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.
SUBMITTER: Smalley JP
PROVIDER: S-EPMC7610821 | biostudies-literature |
REPOSITORIES: biostudies-literature
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