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

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Abstract

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.

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

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Article information


Submitted
25 Feb 2020
Accepted
11 Mar 2020
First published
11 Mar 2020

Chem. Commun., 2020, Advance Article
Article type
Communication

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

J. P. Smalley, G. E. Adams, C. J. Millard, Y. Song, J. K. S. Norris, J. W. R. Schwabe, S. M. Cowley and J. T. Hodgkinson, Chem. Commun., 2020, Advance Article , DOI: 10.1039/D0CC01485K

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