Substrate-Selective Enzyme Inhibitors. (October 2019)

• Record Type: Journal Article
• Authors: Chu, Qian; Chang, Tina; Saghatelian, Alan
• Is Part Of: Trends in pharmacological sciences. Volume 40:Number 10(2019)
• Page Start: 716
• Page End: 718
• Publication Date: 2019-10
• Subjects: substrate-selective inhibition -- exo site -- insulin-degrading enzyme -- enzyme reprogramming -- chemical biology; Pharmacology -- Periodicals; Pharmacology -- trends -- Periodicals; Pharmacologie -- Périodiques; Pharmacology; Electronic journals; Periodicals; 615.1
• DOI: 10.1016/j.tips.2019.07.009
• Languages: English
• ISSNs: 0165-6147

Abstract

Abstract : Enzymes with multiple substrates pose a unique challenge for drug development because of an increased potential for on-target side effects. Maianti and colleagues ( Nat. Chem. Biol., 2019) identify novel exo-site inhibitors with abilities to alter the substrate-selectivity of insulin-degrading enzymes (IDE). Their work illuminates new therapeutic avenues for discovering small-molecule enzyme inhibitors and redefines our current understanding of drugging enzymes with multiple substrates.