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Regulating the Master Regulator: Controlling Ubiquitination by Thinking Outside the Active Site.

Abstract：

:The labeling of proteins with ubiquitin/ubiquitin-like (Ubl) proteins is crucial for several physiological processes and in the onset of various diseases. Recently, targeting ubiquitin protein labeling has shifted toward the use of allosteric mechanisms over classical activity-based approaches. Allosteric enzyme regulation offers the potential for greater selectivity and has demonstrated less susceptibility to acquired resistance often associated with active site inhibitors. Furthermore, the isoform diversity among E1 activating, E2 conjugating, E3 ligase, and deubiquitinating (DUB) enzymes offers an ideal platform for modulating activity via allostery. Herein, we have reviewed allosteric inhibitors of the ubiquitin E1-E2-E3 and DUB enzymatic cascade developed over the past decade with a focus on their mechanisms of action. We have highlighted the advantages as well as the challenges associated with designing allosteric modulators of the ubiquitin labeling machinery, and the future promise in targeting these systems using allosteric approaches.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Paiva SL,da Silva SR,de Araujo ED,Gunning PT

doi

10.1021/acs.jmedchem.6b01346

subject

Has Abstract

pub_date

2018-01-25 00:00:00

pages

405-421

issue

2

eissn

0022-2623

issn

1520-4804

journal_volume

61

pub_type

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