Substrate-Selective Enzyme Inhibitors

Publication date: Available online 2 August 2019Source: Trends in Pharmacological SciencesAuthor(s): Qian Chu, Tina Chang, Alan SaghatelianEnzymes 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.
Source: Trends in Pharmacological Sciences - Category: Drugs & Pharmacology Source Type: research