulated by the VRK1 chromatin kinase

0 | Jul 16 2023

The chromatin kinase VRK1 plays a crucial role in regulating the epigenetic patterns of histone H3 acetylation and methylation, thereby influencing chromatin organization and associated nuclear functions. [Read the Full Post]

Regulation, genomics, and clinical characteristics of cuproptosis regulators in pan-cancer

54 | Jul 16 2023

This study comprehensively elucidated the expression, prognostic significance, biological functions, genomic characteristics, immune microenvironment interactions, and drug sensitivity of cuproptosis regulators in pan-cancer, providing valuable insights into their potential role in cancer biology. [Read the Full Post]

Dynamin-independent CaV1.2 and KCa1.1 channels regulation and vascular tone modulation by the mitochondrial fission inhibitors dynasore and dyngo-4a

44 | Jul 15 2023

The study raises caution regarding the use of dynasore, mdivi-1, and dyngo-4a as tools to investigate the role of mitochondrial fission in vascular contraction, emphasizing the need for a selective dynamin inhibitor and/or alternative experimental approaches. [Read the Full Post]

Higher efficacy of Etoposide + Cytarabine Plus Pegfilgrastim in poorly mobilizing Multiple Myeloma and lymphoma Patients

64 | Jul 13 2023

The retrospective analysis suggests that chemo-mobilization with etoposide, cytarabine, and pegfilgrastim is a highly effective and tolerable strategy for mobilizing hematopoietic stem cells in poorly mobilizing patients with multiple myeloma (MM) or lymphoma. [Read the Full Post]

AMD3100-mediated CXCR4 inhibition impairs development of primary lymphoma of the central nervous system

133 | Jul 13 2023

The inhibition of CXCR4-CXCL12 interactions by AMD3100 in primary lymphoma of the central nervous system (PCNSL) downregulates CD200 expression in lymphoma cells, leading to increased microglial activation, impaired lymphoma cell invasion, and reduced tumor size, suggesting the potential therapeutic utility of AMD3100 in PCNSL. [Read the Full Post]

Efficacy of favipiravir against influenza virus resistant to both baloxavir and neuraminidase inhibitors

70 | Jul 09 2023

The study findings suggest that favipiravir should be used as a treatment option for patients suspected of having influenza virus infections resistant to NA inhibitors and baloxavir. [Read the Full Post]

A Facile Raman Spectroscopy Method for Online Monitoring of Crystal Plane Orientation of Favipiravir

132 | Jul 09 2023

This paper describes a facile method for online monitoring of the crystal plane orientation of favipiravir using Raman spectroscopy, providing a non-contact, fast, and sample preparation-free approach with potential applications in pharmaceutical processes. [Read the Full Post]

Proteasome Inhibition Sensitizes Liposarcoma to MDM2 Inhibition with Nutlin-3 by Activating the ATF4/CHOP Stress Response Pathway

96 | Jul 03 2023

The study suggests that combining MDM2 inhibitors with proteasome inhibitors could improve the efficacy of treatment for liposarcoma by inducing apoptosis through activation of the ATF4/CHOP stress response axis. [Read the Full Post]

Cabotegravir (Apretude) for Pre-exposure Prophylaxis for HIV Type 1 Infection

25 | Jun 27 2023

Cabotegravir (Apretude) is an extended-release injectable HIV-1 antiretroviral medication used as pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in HIV-negative individuals at high risk. [Read the Full Post]

Celastrol inhibits necroptosis by attenuating the RIPK1/RIPK3/MLKL pathway and confers protection against acute pancreatitis in mice

0 | Jun 27 2023

Celastrol demonstrates potential as a therapeutic agent for inhibiting necroptosis and reducing the severity of necroptotic-related diseases such as pancreatitis [Read the Full Post]

Efficacy and safety of long-acting cabotegravir versus oral tenofovir disoproxil fumarate-emtricitabine as HIV pre-exposure prophylaxis: A systematic review and meta-analysis

50 | Jun 26 2023

The study found that long-acting injectable cabotegravir (CAB-LA) was more effective than daily oral tenofovir disoproxil fumarate-emtricitabine (TDF-FTC) in preventing HIV infection among at-risk cisgender men who have sex with men (MSM) and transgender women who have sex with men. [Read the Full Post]

Cheminformatics-Based Study Identifies Potential Ebola VP40 Inhibitors

0 | Jun 17 2023

This study identified potential lead compounds, including natural-product-derived compounds and approved drugs, that have the potential to be developed as anti-Ebola drugs, pending further experimental testing. [Read the Full Post]

Wolbachia Ferrochelatase as a potential drug target against filarial infections

91 | Jun 16 2023

Targeting the ferrochelatase enzyme in Wolbachia's heme biosynthetic pathway presents a potential therapeutic strategy for filarial infections, leading to the discovery of four promising drug candidates that can inhibit the worms' growth and survival. [Read the Full Post]

DEEMD: Drug Efficacy Estimation Against SARS-CoV-2 Based on Cell Morphology With Deep Multiple Instance Learning

60 | Jun 07 2023

DEEMD is a computational pipeline using deep neural network models within a multiple instance learning framework to identify putative treatments effective against SARS-CoV-2 based on morphological analysis of the RxRx19a dataset. [Read the Full Post]

Aberrant m5C hypermethylation mediates intrinsic resistance to gefitinib through NSUN2/YBX1/QSOX1 axis in EGFR-mutant non-small-cell lung cancer

38 | Jun 07 2023

This study demonstrates that aberrant RNA m5C modification via the NSUN2-YBX1-QSOX1 axis plays a critical role in mediating intrinsic resistance to gefitinib in EGFR-mutant NSCLC. [Read the Full Post]

Characterization of a Novel Milk-Clotting Aspartic Protease from Penicillium sp. and Structural Explanation for its High Milk-Clotting Index

77 | Jun 06 2023

PsMCE is a novel milk-clotting enzyme with specific hydrolysis activity on κ-casein proteins and potential applications in cheese making due to its thermolability and high milk-clotting index value. [Read the Full Post]

Canine distemper virus N protein induces autophagy to facilitate viral replication

62 | Jun 06 2023

This study revealed that CDV N protein induces complete autophagy to facilitate viral replication, providing new insights into the interaction between CDV and the host autophagy machinery. [Read the Full Post]

Phytochemical characterization, antioxidant activity and antihypertensive evaluation of Ocimum basilicum L. in l-NAME induced hypertensive rats and its correlation analysis

90 | Jun 05 2023

The study found that Ocimum basilicum Linn. leaves extracts have potential as antihypertensive drugs due to their bioactive metabolites, with phenolic compounds playing a role in inhibiting l-Name induced hypertension and flavonoids contributing to antioxidant activities. [Read the Full Post]

Kv1.3 blockade by ShK186 modulates CD4+ effector memory T-cell activity of patients with Granulomatosis with polyangiitis

49 | May 19 2023

The study suggests that Kv1.3 blockade using ShK-186 may be a potential treatment strategy for GPA by modulating the activity of CD4+TEM cells and reducing the production of pro-inflammatory cytokines, with less harmful side effects than current immunosuppressive regimens. [Read the Full Post]

SMAC Mimetics Synergistically Cooperate with HDAC Inhibitors Enhancing TNF-α Autocrine Signaling

33 | May 18 2023

The combination of SMAC mimetics and HDAC inhibitors shows remarkable synergy in suppressing IAP proteins and restoring apoptotic pathways, providing a potential therapeutic strategy for recurrent ovarian cancer. [Read the Full Post]

Mutiple myeloma resistant to melphalan (NSC-8806) treated with cyclophosphamide (NSC-26271), prednisone (NSC-10023), and chloroquine (NSC-187208)

41 | May 17 2023

This prospective randomized study compared the effectiveness of two therapeutic regimens in 41 patients with multiple myeloma resistant to melphalan, with no significant differences in response or toxicity observed between the groups, despite the addition of chloroquine to one regimen. [Read the Full Post]

A myeloid leukemia factor homolog is involved in tolerance to stresses and stress-induced protein metabolism in Giardia lamblia

37 | May 16 2023

This study investigated the role of MLF vesicles in G. lamblia and found that they share similar stress-induced characteristics with autophagy compartments and are important for survival in stress conditions. [Read the Full Post]

Efficient production of recombinant proteins in suspension CHO cells culture using the Tol2 transposon system coupled with cycloheximide resistance selection

31 | May 16 2023

The study demonstrates an efficient method for producing therapeutic proteins using DNA recombination techniques in mammalian cells, combining the Tol2 transposon system and cell selection by cycloheximide resistance to produce stable cell lines with constant productivity and cell growth suitable for commercial production. [Read the Full Post]

Comparative analysis of pre-existing HIV drug resistance mutations in proviral DNA via Next-Generation Sequencing and routine HIV RNA genotyping

100 | May 08 2023

The study found that deep sequencing of archived HIV DNA can detect transmitted drug resistance mutations that are not identified by routine bulk sequencing, including low-frequency mutations that could become dominant under drug selection pressure. [Read the Full Post]

Lipids and transaminase elevations in ARV-experienced PLWH switching to a doravirine-based regimen from rilpivirine or other regimens

16 | May 07 2023

The study found that the lipid-lowering effect of DOR in people living with HIV was observed in those switching from other NNRTIs and INSTI-including regimens, but not in those switching from RPV, suggesting that the effect is drug class-related. [Read the Full Post]

Stability-Indicating Method Development and Validation for Quantitative Estimation of Assay and Organic Impurities of anti-viral drug Baloxavir-Marboxil in Drug Substance and Pharmaceutical Dosage Form using HPLC and LC-MS Methods

71 | May 06 2023

A liquid chromatographic method was developed and validated for estimating the assay and impurities of Baloxavir-Marboxil in drug substance and pharmaceutical formulations, demonstrating reliable and robust separation of known and unknown impurities and stability-indicating properties. [Read the Full Post]

Cheminformatics-Based Study Identifies Potential Ebola VP40 Inhibitors

37 | May 05 2023

This study used an in silico approach to identify potential small molecule inhibitors of the Ebola virus by targeting the N-terminal domain of VP40, resulting in the identification of several natural-product-derived compounds and approved drugs with potential anti-EBOV activity that can be further explored for EVD treatment. [Read the Full Post]

Long-term follow-up of HCV-infected patients with end-stage chronic kidney disease after sustained virological response with direct-acting antiviral therapy

48 | May 04 2023

The study found that although HCV cure may play a positive role in renal function in CKD stage 3b-4, long-term mortality remained high among end-stage CKD patients, with no improvement in renal function observed and a high proportion of patients requiring kidney transplantation. [Read the Full Post]

Potential drug candidates as P-glycoprotein inhibitors to reverse multidrug resistance in cancer: an in silico drug discovery study

28 | May 04 2023

This study aimed to identify potential P-glycoprotein inhibitors for the treatment of carcinoma using in silico techniques, and identified five promising drug candidates with high binding energies and good pharmacokinetic properties. [Read the Full Post]

Dasabuvir suppresses esophageal squamous cell carcinoma growth in vitro and in vivo through targeting ROCK1

27 | May 03 2023

The discovery that dasabuvir, an FDA-approved drug for HCV treatment, acts as a ROCK1 inhibitor and suppresses ESCC growth through blocking ROCK1/ERK signaling pathway provides a promising candidate for further investigation as an anti-cancer therapy for ESCC. [Read the Full Post]

Structural and functional characterization of RNA dependent RNA polymerase of Macrobrachium rosenbergii nodavirus (MnRdRp)

34 | May 03 2023

The study provides insights into the structure and potential drug targeting of MnRdRp, the RNA-dependent RNA polymerase of the MrNV virus that causes white tail disease in farmed Macrobrachium rosenbergii. [Read the Full Post]

The effect of different direct antivirals on hepatic steatosis in nondiabetic and naïve hepatitis C-infected Egyptian patients

35 | May 03 2023

This study found that achieving sustained virological response after 12 weeks of treatment with direct antiviral drugs improved the metabolic profile and reduced hepatic steatosis and fibrosis in nondiabetic, chronically infected HCV Egyptian patients naive to any form of HCV treatment, but was also associated with an increase in LDL mostly due to viral-host molecular interaction. [Read the Full Post]

Efficacy and safety of ombitasvir/paritaprevir/ritonavir-based therapy in HCV patients with chronic kidney disease

38 | May 03 2023

The study showed that ombitasvir/paritaprevir/ritonavir-based therapy is highly effective and safe in chronic HCV patients with CKD, with the highest SVR achieved with ombitasvir/paritaprevir/ritonavir plus ribavirin. [Read the Full Post]

Assessment of alteration in antiviral plasma concentration across dialysis days: computational and analytical study

35 | May 03 2023

This study found that protein-bound uremic toxins have a lower binding affinity than directly acting antivirals, indicating a reduced liability of competitive displacement and suggesting that PBUT accumulation may have limited effect on the disposition of DAAs. [Read the Full Post]

A large-scale functional analysis of genes expressed differentially in insulin secreting MIN6 sublines with high versus mildly reduced glucose-responsiveness

43 | May 01 2023

This study identified 18 genes that altered glucose-stimulated insulin secretion (GSIS) in pancreatic β-cells, and confirmed Sox11 as a negative regulator of insulin secretion and its role in glucose metabolism. [Read the Full Post]

Acceptability of a new 4-in-1 Abacavir/Lamivudine/Lopinavir/Ritonavir paediatric fixed-dose combination: the caregiver-child dyads' perspective

85 | May 01 2023

The study found that caregivers in Uganda found the new 4-in-1 strawberry-flavoured granules formulation highly acceptable for children living with HIV compared to previous formulations, with factors such as appealing taste, ease of administration, and comprehensive healthcare provider support contributing to its acceptability. [Read the Full Post]

An indirect comparison of 144-week efficacy, safety, and tolerability of dolutegravir plus lamivudine and second-generation integrase inhibitor-based, 3-drug, single-tablet regimens in therapy-naive people with HIV-1

