PROTAC-Mediated Degradation of Class I Histone Deacetylase Enzymes in Corepressor Complexes

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 via...

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Bibliographic Details
Published in:Chem Commun (Camb)
Main Authors: Smalley, Joshua P., Adams, Grace E., Millard, Christopher J., Song, Yun, Norris, James K.S., Schwabe, John W.R., Cowley, Shaun M., Hodgkinson, James T.
Format: Artigo
Language:Inglês
Published: 2020
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Article
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC7610821/
https://ncbi.nlm.nih.gov/pubmed/32201871
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/d0cc01485k
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