Literature DB >> 31383375

Substrate-Selective Enzyme Inhibitors.

Qian Chu1, Tina Chang1, Alan Saghatelian2.   

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.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  chemical biology; enzyme reprogramming; exo site; insulin-degrading enzyme; substrate-selective inhibition

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Substances:

Year:  2019        PMID: 31383375     DOI: 10.1016/j.tips.2019.07.009

Source DB:  PubMed          Journal:  Trends Pharmacol Sci        ISSN: 0165-6147            Impact factor:   14.819


  1 in total

1.  Hydroxypyridinethione Inhibitors of Human Insulin-Degrading Enzyme.

Authors:  Rebecca N Adamek; Caitlin N Suire; Ryjul W Stokes; Monica K Brizuela; Seth M Cohen; Malcolm A Leissring
Journal:  ChemMedChem       Date:  2021-03-31       Impact factor: 3.466

  1 in total

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