19 | May 01 2023

The study found that the 2-drug regimen of dolutegravir (DTG) + lamivudine (3TC) offers comparable and durable efficacy with fewer serious adverse events compared to two 3-drug single-tablet regimens in antiretroviral therapy-naive people with HIV-1 at Week 144 after treatment initiation. [Read the Full Post]

Factors Associated With Adherence to First-line Antiviral Therapy Among Commercially Insured Patients With Chronic Hepatitis B

22 | May 01 2023

The study found that longer-duration supplies of entecavir and TDF and use of mail order pharmacies may improve adherence among patients with CHB, while high out-of-pocket costs for TDF were associated with reduced medication adherence. [Read the Full Post]

Tuberculosis: Pathogenesis, Current Treatment Regimens and New Drug Targets

49 | Apr 30 2023

Tuberculosis (TB) caused by Mycobacterium tuberculosis is a global health concern that requires the development of new anti-TB drugs due to the emergence of drug-resistant strains and the challenges of current treatment protocols. [Read the Full Post]

Development of UPLC method for simultaneous assay of some COVID-19 drugs utilizing novel instrumental standard addition and factorial design

31 | Apr 30 2023

The proposed method is a green, rapid, and simple RP-UPLC method developed and optimized by full factorial design for the simultaneous separation of oseltamivir phosphate, daclatasivir dihydrochloride, and remdesivir, with dexamethasone as a co-administered drug, and it demonstrated linearity, precision, and accuracy with low limits of quantitation and detection, and high percentage recoveries, making it an eco-friendly and efficient analytical procedure. [Read the Full Post]

Use of In Vivo Imaging and Physiologically-Based Kinetic Modelling to Predict Hepatic Transporter Mediated Drug-Drug Interactions in Rats

36 | Apr 29 2023

The study investigated the effect of six drugs on the transport of gadoxetate in rats using PBPK modelling and tracer-kinetic models, demonstrating a framework for prospective quantification of hepatic transporter-mediated DDI in humans. [Read the Full Post]

Analysis of Hepatitis C Virus Resistance-Associated Substitutions in Direct-Acting Antiviral Failure in South Korea Using Next-Generation Sequencing

27 | Apr 29 2023

This study found that retreatment with pan-genotypic DAA was highly successful in Korean patients with chronic HCV infection who failed initial DAA treatment, despite the presence of baseline or treatment-emergent RAS. [Read the Full Post]

JAK inhibitors for rheumatoid arthritis

88 | Apr 29 2023

JAK inhibitors represent a promising class of drugs for the treatment of rheumatoid arthritis, with varying degrees of selectivity for different JAK isoforms, and precision medicine approaches may enhance their effectiveness in the future. [Read the Full Post]

Glucose induced-AKT/mTOR activation accelerates glycolysis and promotes cell survival in acute myeloid leukemia

40 | Apr 28 2023

The study found that glucose-induced AKT/mTOR activation promotes AML growth and inhibition of glycolysis may be a potential therapy strategy for AML. [Read the Full Post]

The usefulness of pretreatment controlling nutritional status score for predicting recurrence in patients with esophageal squamous cell carcinoma undergoing neoadjuvant immunochemotherapy: A real-world study

36 | Apr 28 2023

The study suggests that the controlling nutritional status (CONUT) score is a reliable prognostic indicator in esophageal squamous cell carcinoma (ESCC) patients undergoing neoadjuvant immunochemotherapy (nICT), with a low pretreatment CONUT score associated with a better response to treatment and a lower recurrence rate. [Read the Full Post]

Relating CYP2B6 genotype and efavirenz resistance among post-partum women living with HIV with high viremia in Uganda: a nested cross-sectional study

42 | Apr 27 2023

The study investigated the association between CYP2B6 polymorphisms and efavirenz drug resistance among women living with HIV who started on antiretroviral therapy during pregnancy and had high viremia in the postpartum period, and found no statistically significant difference in EFV resistance between EFV metabolizer genotypes, but a numerical trend was observed, calling for further confirmation in a large, well-designed, statistically powered study. [Read the Full Post]

Positron Emission Tomography Imaging in Vasculitis

80 | Apr 27 2023

FDG-PET/CT is an important imaging tool in the diagnosis and therapeutic monitoring of vasculitides affecting large-sized and medium-sized vessels, and with advancements in newer generation scanners and development of novel tracers, it has shown significant potential in accurately assessing the full disease extent and detecting vascular infiltrates. [Read the Full Post]

Highly Sensitive Imaging of Tumor Metastasis Based on the Targeting and Polarization of M2-like Macrophages

77 | Apr 26 2023

This research developed a nanoprobe that targets M2-like macrophages to track their migration and polarization in real-time during tumor metastasis, revealing their critical role in early tumor metastasis. [Read the Full Post]

Comparison of in vitro Susceptibilities of Talaromyces marneffei in Mold and Yeast Forms in Malaysia

29 | Apr 25 2023

The study found that the susceptibility of T. marneffei to most antifungal drugs was similar for both yeast and mold forms, except for caspofungin and micafungin, which had significant differences in GM MIC. [Read the Full Post]

Plasma and Cerebrospinal Fluid Concentrations of Micafungin Administered at High Doses in Critically Ill Infants with Systemic Candidiasis: A Pooled Analysis of Two Studies

43 | Apr 25 2023

The pharmacokinetics of micafungin were analyzed in 53 neonates with systemic candidiasis, revealing that neonates may require higher doses of micafungin than adults to reach therapeutic levels, and micafungin crosses the blood-brain barrier reaching therapeutic levels in CSF with doses ranging between 8 and 15 mg/kg/day. [Read the Full Post]

Auranofin Targeting the NDM-1 Beta-Lactamase: Computational Insights into the Electronic Configuration and Quasi-Tetrahedral Coordination of Gold Ions

63 | Apr 25 2023

Recent research has demonstrated that auranofin can restore penicillin and cephalosporin sensitivity in resistant bacterial strains via the inhibition of the NDM-1 beta-lactamase enzyme, accomplished through substituting gold for zinc in the enzyme's bimetallic core. [Read the Full Post]

Therapeutic Options for Adult Patients With Persistent Methicillin-Susceptible Staphylococcus aureus Bacteremia: A Narrative Review

72 | Apr 25 2023

The available evidence suggests that a combination of antibiotics targeting MSSA, along with source control measures and consultation with an infectious diseases specialist, may be necessary to effectively manage persistent MSSA bacteremia. [Read the Full Post]

Pioneer Use of Antimalarial Transdermal Combination Therapy in Rodent Malaria Model

29 | Apr 25 2023

The study found that transdermal N-89 combined with mefloquine or pyrimethamine provided a promising antimalarial form for children, with a synergistic effect and better antimalarial activity and cure effect compared to N-89 alone or combined with chloroquine. [Read the Full Post]

Characterization of the Interactions between Minocycline Hydrochloride and Trypsin with Spectroscopic and Molecular Docking Technology

85 | Apr 24 2023

This study investigated the interaction between minocycline hydrochloride and trypsin using various spectroscopic and molecular docking techniques and demonstrated its impact on the secondary structure of trypsin. [Read the Full Post]

The CNC-family transcription factor Nrf3 coordinates the melanogenesis cascade through macropinocytosis and autophagy regulation

69 | Apr 24 2023

The research shows that the transcription factor Nrf3 regulates macropinocytosis and autophagy to coordinate melanogenesis, and has potential therapeutic implications for hyperpigmentation disorders and as an anti-melanogenic target in HIV-1 infected individuals taking nelfinavir. [Read the Full Post]

Targeting chromosome 12q amplification in relapsed glioblastoma: the use of computational biological modeling to identify effective therapy-a case report

66 | Apr 24 2023

The case report demonstrates the utility of biosimulation in identifying effective treatment options based on comprehensive genomic abnormalities and highlights a promising treatment combination for GBM and potentially other cancers harboring chromosome 12q amplification. [Read the Full Post]

PK/PD modeling and simulation of the in vitro activity of the combinations of isavuconazole with echinocandins against Candida auris

45 | Apr 24 2023

The study used a pharmacokinetic/pharmacodynamic modeling and simulation approach based on in vitro data to predict the in vivo response to combination therapy against Candida auris, highlighting the importance of bridging in vitro results to the clinic. [Read the Full Post]

Toxicity interactions of azole fungicide mixtures on Chlorella pyrenoidosa

79 | Apr 23 2023

The study investigated the combined toxicities and toxic interactions of 225 binary mixtures and 126 multi-component mixtures of 10 azole fungicides on Chlorella pyrenoidosa, finding that the toxicity interactions at low concentrations are dominated by additive effects, while at high concentrations, both synergistic and antagonistic effects are observed, with epoxiconazole inducing synergistic effects and clotrimazole inducing antagonistic effects. [Read the Full Post]

The Chinese herbal prescription JieZe-1 inhibits caspase-1-dependent pyroptosis induced by herpes simplex virus-2 infection in vitro

17 | Apr 23 2023

The study found that JieZe-1 (JZ-1) inhibits caspase-1-dependent pyroptosis induced by herpes simplex virus type 2 (HSV-2) infection and has excellent anti-HSV-2 activity in VK2/E6E7 cells. [Read the Full Post]

Multifunctional porous poly (L-lactic acid) nanofiber membranes with enhanced anti-inflammation, angiogenesis and antibacterial properties for diabetic wound healing

102 | Apr 22 2023

The study developed porous PLA/SCS/PDA-GS nanofiber membranes with enhanced antibacterial, anti-inflammatory, and angiogenic properties, demonstrating promising potential in diabetic wound healing processes. [Read the Full Post]

Assessing the risk of adverse pregnancy outcomes and birth defects reporting in women exposed to ganciclovir or valganciclovir during pregnancy: a pharmacovigilance study

71 | Apr 22 2023

The analysis of VigiBase found no evidence of increased risk of adverse pregnancy outcomes or birth defects associated with the use of (val)ganciclovir compared to (val)aciclovir during pregnancy, with the exception of four cases of oesophageal and anorectal atresia that require further analysis. [Read the Full Post]

SARS-CoV-2 Main Protease Drug Design, Assay Development, and Drug Resistance Studies

106 | Apr 21 2023

This Account describes efforts to develop covalent and noncovalent inhibitors of the SARS-CoV-2 main protease and the identification of nirmatrelvir-resistant mutants, providing guidance for the development of effective antivirals against COVID-19. [Read the Full Post]

Budget impact analysis of two treatment approaches for hepatitis C in Malaysia through the use of voluntary and compulsory licensing options

37 | Apr 20 2023

The study suggests that a stratified treatment cascade with SOF/VEL for cirrhotic patients and SOF/DAC for non-cirrhotic patients in Malaysia is a cost-saving approach. [Read the Full Post]

Safety and efficacy of elbasvir/grazoprevir in patients infected with hepatitis C virus genotype 4 in Qassim region of Saudi Arabia

17 | Apr 20 2023

The study found that the elbasvir/grazoprevir (EBR-GZR) treatment regimen for 12 weeks is safe and effective in achieving sustained virological response (SVR12) in HCV genotype 4-infected treatment-naïve Saudi patients, with improvement in prognostic markers of liver disease in participants with compensated cirrhosis. [Read the Full Post]

Bacterial species and antimicrobial resistance differ between catheter and non-catheter-associated urinary tract infections: Data from a national surveillance network

43 | Apr 19 2023

The study found that CAUTI pathogens were more often resistant to recommended empirical antibiotics than non-CAUTI pathogens, emphasizing the need for urine sampling for culturing before initiating therapy for CAUTI and the importance of considering therapeutic alternatives. [Read the Full Post]

The effect of pentosan polysulfate sodium for improving dyslipidaemia and knee pain in people with knee osteoarthritis: A pilot study

68 | Apr 18 2023

The study found that pentosan polysulfate sodium (PPS) has promising effects on improving dyslipidemia and providing symptomatic pain relief in people with knee osteoarthritis (OA), but further studies with larger sample sizes and more rigorous study designs are needed to confirm these findings. [Read the Full Post]

An Overview of Antivirals against Monkeypox Virus and Other Orthopoxviruses

24 | Apr 17 2023

The approval of tecovirimat and brincidofovir for smallpox treatment, and their demonstrated efficacy against monkeypox, has reignited interest in the development of orthopoxvirus antivirals to combat potential outbreaks of related viruses. [Read the Full Post]

Low level of antifungal resistance in Candida species recovered from Iranian HIV-associated oral infection

49 | Apr 16 2023

The study found a high prevalence of oral candidiasis among PLWHA following HAART, and highlighted the need to understand the mechanisms of reduced susceptibility and low-level resistance in Candida species and consider local epidemiology in their management. [Read the Full Post]

Echinocandin Resistance in Candida auris Occurs in the Murine Gastrointestinal Tract Due to FKS1 Mutations

35 | Apr 16 2023

The study found that Candida auris isolates with FKS1 mutations were resistant to echinocandins in vivo, including micafungin and caspofungin, and that mutations in R1354 resulted in in vivo resistance despite remaining below the micafungin breakpoint in vitro. [Read the Full Post]

Investigation of the impact of rosuvastatin and telmisartan in doxorubicin-induced acute cardiotoxicity

84 | Apr 15 2023

The study found that pre-treatment with rosuvastatin and telmisartan, alone or in combination, showed significant cardio-protective effects against the acute cardiotoxicity induced by doxorubicin. [Read the Full Post]

A systemic review on medicinal plants and their bioactive constituents against avian influenza and further confirmation through in-silico analysis

109 | Apr 14 2023

The review provides information on natural plant sources for combating avian influenza in chickens and identifies potential targets for future drug development. [Read the Full Post]

An efficient transformation method for tannin-containing sorghum

94 | Apr 14 2023

The successful establishment of an efficient microprojectile transformation system for tannin-containing sorghum using immature embryos of Hongyingzi as explants offers the possibility of breaking the restriction imposed by tannins in plants and improving the nutritional value and potential of sorghum as a food and feed crop. [Read the Full Post]

