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PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes

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journal contribution
posted on 10.07.2020, 15:15 by Joshua P Smalley, Grace E Adams, Christopher J Millard, Yun Song, James KS Norris, John WR Schwabe, Shaun Michael Cowley, James T Hodgkinson
We have identified a proteolysis targeting chimera (PROTAC) of class I HDACs 1, 2 and 3. The most active degrader consists of a benzamide HDAC inhibitor, an alkyl linker, and the von Hippel-Lindau E3 ligand. Our PROTAC increased histone acetylation levels and compromised colon cancer HCT116 cell viability, establishing a degradation strategy as an alternative to class I HDAC inhibition.

History

Citation

Chem. Commun., 2020,56, 4476-4479

Author affiliation

Leicester Institute of Structural and Chemical Biology and Department of Chemistry

Version

AM (Accepted Manuscript)

Published in

Chemical Communications

Volume

56

Issue

32

Pagination

4476 - 4479

Publisher

Royal Society of Chemistry

issn

1359-7345

eissn

1364-548X

Acceptance date

11/03/2020

Copyright date

2020

Available date

11/03/2020

Spatial coverage

England

Language

English

Publisher version

https://pubs.rsc.org/en/content/articlelanding/2020/cc/d0cc01485k#!divAbstract