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.
Development and optimization of novel oral selective hematopoietic progenitor kinase 1 (HPK1) inhibitors for immuno-oncology (IO) treatment were reported by scientists from Astrazeneca plc in two presentations during the ACS meeting this week.
Rigel Pharmaceuticals Inc. presented findings from collaborative work with Medpharm that identified R-209, an interleukin-1 receptor-associated kinase 1 and 4 (IRAK-1/4) inhibitor with optimized properties for topical application.
Merck & Co. has revealed the discovery of novel oral SARS-CoV-2 3C-like proteinase (3CLpro; Mpro) inhibitors for the potential treatment and/or prophylaxis of COVID-19. 3CLpro plays a key role in viral life cycle by cleaving viral protein and helps in replication and infection, which make 3CLpro a target for designing drugs to treat COVID-19.
Researchers from the University of Illinois at Chicago and University of Arizona presented the discovery and preclinical evaluation of a novel BD1-selective BET inhibitor, XL-126, being developed as a potential anti-inflammatory agent.
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