A Versatile Toolset for Genetic Manipulation of the Wine Yeast Hanseniaspora uvarum

59 | Apr 14 2023

The passage describes the development of a toolset for efficient and targeted genetic manipulation of the yeast species Hanseniaspora uvarum, which includes the creation of homozygous auxotrophic deletion markers, self-replicating cloning vectors, and a chemical transformation procedure. [Read the Full Post]

A highly efficient genetic transformation system for broccoli and subcellular localization

72 | Apr 12 2023

This study provides new insights into the improvement of the genetic transformation and molecular breeding of broccoli, which could lead to the development of improved crop varieties with enhanced traits. [Read the Full Post]

Interaction of copper potential metallodrugs with TMPRSS2: A comparative study of docking tools and its implications on COVID-19

21 | Apr 10 2023

The research on Casiopeina-analogs as TMPRSS2 inhibitors and their interaction with the catalytic triad provides valuable insights into potential drug candidates for treating COVID-19. [Read the Full Post]

Omicron-induced interferon signalling prevents influenza A H1N1 and H5N1 virus infection

93 | Apr 09 2023

Recent research shows that Omicron but not Delta induces a strong interferon response in primary human cells, protects cells from super-infection with influenza A viruses, and the response is mediated via MDA5 recognition of double-stranded RNA and involves the production of biologically active type I (α/β) and III (λ) interferons. [Read the Full Post]

Excellent Repigmentation of Generalized Vitiligo with Oral Baricitinib Combined with NB-UVB Phototherapy

67 | Apr 09 2023

Oral baricitinib combined with NB-UVB phototherapy has shown to be a successful treatment option for refractory vitiligo by blocking the JAK-STAT pathway and stimulating melanocyte production. [Read the Full Post]

The cytotoxic activity of carfilzomib together with nelfinavir is superior to the bortezomib/nelfinavir combination in non-small cell lung carcinoma

52 | Apr 09 2023

Combining carfilzomib with nelfinavir shows superior efficacy in inducing proteotoxicity and endoplasmic reticulum stress in non-small-cell-lung carcinoma (NSCLC) compared to the combination of bortezomib and nelfinavir, and may represent a future treatment option for NSCLC. [Read the Full Post]

Design, synthesis and bioevaluation of 1,2,4-thiadiazolidine-3,5-dione derivatives as potential GSK-3β inhibitors for the treatment of Alzheimer's disease

117 | Apr 07 2023

The development of compound 10a as a potential GSK-3β inhibitor for Alzheimer's disease shows promising results in vitro and in vivo. [Read the Full Post]

Preclinical pharmacologic evaluation of geldanamycin as an antitumor agent

58 | Mar 31 2023

The passage describes the pharmacokinetics of geldanamycin in mice and a dog and highlights the potential for acute hepatotoxic reactions, indicating a need for further pharmacological and therapeutic information before considering the drug for clinical development. [Read the Full Post]

Identification of significant gene expression changes in multiple perturbation experiments using knockoffs

113 | Mar 30 2023

The approach described uses the model-X knockoffs framework and Deep Neural Networks to identify significant gene expression changes in multiple perturbation experiments, allowing for better understanding of underlying mechanisms of disease and identification of new drug targets. [Read the Full Post]

Acute Care Management of the HIV-Infected Patient: A Report from the HIV Practice and Research Network of the American College of Clinical Pharmacy

16 | Mar 28 2023

This report provides guidance for clinicians managing HIV-infected patients and antiretroviral therapy in the inpatient setting, highlighting the need for a thorough medication history, consideration of drug-drug interactions and organ dysfunction, and timely follow-up to prevent medication errors and readmissions. [Read the Full Post]

Iatrogenic Cushing's Syndrome: The Result of Cobicistat and Glucocorticoid Interaction in an HIV Patient After Bariatric Surgery

31 | Mar 27 2023

The case report describes a patient with HIV-hepatitis C virus co-infection who developed iatrogenic Cushing's syndrome due to an interaction between cobicistat-boosted darunavir and inhaled corticosteroids after undergoing sleeve gastrectomy for morbid obesity. [Read the Full Post]

Systemic Capillary Leak Syndrome Induced by Influenza Type A Infection: A Case Report

53 | Mar 25 2023

This case highlights the potential for severe complications with influenza, including rhabdomyolysis and systemic capillary leak syndrome, and emphasizes the importance of prompt recognition and intensive care management. [Read the Full Post]

Antibiotic cement-coated rigid locked nails in infected femoral and tibial nonunion. Reoperation rates of commercial versus custom-made nails

26 | Mar 24 2023

This retrospective study assessed bone union, infection control, and reoperation rates in patients with infected femoral or tibial nonunion treated with antibiotic-cement-coated rigid nails and found that custom-made nails had a higher risk of reoperation compared to commercial nails loaded with gentamicin cement. [Read the Full Post]

Selective inhibition of HDAC6 promotes bladder cancer radiosensitization and mitigates the radiation-induced CXCL1 signalling

67 | Mar 20 2023

This study found that selective inhibition of histone deacetylase 6 (HDAC6) can enhance the radiosensitivity of bladder cancer cells and suppress radiation-induced oncogenic signaling, suggesting its potential as a therapeutic strategy in combination with radiation therapy. [Read the Full Post]

The effect of lipid-lowering therapies on the pro-inflammatory and anti-inflammatory properties of vascular endothelial cells

44 | Mar 16 2023

The study found that both statins, particularly rosuvastatin, had a stronger anti-inflammatory effect than ezetimibe in endothelial cells damaged by 25-hydroxycholesterol. [Read the Full Post]

Mechanistic in vitro studies indicate that the clinical drug-drug interactions between protease inhibitors and rosuvastatin are driven by inhibition of intestinal BCRP and hepatic OATP1B1 with minimal contribution from OATP1B3, NTCP and OAT3

33 | Mar 15 2023

This passage describes the use of a mechanistic static model to reconcile the disconnect between predicted and clinically observed area under the plasma concentration-time curve ratio (AUCR) of rosuvastatin due to drug-drug interaction (DDI) with atazanavir, by evaluating the inhibitory effects of atazanavir and other protease inhibitors on additional transporters, and integrating a combined hepatic transport component into the model. [Read the Full Post]

In silico prediction of potential inhibitors for SARS-CoV-2 Omicron variant using molecular docking and dynamics simulation-based drug repurposing

29 | Mar 13 2023

The study aimed to identify potential drugs against Omicron by testing previously repurposed anti-COVID-19 drugs, and raltegravir and hesperidin were found to have high binding affinities and stabilities to Omicron and may be potential drugs, but further clinical studies are needed to confirm their efficacy and safety. [Read the Full Post]

Multivariate Chemometric Comparison of Forced Degradation and Electrochemical Oxidation LC-MS Profiles of Maraviroc

74 | Mar 12 2023

The study found that maraviroc is susceptible to UVA, H2O2, and electrochemical degradation, and suggests that electrochemical methods can be used as a supplement to forced degradation procedures for a quicker and relatively low-cost alternative. [Read the Full Post]

TGFβ1+CCR5+ neutrophil subset increases in bone marrow and causes age-related osteoporosis in male mice

43 | Mar 12 2023

The study suggests that reducing the numbers of TGFβ1+CCR5+ neutrophils in the bone marrow, potentially through the use of a CCR5 antagonist like maraviroc, could be a treatment for age-related osteoporosis. [Read the Full Post]

Alginate oligosaccharides enhance the antifungal activity of nystatin against candidal biofilms

77 | Mar 11 2023

The study demonstrates the potential clinical utility of OligoG in conjunction with nystatin against Candida spp. in the prevention and topical treatment of candidal biofilm infections. [Read the Full Post]

Surface-Functionalized Metal-Organic Frameworks for Binding Coronavirus Proteins

43 | Mar 11 2023

The research proposes using metal-organic frameworks (MOFs) functionalized with repurposed antiviral agents to selectively bind and deactivate respiratory coronaviruses, highlighting their potential in combating future pandemics. [Read the Full Post]

Optimizing ganciclovir and valganciclovir dosing regimens in pediatric patients with cytomegalovirus infection: a spotlight on therapeutic drug monitoring

27 | Mar 10 2023

Therapeutic drug monitoring (TDM) has the potential to improve the efficacy and safety of ganciclovir/valganciclovir use in pediatrics, but further studies are necessary to establish optimal dosing regimens and evaluate the clinical impact of TDM. [Read the Full Post]

Treatment of Congenital Cytomegalovirus and Ganciclovir Therapeutic Drug Monitoring in Twin Preterm Infants

18 | Mar 10 2023

The case report highlights the importance of individualized treatment and close monitoring in premature infants with congenital cytomegalovirus infection, and the use of therapeutic drug monitoring to adapt to their evolving physiologic maturation. [Read the Full Post]

Emerging drug targets for sickle cell disease: shedding light on new knowledge and advances at the molecular level

86 | Mar 10 2023

Understanding early events in sickle cell disease pathogenesis associated with the presence of hemoglobin S is crucial for identifying new targets for treatment, including reducing HbS levels, reducing the impact of HbS polymers, and targeting membrane events, and exploiting the unique permeability of sickle cells for developing targeted therapies. [Read the Full Post]

DTIC (nsc-45388) and combination therapy for melanoma. I. Studies with DTIC, BCNU (NSC-409962), CCNU (NSC-79037), vincristine (NSC-67574), and hydroxyurea (NSC-32065)

49 | Mar 10 2023

The study found that combination chemotherapy regimens can improve response rates and survival times in patients with metastatic malignant melanoma, but careful monitoring of toxicity is necessary and treatment decisions should be individualized based on the patient's clinical profile. [Read the Full Post]

Effect of hybrid compounds of stilbene and pentadienone on inhibition of tubulin polymerization

99 | Mar 09 2023

The study designed and synthesized hybrid compounds with excellent anticancer properties that inhibit tubulin polymerization and induce cell cycle arrest in MDA-MB-231 human breast cancer cells. [Read the Full Post]

Evaluation of cytomegalovirus infection/disease in IgG positive renal transplantation recipients on valaciclovir prophylaxis

42 | Mar 09 2023

This study found that valacyclovir may be a preferable prophylaxis for CMV infection in renal transplant recipients due to its efficacy and fewer side effects compared to valganciclovir. [Read the Full Post]

Chemotherapeutic Activity of Pitavastatin in Vincristine Resistant B-Cell Acute Lymphoblastic Leukemia

53 | Mar 07 2023

The study suggests that pitavastatin may have potential as a repurposed chemotherapeutic agent for vincristine-resistant B-cell acute lymphoblastic leukemia. [Read the Full Post]

Predict the Effects of Dolutegravir (DTG) Plus Lamivudine (3TC) on Immunological Responses in People Living with HIV (PLWHIV)

28 | Mar 05 2023

The study identified factors that limit or enhance immune recovery in PLWHIV after switching to DTG plus 3TC and may help clinicians predict treatment effects on immunological responses before the switch. [Read the Full Post]

Long-term clinical, immunologic, and virologic outcomes among early-treated children with HIV in Botswana: a nonrandomized controlled clinical trial

24 | Mar 05 2023

The Early Infant Treatment Study in Botswana found that initiating antiretroviral treatment in the first week of life led to positive clinical outcomes and low viral reservoir through 96 weeks, with pre-ART reservoir size at birth predicting the viral reservoir at 84/96 weeks. [Read the Full Post]

Substrate binding and lipid-mediated allostery in the human organic anion transporter 1 at the atomic-scale

57 | Mar 05 2023

The study investigated hOAT1 transport function, modulation of activity, and transport dysfunctions arising from mutations using molecular dynamics simulations and proposed a structural rationalization of the observations. [Read the Full Post]

Efficacy of nucleos(t)ide analogues(NAs) in preventing virus reactivation in oncology patients with HBV infection after chemotherapy or surgery: A network meta-analysis

28 | Mar 05 2023

This study used a network meta-analysis to compare the effectiveness of different NAs in reducing reactivation of HBV, chemotherapy disruption, and improving survival in oncology patients with HBV, finding that lamivudine and entecavir were effective in prolonging survival, while tenofovir was best for reducing chemotherapy disruption. [Read the Full Post]

First report of rot disease in Prunus salicina var. taoxingli fruit caused by Fusarium lateritium in China

0 | Mar 03 2023

A study reports on Fusarium lateritium causing rot on Shengzhou nane fruits in Zhejiang province, China, and highlights the need for effective control strategies to reduce its incidence. [Read the Full Post]

Effect of Disulfiram on the Reproductive Capacity of Female Mice

80 | Mar 03 2023

Disulfiram (DSF) has been found to increase ovulation rate, enhance antioxidant capacity of oocytes, and promote successful pregnancy in mice by regulating gene expression related to angiogenesis, follicular development, ovulation, and antioxidants, however, more research is needed to determine if these results can be translated to humans and the safety of using DSF during pregnancy. [Read the Full Post]

Medications for the Treatment of Alcohol Dependence-Current State of Knowledge and Future Perspectives from a Public Health Perspective

111 | Mar 03 2023

The treatment of alcohol dependence requires a multi-disciplinary approach, combining psychotherapy with medications, and more research is needed to find new and effective treatments for this complex condition. [Read the Full Post]

In-vitro dynamic dissolution/bioconversion/permeation of fosamprenavir using a novel tool with an artificial biomimetic permeation barrier and microdialysis-sampling

38 | Mar 02 2023

A novel cell-free in vitro setup was developed and tested to evaluate the dynamic dissolution, bio-conversion, and permeation of fosamprenavir, showing promising results for gaining a deeper understanding of the bioconversion and permeation of phosphate-ester prodrugs. [Read the Full Post]

The successful treatment of Enterocytozoon bieneusi Microsporidiosis with nitazoxanide in a patient with B-ALL: A Case Report

