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ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

Blog of Signaling Pathways

Discovery of Novel Dual c-Met/HDAC Inhibitors as a Promising Strategy for Cancer Therapy

502 views | Jul 07 2020

Hao Hu et al. provided an efficient strategy for discovery of multitarget antitumor drugs. [Read the Full Post]

Berzosertib Plus Gemcitabine Versus Gemcitabine Alone in Platinum-Resistant High-Grade Serous Ovarian Cancer: A Multicentre, Open-Label, Randomised, Phase 2 Trial

356 views | Jul 06 2020

Panagiotis A Konstantinopoulos et al. showed a benefit of adding berzosertib to gemcitabine in platinum-resistant high-grade serous ovarian cancer. [Read the Full Post]

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

761 views | 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]

The Gαh/phospholipase C-δ1 Interaction Promotes Autophagosome Degradation by Activating the Akt/mTORC1 Pathway in Metastatic Triple-Negative Breast Cancer

319 views | Jul 05 2020

Hui-Yu Lin et al. demonstrated that the induction of autophagy activity or the inhibition of Akt-mTORC1 axis provided a useful strategy to combat the Gαh/PLC-δ1-driven LM of TNBC. [Read the Full Post]

Effect of Morphology on the Photoelectrochemical Performance of Nanostructured Cu2O Photocathodes

346 views | Jul 05 2020

Lian C T Shoute found that although different deposition methods showed a similar average photocurrent density 2.8±0.3 mA/cm2 at 0 V vs RHE, large variations in the photocurrent density were observed for samples prepared under nominally identical deposition methods. [Read the Full Post]

Efficacy of Gefitinib Combined With 125 I Radioactive Particles in the Treatment of Transplanted Lung Cancer Tumors in Nude Mice

594 views | Jul 02 2020

Chaojie Li et al. found that Gefitinib combined with 125I radioactive particles brachytherapy could significantly inhibit tumor growth. [Read the Full Post]

Differential Therapeutic Effects of PARP and ATR Inhibition Combined With Radiotherapy in the Treatment of Subcutaneous Versus Orthotopic Lung Tumour Models

319 views | Jul 02 2020

Vanessa Tran Chau et al. highlighted the importance of using more pathologically relevant models, such as syngeneic orthotopic models, to determine the most appropriate therapeutic approaches for translation to the clinic. [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

715 views | 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

671 views | 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]

MEK Inhibitors Combined With Programmed Cell death-1 Blockade Immunotherapy for Metastatic Uveal Melanoma: Is It Warranted?

370 views | Jun 30 2020

Anais Zanella et al. highlighted the need to evaluate the safety and efficacy of new treatment options such as MEKi and anti-PD-1 for mUM. [Read the Full Post]

A New Compound With Increased Antitumor Activity by Cotargeting MEK and Pim-1

386 views | Jun 30 2020

Yanan Li et al. uncovered a new MEK inhibitor KZ-02 with significantly enhanced antitumor activity by co-targeting MEK and Pim-1. [Read the Full Post]

Quantification and Pharmacokinetic Property of Verubecestat an BACE1 Inhibitor in Rat Plasma

319 views | Jun 29 2020

Qiong Wang et al. designed an ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) approach to measure the rat plasma levels of verubecestat with diazepam as the internal standard. [Read the Full Post]

Targeting BCL-2 Proteins in Pediatric Cancer: Dual Inhibition of BCL-X L and MCL-1 Leads to Rapid Induction of Intrinsic Apoptosis

237 views | Jun 29 2020

Sarah Kehr et al. demonstrated the potency of A-1331852/S63845 in pediatric solid tumor cells and to describe the molecular mechanisms of A-1331852/S63845 co-treatment underlining the potential of BCL-XL and MCL-1 inhibition as treatment regime. [Read the Full Post]

Volumetric Absorptive Microsampling (VAMS) for Assaying Immunosuppressants From Venous Whole Blood by LC-MS/MS Using a Novel Atmospheric Pressure Ionization Probe (UniSpray™)

1672 views | Jun 28 2020

Lucía Paniagua-González et al. showed that venous blood VAMS concentrations were correlated to those found in the original liquid venous blood, proving that the VAMS material itself will not bias blood drug concentrations. [Read the Full Post]

HMTase Inhibitors as a Potential Epigenetic-Based Therapeutic Approach for Friedreich's Ataxia

510 views | Jun 28 2020

Mursal Sherzai et al. showed that a combination treatment of BIX0194 and GSK126, significantly increased FXN gene expression levels and reduced the repressive histone marks. However, no increase in frataxin protein levels was observed. [Read the Full Post]

Sequential Bortezomib and Temozolomide Treatment Promotes Immunological Responses in Glioblastoma Patients With Positive Clinical Outcomes: A Phase 1B Study

828 views | Jun 25 2020

Mohummad A Rahman et al. found that Sequential BTZ + TMZ treatment was safe and promotes Th1-driven immunological responsed in selected patients with improved clinical outcomes (Clinicaltrial.gov (NCT03643549)). [Read the Full Post]

In Vitro and In Vivo Efficacy of AZD3965 and Alpha-Cyano-4-Hydroxycinnamic Acid in the Murine 4T1 Breast Tumor Model

338 views | Jun 25 2020

Xiaowen Guan et al. indicated AZD3965 was a potent MCT1 inhibitor that accumulated to high concentrations in 4T1 xenograft tumors, where it increased tumor lactate concentrations and produced beneficial effects on markers of TNBC [Read the Full Post]

Anti-Inflammatory Properties of Chemical Probes in Human Whole Blood: Focus on Prostaglandin E 2 Production

305 views | Jun 24 2020

Filip Bergqvist et al. deployed a semi-high throughput and robust methodology to investigate anti-inflammatory properties of new chemical probes. [Read the Full Post]

Analysis of Dual Class I Histone Deacetylase and Lysine Demethylase Inhibitor Domatinostat (4SC-202) on Growth and Cellular and Genomic Landscape of Atypical Teratoid/Rhabdoid

401 views | Jun 24 2020

Mariah M Hoffman et al. indicated that 4SC-202 had both cytotoxic and cytostatic effects on ATRT, targets specific cell sub-populations, including those with cancer stem-like features, and was an important potential cancer therapeutic to be investigated in vivo. [Read the Full Post]

Disrupting Phosphatase SHP2 in Macrophages Protects Mice From High-Fat Diet-Induced Hepatic Steatosis and Insulin Resistance by Elevating IL-18 Levels

289 views | Jun 23 2020

Wen Liu et al. concluded that pharmacological inhibition of SHP2 might represent a possible therapeutic strategy for the management of type 2 diabetes. [Read the Full Post]