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Targeting Cullin-RING E3 Ubiquitin Ligase 4 by Small Molecule Modulators.


ABSTRACT: Cullin-RING E3 ubiquitin ligase 4 (CRL4) plays an essential role in cell cycle progression. Recent efforts using high throughput screening and follow up hit-to-lead studies have led to identification of small molecules 33-11 and KH-4-43 that inhibit E3 CRL4's core ligase complex and exhibit anticancer potential. This review provides: 1) an updated perspective of E3 CRL4, including structural organization, major substrate targets and role in cancer; 2) a discussion of the challenges and strategies for finding the CRL inhibitor; and 3) a summary of the properties of the identified CRL4 inhibitors as well as a perspective on their potential utility to probe CRL4 biology and act as therapeutic agents.

SUBMITTER: Wu K 

PROVIDER: S-EPMC8486283 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature

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Targeting Cullin-RING E3 Ubiquitin Ligase 4 by Small Molecule Modulators.

Wu Kenneth K   Hopkins Benjamin D BD   Sanchez Roberto R   DeVita Robert J RJ   Pan Zhen-Qiang ZQ  

Journal of cellular signaling 20210101 3


Cullin-RING E3 ubiquitin ligase 4 (CRL4) plays an essential role in cell cycle progression. Recent efforts using high throughput screening and follow up hit-to-lead studies have led to identification of small molecules <b>33-11</b> and <b>KH-4-43</b> that inhibit E3 CRL4's core ligase complex and exhibit anticancer potential. This review provides: 1) an updated perspective of E3 CRL4, including structural organization, major substrate targets and role in cancer; 2) a discussion of the challenges  ...[more]

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