52 | Mar 01 2023

This case highlights the need to consider opportunistic infections in immunocompromised patients and the importance of using metagenomic sequencing in diagnosing such infections, as well as the limited available options for treating E. bieneusi infections and the need for further research. [Read the Full Post]

Addition of Nitazoxanide to Standard Clarithromycin Based Triple Therapy for 2 Weeks Effectively Eradicates Treatment-Naive Helicobacter Pylori Infection. A Single Centre prospective, open-label study

93 | Mar 01 2023

The NACE regimen (nitazoxanide, amoxicillin, clarithromycin, and esomeprazole) was found to be an effective and well-tolerated treatment for H. pylori infection, resulting in eradication in over 90% of patients in both per-protocol and intention to treat analyses. [Read the Full Post]

Exploring drug repositioning for leishmaniasis treatment: Ivermectin plus polymeric micelles induce immunological response and protection against tegumentary leishmaniasis

34 | Mar 01 2023

The study found that ivermectin has the potential to be a candidate for the treatment of leishmaniasis caused by different species of Leishmania, as it showed efficacy in reducing parasite load and lesion size in infected mice, with low toxicity, and maintained efficacy 30 days after therapy. [Read the Full Post]

Understanding the impact of halogen functional group (Br, Cl, F, OH) in amprenavir ligand of the HIV protease

94 | Mar 01 2023

Study provides valuable insights into the structure-activity relationship of protein-ligand interactions in HIV/AIDS research and highlights the importance of halogen and hydrogen bond interactions in the development of new antiviral drugs. [Read the Full Post]

Understanding drug resistance patterns across different classes of antiretrovirals used in HIV-1-infected treatment-Naïve and experienced patients in Mumbai, India

43 | Feb 28 2023

The study found that treatment-experienced patients had higher incidence of high-level resistance to antiretroviral drugs compared to treatment-naive patients, with a positive correlation observed for within class resistance across antiretrovirals, and highlights the importance of genotypic drug resistance testing before starting treatment. [Read the Full Post]

Excess copper catalyzes protein disulfide bond formation in the bacterial periplasm but not in the cytoplasm

76 | Feb 28 2023

Copper toxicity was found to impact proteins by generating disulfide bonds in the periplasm and inactivating enzymes with solvent-exposed [4Fe-4S] clusters, but it was too inefficient at creating disulfide stress in the cytoplasm due to a slow rate of oxygen regeneration. [Read the Full Post]

High Glucose-Induced Kidney Injury via Activation of Necroptosis in Diabetic Kidney Disease

100 | Feb 28 2023

The study found that inhibiting the RIPK1/RIPK3/MLKL pathway through the use of necrostatin-1 or N-acetylcysteine can effectively protect the kidney against high glucose-induced damage in diabetic mice and could be a therapeutic target for diabetic kidney disease. [Read the Full Post]

Nanodroplet-enhanced sonodynamic therapy potentiates immune checkpoint blockade for systemic suppression of triple-negative breast cancer

130 | Feb 25 2023

The combination of STING activation, hypoxia relief, and sonodynamic therapy with anti-PD-L1 therapy using an O2-filled nanodroplet shows strong efficacy in suppressing triple-negative breast cancer growth and improving therapeutic outcome by promoting mature DCs, inducing immunogenic cell death, and enhancing tumor infiltration of CTLs. [Read the Full Post]

Emergence of monkeypox: a worldwide public health crisis

29 | Feb 23 2023

Monkeypox, a zoonotic virus similar to smallpox that infects humans, has become a global health threat with growing incidence and geographic distribution, and currently lacks a specific therapy but can be treated with vaccines and FDA-approved antiviral medications such as brincidofovir, tecovirimat, and cidofovir. [Read the Full Post]

Bowen's disease on two different unrelated anatomical sites (genitals and nail) in succession in an immunocompromised patient

54 | Feb 21 2023

A 43-year-old immunocompromised male with a history of multiple unprotected sexual exposures was diagnosed with verruca vulgaris and pigmented Bowen's disease on biopsy of hyperpigmented lesions on his genitals, and later developed longitudinal melanonychia with a subungual hyperpigmented mass on his right middle finger nail which was treated successfully with 5-fluorouracil and podophyllin. [Read the Full Post]

HIV-Tat Exacerbates the Actions of Atazanavir, Efavirenz, and Ritonavir on Cardiac Ryanodine Receptor (RyR2)

74 | Feb 21 2023

The study shows that HIV-Tat, ATV, EFV, and RTV can bind to and modulate the activity of the type 2 ryanodine receptor (RyR2) in the heart and that HIV-Tat can exacerbate the actions of ATV, EFV, and RTV on RyR2, potentially increasing the risk of cardiac arrhythmias and sudden cardiac death. [Read the Full Post]

Critical Role of Position 10 Residue in the Polymyxin Antimicrobial Activity

72 | Feb 19 2023

The study synthesized 30 novel analogues of polymyxin B1 modified at position 10 to examine their antimicrobial activity against Gram-negative bacteria and toxicity, revealing the role of the β-hydroxy side chain in promoting the correctly folded conformation of the polymyxin that drives outer membrane penetration and antibacterial activity, providing important information for developing new-generation polymyxin antibiotics. [Read the Full Post]

Pregnancy and neonatal safety outcomes of timing of initiation of daily oral tenofovir disoproxil fumarate and emtricitabine pre-exposure prophylaxis for HIV prevention (CAP016): an open-label, randomised, non-inferiority trial

115 | Feb 19 2023

In a study comparing the safety of tenofovir disoproxil fumarate and emtricitabine PrEP in pregnant women, PrEP was not associated with preterm birth or small for gestational age infants, supporting its use in pregnancy and allaying safety concerns. [Read the Full Post]

Predicting the systemic exposure and lung concentration of nafamostat using physiologically-based pharmacokinetic modeling

52 | Feb 18 2023

This study used a physiologically based pharmacokinetic (PBPK) approach and global sensitivity analysis to predict and evaluate the pharmacokinetic profiles of nafamostat in a virtual healthy population under various dosing regimens and found that the approach is valuable in predicting the PK profile and designing an appropriate dosage regimen for the treatment of COVID-19. [Read the Full Post]

Crusted scabies in AIDS patient, a clinical challenge to be sorted out with a simple bedside test

73 | Feb 17 2023

A case of crusted scabies, a severe and highly contagious variant of scabies, was reported in an AIDS patient with hyperpigmented macules covered in thick crusts on the axilla, inguinal region, and gluteal region, and was treated with ivermectin, permethrin, and keratolytics after a KOH microscopy revealed a population of more than 1 million mites. [Read the Full Post]

A pilot study of chemotherapy combinations in rats: Focus on mammary cancer treatment in female dogs

100 | Feb 17 2023

This study found that the bioavailability of carboplatin increased when combined with ivermectin and cyclophosphamide in rats, but with a higher increase in the latter, suggesting a slight reduction in carboplatin's dose when combined with cyclophosphamide to avoid increased adverse effects. [Read the Full Post]

Allolobophora caliginosa coelomic fluid and extract alleviate glucocorticoid-induced osteoporosis in mice by suppressing oxidative stress and regulating osteoblastic/osteoclastic-related markers

90 | Feb 16 2023

This study investigated the chemo-preventive activity of A.calignosa coelomic fluid and extract on glucocorticoid-induced osteoporosis in mice, revealing that both showed chemo-preventive activity by inhibiting oxidative stress and regulating expression and activity of osteoblast/osteoclast-related markers, resulting in increased bone mineral density and decreased activity of alkaline phosphatase and parathyroid hormone. [Read the Full Post]

16a-Methyl corticosteroids; a new series of anti-inflammatory compounds; clinical appraisal of their antirheumatic potencies

71 | Feb 16 2023

Four new derivatives of hydrocortisone with a methyl grouping at the 16a-carbon position were synthesized and studied in human subjects for anti-inflammatory activity, with 16a-methyl 9a-fluoroprednisolone showing the highest potency per milligram and potential for long-term therapeutic use. [Read the Full Post]

Synthesis of Benzimidazole-1,2,4-triazole Derivatives as Potential Antifungal Agents Targeting 14α-Demethylase

38 | Feb 16 2023

Benzimidazole-1,2,4-triazole derivatives were synthesized and screened for their antifungal activity against C. albicans, C. glabrata, C. krusei, and C. parapsilopsis, with three compounds (6b, 6i, and 6j) showing higher antifungal activity than voriconazole and fluconazole, and potential for use as a new fungicidal lead targeting 14α-demethylase with effects on the L929 cell line and C. glabrata cells evaluated. [Read the Full Post]

Pulmonary cryptococcosis after immunomodulator treatment in patients with Crohn's disease: Three case reports

25 | Feb 16 2023

Three patients with Crohn's disease developed pulmonary cryptococcosis after receiving immunomodulatory treatment and were successfully treated with fluconazole; increased incidence of this opportunistic infection highlights the need for clinical vigilance and early identification for standardized treatment. [Read the Full Post]

Inhibition of multiple CDKs potentiates colon cancer chemotherapy via p73-mediated DR5 induction

55 | Feb 10 2023

CDK inhibitors sensitize colorectal cancer cells to therapy-induced apoptosis by inducing Death Receptor 5 via p73-mediated transcriptional activation, making p73-mediated DR5 induction a critical target engaged by CDKIs in potentiating therapy-induced apoptosis in colorectal cancer cells. [Read the Full Post]

Flavopiridol Protects against Fungal Keratitis due to Aspergillus fumigatus by Alleviating Inflammation through the Promotion of Autophagy

22 | Feb 10 2023

Flavopiridol reduces inflammation in fungal keratitis by promoting autophagy, phagocytosis, and antifungal activity, indicating its potential as a therapeutic option for fungal keratitis. [Read the Full Post]

Biased Clonal Evolution in Acute Promyelocytic Leukemia through Imbalances Affecting the der(17) but Not the der(15) Chromosome: Report of Two Cases

35 | Feb 09 2023

Two cases of acute promyelocytic leukemia with the secondary chromosomal change of ider(17)(q10) were treated with ATRA plus idarubicin and achieved long event-free survival according to the PETHEMA LPA 2012 protocol. [Read the Full Post]

Comparative study between two different morphological structures based on polylactic acid, nanocellulose and magnetite for co-delivery of flurouracil and curcumin

69 | Feb 07 2023

The magnetic copolymeric micelles M-PLA-co-NC/5-FU/CUR showed superior antibacterial and antitumor efficacy, slower release and higher loading % of CUR compared to the blended formulation PLA/M-NC/5-FU/CUR, making them a promising nanomedicine against bacteria and multiple cell lines. [Read the Full Post]

Extracellular vesicles derived from dental mesenchymal stem/stromal cells with gemcitabine as cargo have an inhibitory effect on the growth of pancreatic carcinoma cell lines in vitro

63 | Feb 07 2023

DP-MSC-EVs have therapeutic potential as a drug delivery tool for cancer therapy by absorbing and secreting gemcitabine and expressing a suicide gene to convert non-toxic prodrug 5-FC to cytotoxic drug 5-FU, resulting in significant inhibition of cancer cell growth. [Read the Full Post]

[Single-center study of different treatment for advanced or unresectable angiosarcoma patients]

125 | Feb 06 2023

This study found that doxorubicin-based and paclitaxel-based chemotherapy are the most common treatments for advanced angiosarcoma, and combined targeted therapy with anti-PD-1 immunotherapy showed potential efficacy in some patients with long duration of response and moderate adverse events. [Read the Full Post]

Novel carboxymethyl cellulose-halloysite-polyethylene glycol nanocomposite for improved 5-FU delivery

114 | Feb 06 2023

This study synthesized a pH-responsive nanocomposite based on halloysite nanotube (HNT) coated with carboxymethyl cellulose (CMC)/polyethylene glycol (PEG) hydrogel for controlled delivery of 5-Fluorouracil (5-FU), a hydrophobic chemotherapy drug, using the W/O/W technique, achieving high drug entrapment and loading and showing improved and sustained 5-FU delivery in acid environment and considerable cytotoxicity on MCF-7 breast cancer cells. [Read the Full Post]

Addressing adherence to guidelines on prevention of acute chemotherapy-induced nausea and vomiting in pediatric patients

75 | Feb 04 2023

Guideline adherence for prevention of chemotherapy-induced nausea and vomiting improved significantly, particularly in the high emetogenic chemotherapy group, with education, addition of anti-emetics to formulary, and implementation of a standardized guideline tool, but further improvement is needed in the moderately emetogenic chemotherapy group. [Read the Full Post]

Antiemetic use and chemotherapy induced nausea and vomiting related hospitalization costs after highly or moderately emetogenic chemotherapy

64 | Feb 04 2023

PrecisionQ's database analysis found lower CINV related hospitalization costs among patients receiving netupitant/fosnetupitant with palonosetron (NEPA) compared to aprepitant/fosaprepitant with ondansetron (APON) or aprepitant/fosaprepitant with palonosetron (APPA) during highly emetogenic chemotherapy or moderately emetogenic chemotherapy. [Read the Full Post]

Effectiveness of different treatment regimens on patients with COVID-19, hospitalized in Sanandaj hospitals: a retrospective cohort study

37 | Feb 03 2023

The study found that the drug regimen 2 (Interferons (ReciGen/Ziphron) or Interferon Vectra (lopinavir/ritonavir)) increased the days of hospitalization and hospitalization in ICU, while other drug regimens had no significant effect on mortality, use of a ventilator, or reducing mortality compared to the others. [Read the Full Post]

Awareness on current status of usage of ritonavir in the management of covid among dental students

49 | Feb 03 2023

A survey of 100 dental students in Chennai showed that postgraduate students had greater knowledge of the current use of Ritonavir in the management of COVID-19, but the study highlights the need for regular education and training programs for all healthcare workers on COVID-19 infection control procedures. [Read the Full Post]

