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Trends Pharmacol Sci. 2019 Oct;40(10):716-718. doi: 10.1016/j.tips.2019.07.009. Epub 2019 Aug 2.

Substrate-Selective Enzyme Inhibitors.

Author information

1
The Salk Institute for Biological Studies, Clayton Foundation Laboratories for Peptide Biology, 10010 N. Torrey Pines Rd, La Jolla, CA 92037, USA.
2
The Salk Institute for Biological Studies, Clayton Foundation Laboratories for Peptide Biology, 10010 N. Torrey Pines Rd, La Jolla, CA 92037, USA. Electronic address: asaghatelian@salk.edu.

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.

KEYWORDS:

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

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

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