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Blog of Signaling Pathways

Structural Basis of Activin Receptor-Like Kinase 2 (R206H) Inhibition by Bis-heteroaryl Pyrazole-Based Inhibitors for the Treatment of Fibrodysplasia Ossificans Progressiva Identified by the Integration of Ligand-Based and Structure-Based Drug Design Approaches

345 views | Sep 13 2020

Tomohiro Sato et al. indicated the existence of the additional hydrogen bond via water molecules restricting the attachment point in the pyrazole scaffold [Read the Full Post]

Quizartinib for the treatment of acute myeloid leukemia

437 views | Sep 13 2020

Alejandro Garcia-Horton et al. reviewed the mechanism of action, pharmacology, clinical efficacy, and safety of quizartinib, a FLT3 inhibitor, for the treatment of acute myeloid leukemia. [Read the Full Post]

Gefitinib Versus Gefitinib Plus Pemetrexed and Carboplatin Chemotherapy in EGFR-Mutated Lung Cancer

0 views | Sep 11 2020

Vanita Noronha et al. found that adding pemetrexed and carboplatin chemotherapy to gefitinib significantly prolonged PFS and OS but increased toxicity in patients with NSCLC. [Read the Full Post]

Combined PARP and ATR inhibition potentiates genome instability and cell death in ATM-deficient cancer cells

277 views | Sep 11 2020

Rebecca L Lloyd et al. provided a mechanistic understanding of combined PARP and ATR inhibition in ATM-deficient models, and supported the clinical development of AZD6738 in combination with olaparib. [Read the Full Post]

Anti-inflammatory Effect of AZD6244 on Acrolein-Induced Neuroinflammation

373 views | Sep 10 2020

Wen-Chien Ho et al. suggested that ERK inhibition may be a neuroprotective target against acrolein-induced neuroinflammation in the CNS neurodegenerative diseases. [Read the Full Post]

Fluvastatin potentiates anticancer activity of vorinostat in renal cancer cells

672 views | 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]

Dual inhibition of Src and PLK1 regulate stemness and induce apoptosis through Notch1-SOX2 signaling in EGFRvIII positive glioma stem cells (GSCs)

501 views | Sep 09 2020

Xuetao Li et al. indicated that p-Src and PLK1 contributed to cancer stemness in EGFRvIII-positive GSCs by driving Notch1-SOX2 signaling, a finding that had important clinical implications. [Read the Full Post]

IGF2BP1 is a targetable SRC/MAPK-dependent driver of invasive growth in ovarian cancer

539 views | Sep 09 2020

Nadine Bley et al. provided a rationale for the therapeutic benefit of combinatorial SRC/MEK inhibition in mesenchymal-like HGSOC. [Read the Full Post]

Effective Reconstruction of Functional Urethra Promoted With ICG-001 Delivery Using Core-Shell Collagen/Poly(Llactide-co-caprolactone) [P(LLA-CL)] Nanoyarn-Based Scaffold: A Study in Dog Model

354 views | Sep 08 2020

Kaile Zhang et al. applied a novel drug-delivering nanoyarn scaffold in urethroplasty in dog model, which continuously delivered ICG-001 during tissue reconstruction, and could effectively promote urethral recovery and resume fully functional urethra within 12 weeks. [Read the Full Post]

Sotrastaurin, a PKC inhibitor, attenuates RANKL-induced bone resorption and attenuates osteochondral pathologies associated with the development of OA

380 views | Sep 08 2020

Cong Pang et al. provided evidence for the protective effects of SO against OA by preventing aberrant subchondral bone and articular cartilage changes. [Read the Full Post]

Inhibition of DNA-PKcs activity re-sensitizes uveal melanoma cells to radio- and chemotherapy

472 views | Sep 03 2020

Bingjie Zhang et al. demonstrated increased DNA double strand break repair as a mechanism of resistance to ionizing radiation and Selumetinib, and identified DNA-PKcs as a promising target for radio-and chemotherapy in UM patients. [Read the Full Post]

Tyrosyl-DNA phosphodiesterase and the repair of 3'-phosphoglycolate-terminated DNA double-strand breaks

0 views | Sep 03 2020

Tong Zhou et al. suggested a role for TDP1 in repair of 3'-PG double-strand breaks in vivo. [Read the Full Post]

Mast cells (MCs) induce ductular reaction mimicking liver injury in mice via MC-derived TGF-β1 signaling

452 views | Sep 02 2020

Konstantina Kyritsi et al. demonstrated that reintroduction of MCs mimics cholestatic liver injury and MC-derived TGF-β1 might be a target in chronic cholestatic liver disease. [Read the Full Post]

In Vitro and In Vivo Activity, Tolerability, and Mechanism of Action of BX795 as an Antiviral against Herpes Simplex Virus 2 Genital Infection

447 views | Sep 02 2020

James Hopkins et al. revealed that the mechanism of action of BX795 antiviral activity stemed from the reduction of viral protein translation via inhibition of protein kinase B phosphorylation. [Read the Full Post]

An integrated drug repurposing strategy for the rapid identification of potential SARS-CoV-2 viral inhibitors

259 views | Sep 01 2020

Alfonso Trezza et al. showed that Simeprevir and Lumacaftor bound the receptor-binding domain of the Spike protein with high affinity and prevented ACE2 interaction. [Read the Full Post]

Bucladesine Attenuates Spatial Learning and Hippocampal Mitochondrial Impairments Induced by 3, 4-Methylenedioxymethamphetamine (MDMA)

435 views | Aug 31 2020

Ghorban Taghizadeh et al. highlighted the role of cAMP/PKA signaling in MDMA-induced memory and mitochondrial defects. [Read the Full Post]

Palmitate-TLR4 signaling regulates the histone demethylase, JMJD3, in macrophages and impairs diabetic wound healing

478 views | Aug 31 2020

Frank M Davis et al. concluded that palmitate contributed to the chronic Jmjd3-mediated activation of macrophages in diabetic peripheral tissue and a histone demethylase inhibitor-based therapy might represent a novel treatment for nonhealing diabetic wounds. [Read the Full Post]

Combined treatment with CBP and BET inhibitors reverses inadvertent activation of detrimental super enhancer programs in DIPG cells

359 views | Aug 30 2020

Maria Wiese et al. found that combinatorial treatment with CBP and BET inhibitors was highly efficient in H3K27M-mutant DIPG due to reversal of inadvertent activation of detrimental SE programs in comparison with monotherapy. [Read the Full Post]

Role of sirtuin-1 (SIRT1) in hypoxic injury in pancreatic β-cells

486 views | Aug 30 2020

Ye-Jee Lee et al. suggested that SIRT1 was a potential target for the protection of pancreatic β-cells against hypoxic damage during ITx. [Read the Full Post]

Low-Level Ionizing Radiation Induces Selective Killing of HIV-1-Infected Cells with Reversal of Cytokine Induction Using mTOR Inhibitors

177 views | Aug 28 2020

Daniel O Pinto et al. presented a novel approach allowing for the targeting of viral reservoirs, prevention of immune hyper-activation, and selectively killing latently infected HIV-1 cells. [Read the Full Post]