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.
Rapidly evolving artificial intelligence (AI) is effectively resetting all biopharmaceutical companies to the figurative starting line, and collaboration is a key strategy to winning the drug discovery race, an AI-based startup founder said at the Global Bio Conference (GBC) 2023.
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.
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.
Interleukin-1 receptor-associated kinase 4 (IRAK4) plays a critical role in innate immunity by acting both as a scaffolding protein and a protein kinase, and its overactivation correlates with several autoimmune disorders.
Throughout the body, the vasculature and the nervous system are fellow travelers. Renaissance physician and anatomist Andreas Vesalius described their proximity on the macroanatomical level in the 16th century, and modern microscopic techniques have shown that it extends into the micrometer range – where there is a blood vessel, there is often a nerve nearby, and vice versa.
“Change is the only constant” is an ageless truth. In the search for age-related biomarkers, it is also a prosaic confounding factor.
Age-related biomarkers will be critical for the development of antiaging therapeutics. “Nobody is planning to do a life span study in humans,” Eric Verdin told the audience at the 10th Conference on Aging Research and Drug Development in Copenhagen on Monday. “Hence the need for … surrogate markers.”
Researchers from Genentech Inc. presented preclinical data for the novel transient receptor potential ankyrin 1 (TRPA1) antagonist GDC-6599, currently in phase II development for respiratory indications.