Phenolipid JE improves metabolic profile and inhibits gluconeogenesis via modulating AKT-mediated insulin signaling in STZ-induced diabetic mice

52 | Jan 22 2023

Guihua Wang et al. suggested that JE might be a potent activator for AKT-mediated insulin signaling pathway. [Read the Full Post]

Upregulation of glutamate transporter 1 by mTOR/Akt pathway in astrocyte culture during oxygen-glucose deprivation and reoxygenation

29 | Jan 21 2023

Mi Li et al. suggested that astrocytes might adapt to short-term ischemic-reperfusion injury by regulating cell morphology, apoptosis and GLT-1 upregulation. [Read the Full Post]

Racial and Ethnic Differences in Internal Medicine Residency Assessments

105 | Jan 06 2023

Dowin Boatright et al. found that URiM and Asian internal medicine residents received lower ratings on performance assessments than their White peers during the first and second years of training. [Read the Full Post]

The Novel h DHODH Inhibitor MEDS433 Prevents Influenza Virus Replication by Blocking Pyrimidine Biosynthesis

7 | Dec 18 2022

Giulia Sibille et al. suggested MEDS433 as a potential HTA candidate to develop novel anti-IV intervention approaches, either as a single agent or in combination regimens with DAAs. [Read the Full Post]

Effect of concomitant use of pitavastatin with neoadjuvant chemotherapy protocols in breast cancer patients: A randomized controlled clinical trial

105 | Nov 21 2022

Samar A Dewidar et al. thought that concomitant use of pitavastatin with standard neoadjuvant chemotherapy protocols might improve neoadjuvant chemotherapy responses in patients with breast cancer. [Read the Full Post]

Role of the Glycogen Synthase Kinase 3-Cyclic AMP/Protein Kinase A in the Immobilization of Human Sperm by Tideglusib

47 | Nov 21 2022

Weiwei Wang et al. found the GSK3-cAMP/PKA regulatory loop in human sperm, which might mediate the immobilization effect of tideglusib at low of concentrations (e.g., 1.25 μM) on sperm motility. [Read the Full Post]

Oil-free eye drops containing Cyclosporine A/cyclodextrin/PVA supramolecular complex as a treatment modality for dry eye disease

50 | Oct 06 2022

Pinal Chaudhari et al. demonstrated the potential of the supramolecular complex as an alternative to the oil-based formulation of eye drops for drugs that showed low solubility and poor corneal permeation. [Read the Full Post]

Unraveling the therapeutic potential of GANT61/Dactolisib combination as a novel prostate cancer modality

110 | Sep 08 2022

Mohamed Youssef et al. discovered that Dactolisib/GANT61 combination was promising in PCa treatment. [Read the Full Post]

BEZ235 Prolongs Murine Cardiac Allograft Survival Through the Autophagy Pathway

76 | Sep 08 2022

Xiaolong Miao et al. proposed a theoretical foundation for the strong connection between mTOR-induced autophagy and heart transplant. [Read the Full Post]

Radical S-Adenosyl Methionine Enzyme BlsE Catalyzes a Radical-Mediated 1,2-Diol Dehydration during the Biosynthesis of Blasticidin S

42 | Aug 26 2022

Yu-Hsuan Lee et al. suggested that BlsE catalysis likely proceeded via direct elimination of water from the CGA C4' α-hydroxyalkyl radical as opposed to 1,2-migration of the C3'-hydroxyl prior to dehydration. [Read the Full Post]

Human osteoprogenitor cells obtained from traumatic heterotopic ossification samples showed enhanced osteogenic differentiation potential and ERK/Hedgehog signaling than that from normal bone

60 | Aug 15 2022

Tongtong Zhang et al. found that the activation of ERK and Hedgehog signaling pathway jointly enhanced the osteogenic potential of HO-ops to induce the formation of traumatic HO. [Read the Full Post]

Real-World Characterization of the Portuguese Population Living with HIV who Initiated Raltegravir Based-Regimens: The REALITY Study

45 | Aug 02 2022

Rosário Serrão et al. showed that raltegravir-based regimens seemed like a valid therapeutic option in heterogeneous populations of HIV-infected patients, in patients with previous ART experience and as part of first-line therapeutic options alongside with the latest generation of drugs from its class. [Read the Full Post]

RB loss determines selective resistance and novel vulnerabilities in ER-positive breast cancer models

84 | Jul 27 2022

Vishnu Kumarasamy et al. demonstrated the highly selective use of birinapant based combinations for the treatment of RB-deficient tumors. [Read the Full Post]

Clostridioides difficile toxin B alone and with pro-inflammatory cytokines induces apoptosis in enteric glial cells by activating three different signalling pathways mediated by caspases, calpains and cathepsin B

63 | Jul 24 2022

Katia Fettucciari et al. demonstrated that TcdB induced caspase-dependent, mitochondria-independent enteric glial cell (EGC) apoptosis that was enhanced by the pro-inflammatory cytokines TNF-α and IFN-γ (CKs) by increasing caspase-3/7/9 and PARP activation. [Read the Full Post]

Simulating Colorectal Cancer Trials Using Real-World Data

134 | Jul 18 2022

Zhaoyi Chen et al. simulated five CRC trials, and tested two simulation scenarios with several different configurations demonstrated that our simulations couldrobustly generated effectiveness and safety outcomes comparable with the original trials using real-world data. [Read the Full Post]

Comparative Efficacy and Safety of Janus Kinase Inhibitors and Secukinumab in Patients with Active Ankylosing Spondylitis: A Systematic Review and Meta-Analysis

190 | Jul 13 2022

Young Ho Lee suggested that tofacitinib 5 mg had the highest likelihood of being the best treatment for achieving the ASAS40 response rate, followed by upadacitinib 15 mg, secukinumab 150 mg, filgotinib 200 mg, and placebo. [Read the Full Post]

Carfilzomib plus dexamethasone in patients with relapsed and refractory multiple myeloma: a retro-prospective observational study

126 | Jul 04 2022

Maria Livia Del Giudice et al. thought that Kd56 was an effective and well tolerated regimen in highly pretreated and elderly patients with a good safety profile. [Read the Full Post]

The impact of emricasan on chronic liver diseases: current data

94 | Jul 03 2022

Vasileios Lekakis et al. showed that as emricasan treatment appeared safe and well-tolerated, irrespective the severity of liver disease, more studies were required to clarify better these subgroups of patients who might benefit most from this drug. [Read the Full Post]

Repression of HIV-1 reactivation mediated by CRISPR/dCas9-KRAB in lymphoid and myeloid cell models

204 | Jun 26 2022

Lendel Correia da Costa et al. demonstrated that KRAB repressor protein was crucial to reactivation resistance phenotype. [Read the Full Post]

Histone Deacetylase Inhibitors Counteract CGRP Signaling and Pronociceptive Sensitization in a Rat Model of Medication Overuse Headache

174 | Jun 26 2022

Matteo Urru et al. provided evidence for a key role of HDACs and epigenetics in MOH pathogenesis, highlighting the therapeutic potential of HDAC inhibition in the prevention of migraine chronification. [Read the Full Post]

The PRC2 molecule EED is a target of epigenetic therapy for neuroblastoma

221 | Jun 23 2022

Dilibaerguli Shaliman et al. suggested that inhibitory cell cycle-regulated gene sets were markedly up-regulated. [Read the Full Post]

Real-world experience in treating pediatric relapsed/refractory or therapy-related myeloid malignancies with decitabine, vorinostat, and FLAG therapy based on a phase 1 study run by the TACL consortium

186 | Jun 22 2022

Eric S Schafer et al. found that therapy was well tolerated and effective in pediatric patients with R/R myeloid neoplasms, particularly those with epigenetic alterations, t-AML, and refractory disease. [Read the Full Post]

Three Birds, One Excipient: Development of an Improved pH, Isotonic, and Buffered Ketamine Formulation for Subcutaneous Injection

159 | Jun 03 2022

Jason Wallach et al. found that this strategy has the potential to be readily adapted to other amine-based APIs. [Read the Full Post]

Stability of Captisol-enabled versus propylene glycol-based melphalan at room temperature and after refrigeration

143 | Jun 03 2022

Jitesh D Kawedia et al. found that CE-melphalan at 2 mg/mL has 24-hour stability at RT and can be used for extended infusion times or may be compounded ahead of time. Reconstituted CE-melphalan vials are stable for 48 hours at both RT and 4 °C. [Read the Full Post]

Physicochemical Characterization, Molecular Docking, and In Vitro Dissolution of Glimepiride-Captisol Inclusion Complexes

160 | Jun 01 2022

Arpita Pal et al. found that complexation with Captisol enhanced the water solubility of glimepiride. [Read the Full Post]

Evaluation of mitochondrial oxidative toxicity in mammalian cardiomyocytes by determining the highly reproducible and reliable increase in mitochondrial superoxides after exposure to therapeutic drugs

291 | May 27 2022

Dohee Ahn et al. found that a screening system using MitoSOX™ had the potential to be applied as a reliable biomarker for determining mitochondrial oxidative toxicity in new drug development. [Read the Full Post]

COVID-19: Implications Regarding the Properties and Behaviors of the Coronavirus Disease

192 | May 14 2022

COVID-19 may be inaccurate due to errors in diagnosing and reporting, since other similar illnesses may exhibit similar symptoms. [Read the Full Post]

The Mycotoxin Beauvericin Exhibits Immunostimulatory Effects on Dendritic Cells via Activating the TLR4 Signaling Pathway

295 | May 10 2022

Xiaoli Yang et al. identified TLR4 as a cellular BEA sensor and define BEA as a potent activator of BMDCs, implying that this compound could be exploited as a promising candidate structure for vaccine adjuvants or cancer immunotherapies. [Read the Full Post]

[Ocular toxicity of targeted therapies with MEK inhibitors and BRAF inhibitors in the treatment of metastatic cutaneous melanoma]

299 | May 06 2022

E Fauviaux et al. found that a multidisciplinary approach including ophthalmologists, dermatologists and oncologists was essential in order to adapt treatment in the advent of the ocular complications. [Read the Full Post]

Alternating therapy with osimertinib and afatinib for treatment-naive patients with EGFR-mutated advanced non-small cell lung cancer: A single-group, open-label phase 2 trial (WJOG10818L)

350 | May 02 2022

Hidetoshi Hayashi et al. found that Alternating therapy with osimertinib and afatinib for treatment-naive patients with EGFR- mutated advanced NSCLC did not meet its primary end point, despite the encouraging efficacy and safety profile of this treatment strategy. [Read the Full Post]

Clinically relevant CHK1 inhibitors abrogate wild-type and Y537S mutant ERα expression and proliferation in luminal primary and metastatic breast cancer cells

450 | Apr 20 2022

Sara Pescatori et al. thought that CHK1 could be considered as an appealing novel pharmacological target for the treatment of luminal primary and MBCs. [Read the Full Post]

Factors Influencing the Intracellular Concentrations of the Sofosbuvir Metabolite GS-331007 (in PBMCs) at 30 Days of Therapy

308 | Apr 02 2022

Jessica Cusato et al. presented data on an IC evaluation in a cohort of patients treated with SOF, also considering pharmacogenetics. [Read the Full Post]

Drug repurposing through virtual screening and in vitro validation identifies tigecycline as a novel putative HCV polymerase inhibitor

277 | Apr 01 2022

Mahmoud ElHefnawi et al. found that tigecycline displayed synergistic activity with sofosbuvir and daclatasvir against HCV. [Read the Full Post]

SC75741, A Novel c-Abl Inhibitor, Promotes the Clearance of TDP25 Aggregates via ATG5-Dependent Autophagy Pathway

200 | Feb 26 2022

Dongheng Zhou et al. found that dual-targeted inhibition of c-Abl and NF-κB may be a potential treatment for TDP43 proteinopathies and ALS. [Read the Full Post]

Baricitinib for relapsing giant cell arteritis: a prospective open-label 52-week pilot study

507 | Feb 23 2022

Matthew J Koster et al. showed that in this proof-of-concept study, baricitinib at 4 mg/day was well tolerated and discontinuation of GC was allowed in most patients with relapsing GCA. [Read the Full Post]

Predictors of Treatment Response and Long-Term Outcomes in Young Children with Steroid-Dependent Nephrotic Syndrome Treated with High-Dose Mizoribine as First-Line Steroid-Sparing Agent

316 | Feb 23 2022

Shuichiro Fujinaga et al. discovered that high-dose mizoribine might be an attractive treatment option as initial SSA in young children with low steroid-dependent dose for improved long-term outcomes. [Read the Full Post]

Drug survival of biologics and novel immunomodulators for rheumatoid arthritis, axial spondyloarthritis, psoriatic arthritis, and psoriasis - A nationwide cohort study from the DANBIO and DERMBIO registries

358 | Feb 22 2022

Alexander Egeberg et al. emphasized that although these diseases had many overlaps in their pathogenesis, there was a need for an individualized treatment approach that considered the underlying disease, patient profile, and treatment history. [Read the Full Post]

Screening of the ubiquitin-proteasome system activators for anti-Alzheimer's disease by the high-content fluorescence imaging system

0 | Feb 03 2022

Yi-Ling Wang found that a novel insight into the discovery and development of anti-AD drugs. [Read the Full Post]

A standard knockout procedure alters expression of adjacent loci at the translational level

256 | Feb 02 2022

Artyom A Egorov et al. estimated that in as much as ∼1/5 of knockout strains the expression of neighboring genes might be substantially (>2-fold) deregulated at the level of translation. [Read the Full Post]

Drug repositioning based on gene expression data for human HER2-positive breast cancer

369 | Jan 21 2022

Farkhondeh Khanjani et al. suggested that some repurposed drugs based on gene expression data could be noticed as potential drugs for the treatment of HER2-positive breast cancer. [Read the Full Post]

Integrated Genomic Profiling and Drug Screening of Patient-Derived Cultures Identifies Individualized Copy Number-Dependent Susceptibilities Involving PI3K Pathway and 17q Genes in Neuroblastoma

