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.
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.
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.
Human lipoprotein(a) (Lp(a)) is a lipoprotein complex composed of a low-density lipoprotein (LDL) particle and a large highly polymorphic glycoprotein named apolipoprotein (a) (apo(a)). There is evidence that Lp(a) is linked to cardiovascular disorder risk.
At the recent ESC Congress, researchers from University of Tennessee and Attralus Inc. presented preclinical data on the novel pan-amyloid-binding peptide fusion immunoglobulin AT-02, which is being developed for the treatment of amyloidosis.
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