Journal
CHEMICAL COMMUNICATIONS
Volume 56, Issue 32, Pages 4476-4479Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0cc01485k
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Funding
- EPSRC [EP/S030492/1]
- MRC [MR/J009202/1]
- BBSRC [BB/N002954/1, BB/P021689/1]
- Wellcome Trust Senior Investigator Award [100237/Z/12/Z]
- Royal Society Wolfson Research Merit Award
- Wellcome Trust [100237/Z/12/Z] Funding Source: Wellcome Trust
- BBSRC [BB/P021689/1, BB/N002954/1] Funding Source: UKRI
- EPSRC [EP/S030492/1] Funding Source: UKRI
- MRC [MC_PC_18054] Funding Source: UKRI
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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.
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