227 | Jan 20 2022

Rachel L Y Wong et al. defined individualized dose-dependent relationships between copy number gains of PI3K and STAT family genes particularly on 17q and susceptibility to PI3K and cell cycle agents in neuroblastoma. [Read the Full Post]

Differential time course of glycogen synthase kinase-3 inhibition in experimental autoimmune encephalomyelitis

356 | Dec 29 2021

A S Al-Zaidi et al. found that downregulation of Th1 and Th17 hallmark cytokines by Tideglusib in EAE might be associated with IL-10 production. [Read the Full Post]

Small Dense Low-Density Lipoprotein Cholesterol and Cardiovascular Risk in Statin-Treated Patients with Coronary Artery Disease

412 | Dec 28 2021

Junnichi Ishii et al. investigated the relationship between small dense low-density cholesterol (sdLDL-C) and risk of major adverse cardiovascular events (MACE) in patients treated with high- or low-dose statin therapy. [Read the Full Post]

A nephroprotective iodinated contrast agent with cardioprotective properties: A pilot study

432 | Nov 13 2021

Elizabeth S Rowe et.al suggested that SBECD-iohexol is superior to iohexol alone, for both the preservation of cardiomyocyte integrity and preservation of myocardial function in myocardial ischemia. [Read the Full Post]

Dual PI3K/mTOR inhibitor NVP‑BEZ235 decreases the proliferation of doxorubicin‑resistant K562 cells

1467 | Oct 17 2021

Jie Li et al. suggested that BEZ235 might reverse Doxo resistance in leukemia cells. [Read the Full Post]

Targeting mTOR signaling overcomes acquired resistance to combined BRAF and MEK inhibition in BRAF-mutant melanoma

749 | Oct 17 2021

Beike Wang et al. revealed that mTOR activation was essential for drug resistance of melanoma to MAPK inhibitors, and provided insight into the rewiring of the signaling networks in CR melanoma. [Read the Full Post]

A [3Fe-4S] cluster and tRNA-dependent aminoacyltransferase BlsK in the biosynthesis of Blasticidin S

635 | Oct 03 2021

Xiankun Wang et al. provided an example of an iron-sulfur protein that catalyzed an aminoacyl-tRNA (aa-tRNA)-dependent amide bond formation in a natural product biosynthetic pathway. [Read the Full Post]

EGFR and ERK activation resists flavonoid quercetin-induced anticancer activities in human cervical cancer cells in vitro

558 | Sep 21 2021

Xin Chen et al.determined the role of EGFR and the underlying signaling pathways involved in the anti-cervical cancer malignant behavior induced by Que and identified the negative regulatory association. [Read the Full Post]

Identification of FDA approved drugs against SARS-CoV-2 RNA dependent RNA polymerase (RdRp) and 3-chymotrypsin-like protease (3CLpro), drug repurposing approach

264 | Sep 08 2021

Zahra Molavi et al. recommended further experimental evaluations in vitro and in vivo on FDA-approved drugs to assess their potential antiviral effect on SARS-CoV-2. [Read the Full Post]

Impact of FasL Stimulation on Sclerostin Expression and Osteogenic Profile in IDG-SW3 Osteocytes

573 | Aug 30 2021

Adela Kratochvilova et al. found the caspase-independent impact of FasL stimulation. [Read the Full Post]

ARTEMIN Promotes Oncogenicity and Resistance to 5-Fluorouracil in Colorectal Carcinoma by p44/42 MAPK Dependent Expression of CDH2

809 | Aug 25 2021

Qiu-Shi Zhuang et al. thought that ARTN might be of prognostic and theranostic utility in CRC. [Read the Full Post]

Tofacitinib Ameliorates Lupus Through Suppression of T Cell Activation Mediated by TGF-Beta Type I Receptor

986 | Aug 20 2021

Qing Yan et al. thought that tofacitinib could suppress T cell activation by upregulating TGFβRI expression, which provided a possible molecular mechanism underlying clinical efficacy of tofacitinib in treating SLE patients. [Read the Full Post]

Sinus rhythm heart rate increase after atrial fibrillation ablation is associated with lower risk of arrhythmia recurrence

794 | Aug 11 2021

Ammar M Killu et al. showed that relative changes in HR post AF ablation correlates with AF recurrence. [Read the Full Post]

Efficacy and Safety of Emricasan in Liver Cirrhosis and/or Fibrosis

623 | Aug 10 2021

Li-Ya Mu et al. found that treatment with emricasan was more effective in improving liver function and apoptosis parameters compared to placebo, with a well-tolerated safety profile. [Read the Full Post]

Local ablation of gastric cancer by reconstituted apolipoprotein B lipoparticles carrying epigenetic drugs

1000 | Aug 03 2021

Chia-Lung Yang et al. established rABL-based nanoparticles embedded epigenetic inhibitors for local treatment of gastric cancer, which had good therapeutic effects but do not cause severe side effects. [Read the Full Post]

High-Throughput Mechanistic Screening of Epigenetic Compounds for the Potential Treatment of Meningiomas

1043 | Aug 02 2021

Philip D Tatman et al. suggested an important role of HDACs in meningioma biology and as a targetable mechanism. [Read the Full Post]

Effect of Decitabine (5-aza-2'-deoxycytidine, 5-aza-CdR) in Comparison with Vorinostat (Suberoylanilide Hydroxamic Acid, SAHA) on DNMT1, DNMT3a and DNMT3b, HDAC 1-3, SOCS 1, SOCS 3, JAK2, and STAT3 Gene Expression in Hepatocellular Carcinoma HLE and LCL-PI 11 Cell Lines

747 | Jul 31 2021

Masumeh Sanaei et al. found that 5-Aza-CdR and SAHA could induce cell growth inhibition and apoptosis induction through the JAK/STAT pathway. [Read the Full Post]

Successful Treatment of a Locally Recurrent and Metastatic Malignant Phyllodes Tumor with Accelerated Radiotherapy and Nab-Paclitaxel, Cisplatin, and Liposomal Doxorubicin Chemotherapy

1171 | Jul 08 2021

Ioannis M Koukourakis et al. found that the combination of cisplatin with nab-paclitaxel and liposomal doxorubicin chemotherapy had acceptable toxicity and was highly effective in eradicating metastatic lesions. [Read the Full Post]

Allosteric Activation of SARS-CoV-2 RNA-Dependent RNA Polymerase by Remdesivir Triphosphate and Other Phosphorylated Nucleotides

552 | Jun 23 2021

Bing Wang et al. demonstrated that RdRp was allosterically activated by nontemplating phosphorylated nucleotides, including naturally occurring alarmone ppGpp and synthetic remdesivir triphosphate. [Read the Full Post]

HeLa TI cell-based assay as a new approach to screen for chemicals able to reactivate the expression of epigenetically silenced genes

704 | Jun 18 2021

Varvara Maksimova et al. showed that N-nitrosodiphenylamine and N-nitrosodimethylamine reactivated epigenetically silenced genes, probably by affecting DNA methylation. [Read the Full Post]

Real-world-evidence-for-carfilzomib-dosing-intensity-on-overall-survival-and-treatment-progression-in-multiple-myeloma-patients

775 | Jun 13 2021

Noopur Raje found that patient outcomes could be improved if eligible MM patients are treated with the optimized [Read the Full Post]

Efficacy of tyrosine kinase inhibitors against lung cancer with EGFR exon 18 deletion: Case report and pooled analysis

956 | Jun 08 2021

Rafael Rubiera-Pebe et al. showed that afatinib was associated with a greater tumor response rate and a longer PFS than the first generation TKIs. [Read the Full Post]

Treatment of Luminal Metastatic Breast Cancer beyond CDK4/6 Inhibition: Is There a Standard of Care in Clinical Practice?

1217 | May 21 2021

Athanasios Mavratzas et al. thought that treatment of metastatic luminal breast cancer after progression on CDK4/6 inhibitors remained a challenge. [Read the Full Post]

In vitro antiviral activity of the anti-HCV drugs daclatasvir and sofosbuvir against SARS-CoV-2, the aetiological agent of COVID-19

599 | Apr 22 2021

Carolina Q Sacramento et al. found that daclatasvir, alone or in combination with sofosbuvir, at higher doses than used against HCV, might be further fostered as an anti-COVID-19 therapy. [Read the Full Post]

Naturally Occurring Resistance Associated Substitutions in Non-Cirrhotic, Treatment Naive HCV-HIV Co-Infected Patients Does Not Affect the Treatment Response for Anti-HCV Antiviral Therapy

592 | Apr 22 2021

Ekta Gupta et al. showed that BL-RAS were common in HCV-HIV co-infected patients. [Read the Full Post]

Effect of Eriocalyxin B on prostatic inflammation and pelvic pain in a mouse model of experimental autoimmune prostatitis

620 | Mar 08 2021

Li-Gang Zhang et al. suggested that EriB could alleviate the severity of prostatic inflammation and pelvic pain in an EAP mouse model. [Read the Full Post]

Immediate Effect of Baricitinib on Arthritis and Biological Disease-Modifying Antirheumatic Drug-Induced Psoriasis-Like Skin Lesions in Two Patients with Rheumatoid Arthritis

810 | Mar 05 2021

Yoshifumi Tada et al. found that baricitinib was initiated because of RA flare and resulted in immediate beneficial effects on arthritis as well as skin lesions. [Read the Full Post]

Comparison of Treatment Effect and Tolerance of the Topical Application of Mizoribine and Cyclosporine A in a Mouse Dry Eye Model

715 | Mar 05 2021

Xiang Lin et al. found that MZR (0.05% in PBS) could be a good competitive product for Restasis because of the comparable treatment effect in dry eye diseases and better ocular tolerability in ocular itch and pain. [Read the Full Post]

In-vitro evaluation of the immunomodulatory effects of baricitinib: implication for COVID-19 therapy

843 | Mar 04 2021

Linda Petrone et al. found that exogenous addition of baricitinib decreased the in-vitro SARS-CoV-2-specific response in COVID-19 patients using a whole-blood platform. [Read the Full Post]

The application of nanoparticles in cancer immunotherapy: Targeting tumor microenvironment

770 | Feb 13 2021

Muyue Yang et al. found that the changes of TME at various stages during tumor development are required to be further elucidated so that more individualized nanoplatforms could be designed. [Read the Full Post]

Selective reactivation of STING signaling to target Merkel cell carcinoma

808 | Feb 13 2021

Wei Liu et al. found that targeted delivery and activation of STINGS162A/G230I/Q266I in tumor cells held great therapeutic promise for the treatment of MCC and many other STING-deficient cancers. [Read the Full Post]

The yeast platform engineered for synthetic gRNA-landing pads enables multiple gene integrations by a single gRNA/Cas9 system

626 | Feb 09 2021

Sihyun Baek et al. demonstrated the effectiveness of a single gRNA-mediated CRISPR platform to build complex metabolic pathways in yeast. [Read the Full Post]

[Altered Splicing in Stable Cell Strains Expressing Mini-hF9 Gene with Nonsense Mutation]

578 | Feb 09 2021

Gang Wang et al. found that the nonsense associated altered splicing (NAS) pathway, which generated alternately spliced transcripts, might be triggered in coagulation factor IX gene with nonsense mutation. [Read the Full Post]

CKAP2L promotes non-small cell lung cancer progression through regulation of transcription elongation

523 | Jan 28 2021

Tiziana Monteverde et al. found that the molecular mechanisms through which CKAP2L, a protein involved in CIN, promoted cancer progression and suggested that its inhibition represented a novel therapeutic strategy in NSCLC. [Read the Full Post]

Identification of hub genes and small molecule therapeutic drugs related to breast cancer with comprehensive bioinformatics analysis

503 | Jan 28 2021

Mingqian Hao et al. identified six hub genes and 29 potential drug candidates for breast cancer. [Read the Full Post]

Ebselen, Disulfiram, Carmofur, PX-12, Tideglusib, and Shikonin Are Nonspecific Promiscuous SARS-CoV-2 Main Protease Inhibitors

564 | Jan 07 2021

Chunlong Ma et al. suggested that these six compounds were nonspecific SARS-CoV-2 Mpro inhibitors and urged the scientific community to be stringent with hit validation. [Read the Full Post]

Repurposing FDA Approved Drugs as JNK3 Inhibitor for Prevention of Neuroinflammation Induced by MCAO in Rats

582 | Jan 06 2021

Zikra Zulfiqar et al. demonstrated that the novel FDA-approved medications attenuate ischemic stroke-induced neuronal degeneration, possibly by inhibiting JNK3. [Read the Full Post]

Effect of mechanochemical inclusion of triamterene into sulfobutylether-β-cyclodextrin and its improved dissolution behavior

480 | Nov 23 2020

Hideko Maeda et al. found that the water apparent solubility of TT could be improved by simple mechanical mixing without organic solvents, and improved bioavailability after oral administration was expected. [Read the Full Post]

Brain exposure of the ATM inhibitor AZD1390 in humans - a positron emission tomography (PET) study

524 | Nov 21 2020

Aurelija Jucaite et al. found the potential of PET microdosing in predicting and guiding dose range and schedule for subsequent clinical studies. [Read the Full Post]

A phase I trial of temsirolimus and erlotinib in patients with refractory solid tumors

738 | Nov 15 2020

Haeseong Park et al. found the he combination of temsirolimus and erlotinib at the RP2D was well tolerated, and the regimen resulted in prolonged disease stabilization in selected patients (NCT00770263). [Read the Full Post]

Optimization and Evaluation of Propolis liposomes as a promising therapeutic approach for COVID-19

523 | Nov 11 2020

Hesham Refaat et al. identified the potential of propolis liposomes as a promising treatment approach against COVID-19. [Read the Full Post]

A phase I study of a dual PI3-kinase/mTOR inhibitor BEZ235 in adult patients with relapsed or refractory acute leukemia

