1.
Chem Commun (Camb)
; 56(32): 4476-4479, 2020 Apr 21.
Artigo
em Inglês
| MEDLINE
| ID: mdl-32201871
RESUMO
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.