Work at Bristol Myers Squibb Co. has led to the discovery of selective Toll-like receptor 7 (TLR7) agonists with potential as anticancer agents.

Researchers from Genentech Inc. have reported the discovery of new cyclin-dependent kinase 2 (CDK2) inhibitors as potential anticancer agents.

Molecular glue degraders are compounds intended to prompt the degradation of E3 ubiquitin ligases by engaging and modifying their surface. Molecular glue-induced protein degradation is considered an emerging strategy in drug discovery.

Researchers from Ashvattha Therapeutics LLC recently reported on ASH-41020, a new dendranib compound acting as a CSF-1R inhibitor with anti-inflammatory and immunomodulatory effects.

Current anticoagulant strategies include small-molecule inhibitors and biological entities targeting factor XI (FXI) which, although effective, still have bleeding as a major risk.

Monoacylglycerol lipase (MAGL), a member of the serine hydrolase family expressed in the brain and peripheral tissue, is a key enzyme in the hydrolysis of monoglycerides, converting 2-arachidonoyl glycerol (2-AG) into arachidonic acid and glycerol. MAGL inhibition has been previously shown to induce anxiolytic and analgesic phenotypes in animal models. Researchers from Janssen Pharmaceutica NV recently reported the discovery of novel noncovalent MAGL inhibitors.

Synthesis and optimization of a series of 1H-pyrazolo[4,3d]pyrimidine molecules at Bristol Myers Squibb Co. led to the identification of compound [I] as the lead Toll-like receptor 7 (TLR7) agonist, with EC50 values of 21 and 94 nM for human and mouse TLR7, respectively.

Interleukin-17A (IL-17A) is a pro-inflammatory cytokine involved in the pathogenesis of inflammatory, immune-mediated diseases such as psoriasis, psoriatic arthritis and others.

Apolipoprotein C3 (APOC3) is one of the main regulators of triglyceride metabolism. Hypertriglyceridemia (HTG) is a major risk factor for cardiovascular disease and there is evidence that loss-of-function mutations in APOC3 correlate with decreased plasma triglyceride levels and subsequent reduced cardiometabolic dysfunction.