612 | Oct 22 2020

Fabian Lang et al.thought that combined inhibition of PI3K and mTOR inhibited a clinically meaningful driver pathway in a small subset of patients with ALL, with no benefit in patients with AML. [Read the Full Post]

HPV-induced Nurr1 promotes cancer aggressiveness, self-renewal, and radioresistance via ERK and AKT signaling in cervical cancer

578 | Oct 20 2020

Peter Kok-Ting Wan et al. provided that BEZ, but not GSK, could abolish Nurr1-enhanced radioresistance, suggesting its potential value for radiosensitizing CSLCs in the clinical setting. [Read the Full Post]

CTELS: A Cell-Free System for the Analysis of Translation Termination Rate

619 | Sep 28 2020

Kseniya A Lashkevich et al. revealed a transient stalling event at a "leaky" stop codon context, which likely defined the basis of nonsense suppression. [Read the Full Post]

Proliferation of Vascular Smooth Muscle Cells under ox-LDL Is Regulated by Alismatis rhizoma Decoction via InhibitingERK1/2 and miR-17∼92a Cluster Activation

532 | Sep 14 2020

Julian Shen et al. provided the multitarget mechanisms for application of AD in the treatment of atherosclerosis. [Read the Full Post]

Fluvastatin potentiates anticancer activity of vorinostat in renal cancer cells

777 | Sep 10 2020

Kazuki Okubo et al. found that there was a positive feedback cycle among AMPK activation, histone acetylation, and ER stress induction. [Read the Full Post]

Molecular dynamic simulations to investigate the structural impact of known drug resistance mutations on HIV-1C Integrase-Dolutegravir binding

277 | Aug 24 2020

Rumbidzai Chitongo et al. suggested the G140S mutant had the strongest effect on the HIV-1C IN protein structure and Dolutegravir binding. [Read the Full Post]

Identification of MYC as an antinecroptotic protein that stifles RIPK1-RIPK3 complex formation

505 | Aug 16 2020

Daehyeon Seong et al. found that MYC-mediated suppression of necroptosis was a mechanism of necroptosis resistance in cancer, and approaches targeting MYC to induce necroptosis represent an attractive therapeutic strategy for cancer. [Read the Full Post]

Giardia duodenalis induces extrinsic pathway of apoptosis in intestinal epithelial cells through activation of TNFR1 and K63 de-ubiquitination of RIP1 in vitro

509 | Aug 11 2020

Lin Liu et al. suggested that Giardia trophozoite stimulation could activate CASP3/8 signaling pathways via activation of TNFR1 and K63 de-ubiquitination of RIP1 caused by up-regulated expressions of CYLD and A20, and promoted Caco-2 cell apoptosis. [Read the Full Post]

Gemcitabine combined with cisplatin vs. taxane, cisplatin, and fluorouracil in the treatment of locally advanced nasopharyngeal carcinoma: a retrospective case-control study

627 | Aug 04 2020

Y-M Huang et al. showed that the clinical efficacy of the GP regimen combined with CCRT for the treatment of locoregionally advanced NPC might be better than that of the TPF regimen. [Read the Full Post]

Effectiveness and Costs Among Rheumatoid Arthritis Patients Treated with Targeted Immunomodulators Using Real-World U.S. Data

793 | Jul 28 2020

Mahdi Gharaibeh et al. showed that the range of patients who were effectively treated with first-line therapy was higher for certain tumor necrosis factor inhibitors and tocilizumab. [Read the Full Post]

Phase 1 trial of carfilzomib (PR-171) in combination with vorinostat (SAHA) in patients with relapsed or refractory B-cell lymphomas

779 | Jul 16 2020

Beata Holkova et al. showed a decrease in NF-κB activation and an increase in Bim levels in some patients, but these changes did not correlate with clinical response. [Read the Full Post]

Advanced bioinformatics rapidly identifies existing therapeutics for patients with coronavirus disease-2019 (COVID-19)

566 | Jul 15 2020

Jason Kim et al. highlighted the potential use of two bioinformatics technologies to rapidly discover existing therapeutic agents that warranted further investigation for established and emerging disease processes. [Read the Full Post]

Histone Deacetylase Inhibition Prevents the Growth of Primary and Metastatic Osteosarcoma

1046 | Jul 07 2020

Jeremy J McGuire et al. provided rationale for clinical trials in osteosarcoma patients using the approved therapies panobinostat or romidepsin. [Read the Full Post]

Combination BET Family Protein and HDAC Inhibition Synergistically Elicits Chondrosarcoma Cell Apoptosis Through RAD51-Related DNA Damage Repair

882 | Jul 06 2020

Songwei Huan et al. disclosed that BET and HDAC inhibition synergistically inhibited cell growth and induced cell apoptosis through a mechanism that involved the suppression of RAD51-related HR DNA repair in chondrosarcoma cells. [Read the Full Post]

18 F-Fluoroestradiol ( 18 F-FES)-PET Imaging in a Phase II Trial of Vorinostat to Restore Endocrine Sensitivity in ER+/HER2- Metastatic Breast Cancer

819 | Jul 01 2020

Lanell M Peterson et al. found that Simultaneous HDACi and AI dosing in patients with cancers resistant to AI alone showed clinical benefit (6+ months without progression) in 4 of 10 evaluable patients. [Read the Full Post]

Imaging Assisted Evaluation of Antitumor Efficacy of a New Histone Deacetylase Inhibitor in the Castration-Resistant Prostate Cancer

751 | Jul 01 2020

Zude Chen et al. provided not only a novel epigenetic approach for prostate cancer therapy but also offering a potential tool, [11C] Martinostat PET/CT imaging, to detect the early phase of prostate cancer and monitor therapeutic effect of CN133. [Read the Full Post]

Sulfobutylether-β-cyclodextrin /5,10,15,20-tetrakis(1-methylpyridinium-4-yl)porphine Nanoassemblies With Sustained Antimicrobial Phototherapeutic Action

548 | Jun 08 2020

Roberto Zagami et al. proposed the design and characterization of a novel nanophototherapeutic based on the trade cyclodextrin CAPTISOL® (sulfobutylether-beta-cyclodextrin, SBE-βCD) and 5,10,15,20-tetrakis(1-methylpyridinium-4-yl)porphine tetrakis(p-toluenesulfonate) (TMPyP) to fabricate efficient biocompatible systems for aPDT. [Read the Full Post]

Cell Cycle Arrest and Apoptosis Are Not Dependent on p53 Prior to p53-dependent Embryonic Stem Cell Differentiation

1259 | Jun 02 2020

Sushil K Jaiswal et al. found that the multiple roles of p53 in cell cycle regulation and apoptosis were first acquired during pluripotent stem cell differentiation. [Read the Full Post]

Effects of the Preparation Method on the Formation of True Nimodipine SBE-β-CD/HP-β-CD Inclusion Complexes and Their Dissolution Rates Enhancement

0 | Mar 31 2020

Semcheddine F et al. showed that all the products exhibited higher dissolution rate than those of the physical mixtures and ND alone, in all mediums. However, the kneading complexes displayed the maximum dissolution rate in comparison with drug and other complexes, confirming the influence of the preparation method on the physicochemical properties of the products. [Read the Full Post]

Effects of the Preparation Method on the Formation of True Nimodipine SBE-β-CD/HP-β-CD Inclusion Complexes and Their Dissolution Rates Enhancement

1076 | Feb 18 2020

Farouk Semcheddine et al. showed that all the products exhibited higher dissolution rate than those of the physical mixtures and ND alone, in all mediums. However, the kneading complexes displayed the maximum dissolution rate in comparison with drug and other complexes, confirming the influence of the preparation method on the physicochemical properties of the products. [Read the Full Post]

Safety and efficacy of elvitegravir, dolutegravir, and raltegravir in a real-world cohort of treatment-naïve and -experienced patients

889 | Nov 06 2019

Brehm TT et al. showed that side effects were only rarely observed and generally mild in all subgroups. In light of a slightly higher incidence of vertigo and sleep disturbances in patients switched to DTG, awareness of the potential onset of psychiatric symptoms is warranted during follow-up in those patients. [Read the Full Post]

Supramolecular Nanorods of (N-Methylpyridyl) Porphyrin With Captisol: Effective Photosensitizer for Anti-bacterial and Anti-tumor Activitie

589 | Aug 05 2019

Khurana R et al. indicatted that all these synergistic effects of supramolecular nanorods of Captisol-TMPyP complex make the system an effective photosensitizer and a superior antibacterial and antitumor agent. [Read the Full Post]

Associated-Extraction Efficiency of Six Cyclodextrins on Various Flavonoids in Puerariae Lobatae Radix

540 | Jul 05 2019

Feng T et al. indicated that CDs, especially SBE-β-CD, have a promising application for the associated-extraction of flavonoids from PLR. [Read the Full Post]

In Vitro Activity of Sitafloxacin and Additional Newer Generation Fluoroquinolones Against Ciprofloxacin-Resistant Neisseria gonorrhoeae Isolates

475 | Jul 01 2019

Hamasuna R et al. indicated that sitafloxacin should not be considered for empirical first-line monotherapy of gonorrhea. However, sitafloxacin could be valuable in a dual antimicrobial therapy and for cases with ceftriaxone resistance or allergy. [Read the Full Post]

Raltegravir (MK-0518): an integrase inhibitor for the treatment of HIV-1

483 | Jun 20 2019

Evering TH et al. indicated it has demonstrated a favorable side-effect profile in treatment-naive and -experienced patients and a subset of heavy treatment-experienced patients have been able a achieve virologic suppression with raltegravir as part of combination therapy despite limited treatment options. [Read the Full Post]

Puromycin reaction for the A site-bound peptidyl-tRNA

502 | Jun 16 2019

Semenkov Yu et al. indicated that the transpeptidation reaction per se triggers conformational changes in the ribosomal complex bringing the 3'-end of a newly synthesized peptidyl-tRNA nearer to the peptidyl-site of the peptidyltransferase center. This is detected functionally as the ability of such an A site bound peptidyl-tRNA to react with puromycin. This reaction is highly pronounced at elevated (25 degrees C) temperature but can be hardly detected at 0 degrees C. [Read the Full Post]

In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor

519 | May 28 2019

Kobayashi M et al. demonstrated that S/GSK1349572 would be classified as a next-generation drug in the integrase inhibitor class, with a resistance profile markedly different from that of first-generation integrase inhibitors. [Read the Full Post]

Coformulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection (GS-US-380-1490): a randomised, double-blind, multicentre, phase 3, non-inferiority trial

574 | May 08 2019

Sax PE et al. indicated at 48 weeks, virological suppression with the bictegravir regimen was achieved and was non-inferior to the dolutegravir regimen in previously untreated adults. There was no emergent resistance to either regimen. The fixed-dose combination of bictegravir, emtricitabine, and tenofovir alafenamide was safe and well tolerated compared with the dolutegravir regimen. [Read the Full Post]

MK2206 enhances the cytocidal effects of bufalin in multiple myeloma by inhibiting the AKT/mTOR pathway

569 | Jan 11 2019

Xiang RF et al. suggested that MK2206 significantly enhanced the cytocidal effects of bufalin in MM cells, regardless of the sensitivity to bortezomib, via the inhibition of the AKT/mTOR pathway. The study provided the basis of a promising treatment approach for MM. [Read the Full Post]

Micafungin-Induced Suicidal Erythrocyte Death

602 | Nov 14 2018

Peter T et al. showed effect of Micafungin on annexin-V-binding was not significantly modified by removal of extracellular Ca2+, by PKC inhibitor staurosporine (1 µM), p38 kinase inhibitor SB203580 (2 µM), casein kinase 1α inhibitor D4476 (10 µM) or pancaspase inhibitor zVAD (10 µM). [Read the Full Post]

Smac mimetic with TNF-α targets Pim-1 isoforms and reactive oxygen species production to abrogate transformation from blebbishields

1639 | Oct 29 2018

Jinesh GG et al. demonstrated that Smac mimetic in combination with TNF-α is an ideal candidate to target Pim-1 expression, inhibit ROS production and to block transformation from blebbishields. [Read the Full Post]

Antimicrobial susceptibility testing of rapidly growing mycobacteria isolated in Japan

841 | Oct 28 2018

Hatakeyama S et al. demonstrated the importance of correct identification and antimicrobial susceptibility testing, including the testing of potential new agents, in the management of RGM infections. [Read the Full Post]

Tumor Necrosis Factor Inhibits Spread of Hepatitis C Virus Among Liver Cells, Independent From Interferons

939 | Oct 10 2018

Laidlaw SM et al. found TNF to have antiviral effects independently of, as well as in combination with, IFNs. TNF inhibits HCV infection despite increased HCV envelope glycoprotein-mediated infection of liver cells. These findings contradict those from other studies, which have reported that TNF blocks signal transduction in response to IFNs. The destructive inflammatory effects of TNF must be considered along with its antiviral effects. [Read the Full Post]

PTC725, an NS4B-Targeting Compound, Inhibits a Hepatitis C Virus Genotype 3 Replicon, as Predicted by Genome Sequence Analysis and Determined Experimentally

0 | Oct 09 2018

Graci JD et al. identified previously unreported amino acid substitutions selected by PTC725 treatment which further demonstrate that these compounds target the NS4B first transmembrane region. [Read the Full Post]

Inhibition of Histone Deacetylase Activity Aggravates Coxsackievirus B3-Induced Myocarditis by Promoting Viral Replication and Myocardial Apoptosis

624 | Sep 08 2018

Zhou L et al. found inhibition of HDAC activity enhanced myocardial autophagosome formation, which led to the elevated CVB3 viral replication and ensuing increased myocardial apoptosis. [Read the Full Post]

Hepatitis C Virus NS4B Can Suppress STING Accumulation To Evade Innate Immune Responses

1238 | Aug 13 2018

Yi G et al. showed that 2a/JFH1 NS4B has an additional mechanism to evade STING signaling through suppressing STING accumulation. [Read the Full Post]

