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Repurposing of the FGFR inhibitor AZD4547 as a potent inhibitor of necroptosis by selectively targeting RIPK1
Necroptosis is a form of regulated necrosis involved in various pathological diseases. The process of necroptosis is controlled by...
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Discovery of a novel and highly selective JAK3 inhibitor as a potent hair growth promoter
JAK-STAT signalling pathway inhibitors have emerged as promising therapeutic agents for the treatment of hair loss. Among different JAK isoforms,...
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Identification and characterization of a new potent inhibitor targeting CtBP1/BARS in melanoma cells
BackgroundThe C-terminal-binding protein 1/brefeldin A ADP-ribosylation substrate (CtBP1/BARS) acts both as an oncogenic transcriptional co-repressor...
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Design, synthesis, and biological studies of the new cysteine-N-arylacetamide derivatives as a potent urease inhibitor
Inhibition of Helicobacter pylori urease is an effective method in the treatment of several gastrointestinal diseases in humans. This bacterium plays...
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Azithromycin, a potent autophagy inhibitor for cancer therapy, perturbs cytoskeletal protein dynamics
BackgroundAutophagy plays an important role in tumour cell growth and survival and also promotes resistance to chemotherapy. Hence, autophagy has...
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Sitravatinib as a potent FLT3 inhibitor can overcome gilteritinib resistance in acute myeloid leukemia
BackgroundGilteritinib is the only drug approved as monotherapy for acute myeloid leukemia (AML) patients harboring FMS-like tyrosine kinase 3...
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Discovery of toxoflavin, a potent IRE1α inhibitor acting through structure-dependent oxidative inhibition
Inositol-requiring enzyme 1α (IRE1α) is the most conserved endoplasmic reticulum (ER) stress sensor with two catalytic domains, kinase and RNase, in...
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143D, a novel selective KRASG12C inhibitor exhibits potent antitumor activity in preclinical models
The KRAS G12C mutant has emerged as an important therapeutic target in recent years. Covalent inhibitors have shown promising antitumor activity...
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MC180295 is a highly potent and selective CDK9 inhibitor with preclinical in vitro and in vivo efficacy in cancer
BackgroundInhibition of cyclin-dependent kinase 9 (CDK9), a novel epigenetic target in cancer, can reactivate epigenetically silenced genes in cancer...
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Identification of α-mangostin as a potent inhibitor of β-lactamase OXA-48
The production of carbapenemases is a significant mechanism contributing to carbapenem resistance in Enterobacteriaceae . Among these carbapenemases,...
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A clinical pharmacokinetic drug-drug interaction study between dextromethorphan and emvododstat, a potent anti-SARS-CoV-2 dihydroorotate dehydrogenase inhibitor
PurposeA therapeutic agent that targets both viral replication and the hyper-reactive immune response would offer a highly desirable treatment for...
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Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor
Recent progress in targeting KRAS G12C has provided both insight and inspiration for targeting alternative KRAS mutants. In this study, we evaluated...
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G6PDi-1 is a Potent Inhibitor of G6PDH and of Pentose Phosphate pathway-dependent Metabolic Processes in Cultured Primary Astrocytes
Glucose-6-phosphate dehydrogenase (G6PDH) catalyses the rate limiting first step of the oxidative part of the pentose phosphate pathway (PPP), which...
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In silico identification and in vitro validation of alpha-hederin as a potent inhibitor of Wnt/β-catenin signaling pathway in breast cancer stem cells
Cancer stem cells (CSCs) play a vital role in metastasis, recurrence and chemoresistance in breast cancer. β-catenin, which is a frequently over...
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Luvadaxistat: A Novel Potent and Selective d-Amino Acid Oxidase Inhibitor Improves Cognitive and Social Deficits in Rodent Models for Schizophrenia
N-methyl- d -aspartate (NMDA) receptor hypofunctionality is a well-studied hypothesis for schizophrenia pathophysiology, and daily dosing of the NMDA...
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Plant Essential Oils as Potent Antimicrobials
Antimicrobial resistance (AMR) is spreading at an alarming rate, reducing the effectiveness of antibiotics and producing undesirable results such as...
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Evaluation and identification of green pharmacophore as a potent inhibitor of human tyrosinase related protein 1 using molecular drug interaction, drug likeness and ADMET analyses
Skin is the largest organ of human body which is consistently exposed to various abiotic factors. Among all the environmental factors, ultraviolet...
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CHMFL-26 is a highly potent irreversible HER2 inhibitor for use in the treatment of HER2-positive and HER2-mutant cancers
Oncogene HER2 is amplified in 20%–25% of human breast cancers and 6.1%–23.0% of gastric cancers, and HER2-directed therapy significantly improves the...
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4-Hexylresorcinol as Histone Deacetylase Inhibitor
This chapter investigates the role of 4-hexylresorcinol (4HR) as a histone deacetylase inhibitor (HDACi) specifically targeting Class I and IIa HDACs...
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Preclinical Pharmacokinetics and Translational Pharmacokinetic/Pharmacodynamic Modeling of M8891, a Potent and Reversible Inhibitor of Methionine Aminopeptidase 2
IntroductionM8891 is a selective and reversible inhibitor of methionine aminopeptidase 2 (MetAP2). We describe translational research to define the...
