Results of preclinical studies with a highly potent KRAS (G12D mutant) inhibitor for the treatment of cancer were recently reported by researchers from Betta Pharmaceuticals Co. Ltd. BPI-501836 displayed higher inhibitory activity at KRAS G12D, when compared to the reference compound (IC50=0.25 and 2.4 nM, respectively) in NanoBRET assays.
Researchers from Puhe Biopharma Co. Ltd. presented the discovery and preclinical evaluation of PH027-1, a novel small-molecule Werner syndrome protein (WRN) inhibitor targeting microsatellite instability high (MSI-H) tumors.
Obesity is a chronic disorder tied to other disorders such as hyperglycemia, type 2 diabetes or cardiovascular disease, among others. Recent findings have suggested that EphB tyrosine kinase receptor and its ligand, ephrin B, may be involved in insulin signaling.
ABM Therapeutics Inc. presented a novel small-molecule, ATP-uncompetitive, phosphorylated MEK (pMEK) inhibitor – ABM-4095 – that potently prevents phosphorylation of MEK by RAF with moderate inhibition of MEK kinase activity; it is being investigated for the potential treatment of pancreatic cancer.
Gram-negative bacteria require the metalloenzyme LpxC for their outer membrane biogenesis. Blacksmith Medicines Inc. has identified an LpxC inhibitor, FG-960, which has shown a robust in vitro and in vivo profile against multidrug-resistant Enterobacterales. FG-60 is currently being investigated for the treatment of urinary tract infections (UTIs).
Discovery of novel Nav1.8 inhibitors capable of achieving high levels of target modulation at low oral doses for the potential treatment of pain was reported by Merck & Co. Inc.
Researchers from West China Hospital of Sichuan University announced the discovery of homo sapiens caseinolytic protease P (HsClpP) agonists as new small-molecule candidates for the treatment of colorectal cancer.
To address the need for novel therapeutic candidates against Duchenne muscular dystrophy (DMD), investigators at Mitorx Therapeutics Ltd. developed a library of novel small-molecule mitochondriotropic agents.
Aryl hydrocarbon receptor (AhR) signaling regulates gene expression in immune and skin cells and plays a critical role in maintaining skin homeostasis.
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