Insulin-degrading enzyme (IDE) is a thiol-sensitive zinc-metallopeptidase that acts as the major insulin-degrading protease in vivo, mediating the termination of insulin signaling. [1] In addition to regulating insulin action in diabetes pathogenesis, IDE plays a role in Varicella-Zoster virus infection and degradation of amyloid-β, a peptide implicated in Alzheimer's disease. ML-345 is a small molecule inhibitor that selectively targets cysteine819 in IDE with an EC50 value of 188 nM. [2] It demonstrates 10-fold selectivity for IDE over a panel of enzymes with reactive cysteine residues.[2] Reference:[1]. Maianti, J.P., McFedries, A., Foda, Z.H., et al. Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones. Nature 511(7507), 94-98 (2014).[2]. Bannister, T.D., Wang, H., Abdul-Hay, S.O., et al. ML345, a small-molecule inhibitor of the insulin-degrading enzyme (IDE). 1 R03 DA024888-01 (MLSCN cycle 6), 1-41 (2014).
SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a highly potent inhibitor specifically designed to target and inhibit the activity of SARS-CoV-2 3CL pro, which is a cysteine-protease found in the main coronaviruses. This particular enzyme has been recognized as a highly promising target for the development of effective antiviral drugs. Therefore, SARS-CoV-2 3CLpro-IN-1 holds significant potential for advancing research and development in the field of infectious diseases [1].
Cathepsin K inhibitor 2 是一种 cathepsin K 的有效抑制剂。其中 Cathepsin K (Cat K) 是一种半胱氨酸蛋白酶,在 CTSK 基因调控下表达,与骨质疏松症密切相关,能够水解胶原蛋白。Cathepsin K inhibitor 2 对骨关节炎表现出研究潜力。