A profiling study of a newly developed HCVcc strain PR63cc's sensitivity to direct-acting antivirals

1232 | Aug 12 2018

Tao W et al. showed that PR63cc was more resistant than JFH1 to the asunaprevir/daclatasvir combination treatment. In summary, our study systemically analyzed the DAA sensitivity of a new HCVcc strain and identified critical RAVs. These results are not only important for monitoring the emergence of drug-resistant mutations of current DAA therapies, but also valuable for developing next-generation DAAs. [Read the Full Post]

A simple and cost-saving phenotypic drug susceptibility testing of HIV-1

1505 | Jul 05 2018

Weng Y et al. provided a useful tool for interpreting meaningful genotypic mutations and guiding tailored antiviral treatment of HIV/AIDS in clinical practice. [Read the Full Post]

Dissecting the molecular mechanisms that impair stress granule formation in aging cells

1191 | Jul 04 2018

Moujaber O et al. demonstrated that the loss of CReP correlated with the aging-related hyperphosphorylation of eIF2α. Together, we have identified significant changes in the stress response of aging cells and provide mechanistic insights. Based on our work, we propose that the decline in SG formation can provide a new biomarker to evaluate cellular aging. [Read the Full Post]

HMGB1-mediated autophagy decreases sensitivity to oxymatrine in SW982 human synovial sarcoma cells

1324 | May 13 2018

Cai Y et al. showed that combining OMT with an inhibitor of autophagy or HMGB1 may make OMT more effective in the treatment of human synovial sarcoma. [Read the Full Post]

In silico prediction and in vitro and in vivo validation of acaricide fluazuron as a potential inhibitor of FGFR3 and a candidate anticancer drug for bladder carcinoma

879 | Apr 20 2018

Ke K et al. suggested for the first time that fluazuron is a potential inhibitor of FGFR3 and a candidate anticancer drug for the treatment of BC. [Read the Full Post]

Susceptibility of porcine endogenous retrovirus to anti-retroviral inhibitors

775 | Apr 09 2018

Argaw T et al. indicated that some of the licensed anti-retroviral drugs may be useful for controlling PERV infection. However, the efficacy at nanomolar concentrations put forward integrase inhibitors as a drug that has the potential to be useful in the event that xenotransplantation recipients have evidence of PERV transmission and replication. [Read the Full Post]

In Vitro Antibacterial Activity of Rhodanine Derivatives against Pathogenic Clinical Isolates

1364 | Mar 08 2018

AbdelKhalek A et al. suggested that certain rhodanine compounds may have potential use for the treatment of several multidrug-resistant Gram-positive bacterial infections. [Read the Full Post]

Membrane Interactions of Natural Cyclic Lipodepsipeptides of the Viscosin Group.

957 | Feb 18 2018

Geudens N, et al. found that the CLPs interact both with the polar heads and aliphatic tails of model membrane systems, altering bilayer fluidity, while cholesterol reduces CLP insertion depth. [Read the Full Post]

Antibacterial activity and mechanism of action of auranofin against multi-drug resistant bacterial pathogens

1163 | Feb 03 2018

Thangamani S et al. provided valuable evidence that auranofin has significant promise to be repurposed as a novel antibacterial for treatment of invasive bacterial infections. [Read the Full Post]

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H

982 | Jan 11 2018

Corona A et al. provided new structural information to modulate IN and RNase H inhibitory activities for development of dual-acting anti-HIV agents. [Read the Full Post]

Repurposing auranofin for the treatment of cutaneous staphylococcal infections

1077 | Jan 06 2018

Thangamani S et al. supported that auranofin has potential to be repurposed as a topical antimicrobial agent for the treatment of staphylococcal skin and wound infections. [Read the Full Post]

PTC725, an NS4B-Targeting Compound, Inhibits a Hepatitis C Virus Genotype 3 Replicon, as Predicted by Genome Sequence Analysis and Determined Experimentally.

1516 | Dec 29 2017

Graci JD et al. identified previously unreported amino acid substitutions selected by PTC725 treatment which further demonstrate that these compounds target the NS4B first transmembrane region. [Read the Full Post]

Anidulafungin-Induced Suicidal Erythrocyte Death

0 | Nov 01 2017

Anidulafungin triggers hemolysis and eryptosis with cell shrinkage and phospholipid scrambling of the erythrocyte cell membrane, an effect in part due to Ca2+ entry and activation of p38 kinase. [Read the Full Post]

Ebola VP40 in Exosomes Can Cause Immune Cell Dysfunction

1101 | Sep 24 2017

Dosch JS et al. suggested that the use of drugs such as Oxytetracycline to modulate the levels of exosomes exiting EBOV-infected cells may be able to prevent the devastation of the adaptive immune system and allow for an improved rate of survival. [Read the Full Post]

Cancer stem cell marker phenotypes are reversible and functionally homogeneous in a preclinical model of pancreatic cancer

1624 | Sep 24 2017

Dosch JS, et al. showed that the hierarchical organization of CSCs in human disease is not recapitulated in a commonly used mouse model of pancreatic cancer and therefore provide a new view of the phenotypic and functional heterogeneity of tumor cells. [Read the Full Post]

Antiviral activity of micafungin against enterovirus 71

0 | Aug 05 2017

Kim C et al. identified micafungin, an echinocandin antifungal drug, as a novel inhibitor of EV71. [Read the Full Post]

Cryo-EM reveals a novel octameric integrase structure for betaretroviral intasome function

1315 | Jun 17 2017

Ballandras-Colas A et al. revealed a novel octameric integrase structure for betaretroviral intasome function. [Read the Full Post]

Selectivity for strand-transfer over 3'-processing and susceptibility to clinical resistance of HIV-1 integrase inhibitors are driven by key enzyme-DNA interactions in the active site

1278 | May 13 2017

Métifiot M et al. indicated that the conserved residue Q146 in the flexible loop of HIV-1 integrase is critical for productive viral DNA binding through specific contacts with the virus DNA ends in the 3'-processing and ST reactions. [Read the Full Post]

CD4+ T cell–dependent and –independent cytokine-chemokine network changes in the immune responses of HIV-infected individuals

3751 | Mar 20 2017

Arnold KB et al identified a critical deficiency in NK cell responses of HIV-infected individuals, independent of CD4(+) T cell depletion, which directs secreted profiles. Our findings illustrate a broad approach for identifying key disease-associated nodes in a multicellular, multivariate signaling network. [Read the Full Post]

Solitary inhibition of the breast cancer resistance protein (BCRP) efflux transporter results in a clinically significant drug-drug interaction with rosuvastatin by causing up to a two-fold increase in statin exposure

2581 | Feb 25 2017

Elsby R, et al.'s result shows that solitary inhibition of the intestinal BCRP transporter can result in clinically significant DDIs with rosuvastatin, causing up to a maximum 2-fold increase in exposure, which may warrant statin dose adjustment in clinical practice [Read the Full Post]

Understanding the molecular mechanism of host-based statin resistance in hepatitis C virus replicon containing cells

2309 | Jan 28 2017

Delang L et al. demonstrated that statin resistance in HCV replicon containing hepatoma cells is conferred by changes in the cellular environment. [Read the Full Post]

CD4+ T cell–dependent and –independent cytokine-chemokine network changes in the immune responses of HIV-infected individuals

3874 | Jan 24 2017

Arnold KB, et al. identified a critical deficiency in NK cell responses of HIV-infected individuals, independent of CD4(+) T cell depletion, which directs secreted profiles. Our findings illustrate a broad approach for identifying key disease-associated nodes in a multicellular, multivariate signaling network. [Read the Full Post]

Linking IFNα to apolipoprotein A-I provides a novel therapy of chronic hepadnavirus infection

2456 | Mar 25 2015

Berrondo et al. demonstrated a molecule called InterApo (IA) with IFNα links to apolipoprotein A-I, has antiviral and immunostimulatory activities and lacks IFNα-induced hematological toxicity. In this study, they further explore the safety of IA for chronic HBV infection. [Read the Full Post]

Semen suppresses antiviral activities of microbicides against HIV

2956 | Nov 25 2014

Zirafi et al. reported that microbicides, which can target HIV components, showed ineffective in the presence of semen. [Read the Full Post]

BMS 790052 is the most potent hepatitis C virus inhibitor

4524 | Nov 13 2013

BMS-790052 is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3. [Read the Full Post]

Telaprevir is an associate of a class of antiviral drugs

4622 | Mar 21 2013

Telaprevir is an associate of a class of antiviral drugs called protease inhibitors. Especially, telaprevir prevents the hepatitis C viral enzyme NS3.4A serine protease. Telaprevir is just indicated for use against hepatitis d genotype 1 viral infections and hasnt been which can have an impact on or being protected when employed for other genotypes of the herpes virus. The standard therapy of ribavirin and pegylated interferon is less successful on genotype 1 and a welcome addition is offered by telaprevir to the treatment of this genotype. [Read the Full Post]

Raltegravir is an antiretroviral drug produced by Merck and Co

2878 | Dec 12 2012

Epigenetic marks play a major role in the control of cell fate during mammalian development. Among these, the most studied so far is lysine acetylation, a posttranslational modification of histones which inactivates the positive Raltegravir charge of lysines. [Read the Full Post]

Telaprevir has very poor penetration of the blood brain

5548 | Nov 15 2012

The principal metabolic fate of loperamide in humans involves oxidative N dealkylation to N demethyl loperamide as the principal metabolite. In human liver microsomes, cytochrome P450 3A4 appears to be the major isozyme responsible for loperamide metabolism, with minor contributions from CYP2B6 [Read the Full Post]

BMS-790052 A Tr droplets With twice as many cells pressed

4530 | Oct 23 2012

BMS-790052 A Tr droplets With twice as many cells pressed agA Tr droplets, With twice as many cells pressed against the heart tee h Here cAMP concentration against each other, the proportion of droplets tears reported a positive response [Read the Full Post]

RALTEGRAVIR- AN INTEGRASE INHIBITOR

3637 | Jul 30 2012

HIV-I AND INTEGRASE HIV one of the most tricky viruses on earth that cause immunodeficiency in humans is being studied allot. It is responsible for a deathly disease known AIDS which is a focus of attention of many researchers since last decades. Due to its wide spread and occurrence throughout the world has compelled the scientists to look for a drug that may effectively cure the disease. HIV contains different types of enzymes and genes that help it to utilize the genes and proteins of its host. The most important among all is the integrase enzyme that helps it in integration of its genome into that of the host. Integrase has been an attractive target for the devising a therapy against the disease. A lot of research is being done on integrase inhibitors and several integrase inhibitors have been discovered by high throughput screening that prevent the integration of genome of virus into that of the host hence preventing the proliferation of the host cell. These inhibitors have shown efficacious results when used against HIV-I. One of the examples of such inhibitors is Raltegravir integrase inhibitor. This drug is first of such inhibitors to get FDA approval and is a blessing for the patients of HIV. [Read the Full Post]

RALTEGRAVIR- FAMOUS INTEGRASE INHIBITOR

3957 | Jun 03 2012

INTEGRASE IN CASE OF HIV-1 The most deathly disease on earth, HIV-I, is being researched and studied a lot to find out an effective therapy against it. This virus contains some genes for enzymes/proteins and utilizes some others from the host cells. The enzyme in HIV that helps the virus to integrate its genome into host cell/genome is named as Integrase and gets replicated there. To search for the [roper treatment the first thing that must be keep in mind is resistance development by the mutation of their genes during replication, so it is the need of hour that the research about treatment of cancer must go on further and should be regularly updated. To inhibit their enzymatic activity is an attractive approach. The inhibitors for integrase enzyme have been developed and they inhibit the process of integration of viral genome into the host genome hence prevent its proliferation in the hosting cell. A huge wave of research is going on HIV-I regarding integrase inhibitors that offer promising results against HIV-I virus. Raltegravir integrase inhibitor is such an inhibitor that inhibits the integrase enzyme and it is the first inhibitor to get approved from FDA and its discovery is no doubt considered to be a great blessing. [Read the Full Post]

RALTEGRAVIR- AN INTEGRASE INHIBITOR

4023 | Apr 27 2012

INTEGRASE AND HIV-1 HIV-I, one of the deathly diseases present on earth, is being researched a lot in order to find an efficacious therapy against it. The virus contains some of the genes for proteins/enzymes and utilizes some from the host. Integrase is one of the enzymes present in virus that helps it to integrate its genome into the host genome and get itself replicated there. In order to search for the treatment, first thing that is kept in mind is the development of resistance by getting their genes mutated during replication, therefore it is need of the hour that research on the treatment against cancer must go on and should be updated. Inhibiting the enzymatic activity is one of the approaches. Inhibitors of integrase have also been developed that inhibit the integration of genome of the virus into that of the host and therefore prevent it to proliferate inside the host cell. A lot of research is going on HIV-I in the area of integrase inhibitors which offer new promises in for therapy against HIV-I. Raltegravir integrase inhibitor is one of such inhibitors and the first one to get approval from FDA and the discovery of which is considered a blessing. [Read the Full Post]

RALTEGRAVIR: A POTENT INTEGRASE INHIBITOR

2765 | Apr 01 2012

INTRODUCTION TO HIV-1 AND ITS TREATMENT: HIV-1 is amongst the most destructive viruses and its treatment regime always in a need of more and novel methods to treat this virus because any of the new drugs gives a short time benefit as the virus get resistant against that drug, therefore any of the effective and newly introduced drug is welcomed by the medical practitioners. In order to integrate the genome of virus it needs integrase enzyme, thus inhibitors to this enzyme are potential candidates to inhibit the viral replication inside host cells. For the development and discovery of these inhibitors a lot of work is being done for integrase inhibitors of HIV-1 these inhibitors are also offering new hopes for HIV-1 drugs. Raltegravir integrase inhibitor, first FDA approved HIV integrase inhibitor and the discovery of this inhibitor was much valued. [Read the Full Post]