Journal
CHEMICAL COMMUNICATIONS
Volume -, Issue -, Pages -Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d2cc03712b
Keywords
PROTAC; HDAC; Degrader; cancer
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Funding
- Jurgen Manchot Foundation, Dusseldorf, Germany
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The development of a new class of selective HDAC6 degraders based on a difluoromethyl-1,3,4-oxadiazole (DFMO) warhead as ZBG is reported, providing a promising approach to treat HDAC6-driven diseases.
The targeted degradation of histone deacetylase 6 (HDAC6) by heterobifunctional degraders constitutes a promising approach to treat HDAC6-driven diseases. Previous HDAC6 selective degraders utilised a hydroxamic acid as a zinc-binding group (ZBG) which features mutagenic and genotoxic potential. Here we report the development of a new class of selective HDAC6 degraders based on a difluoromethyl-1,3,4-oxadiazole (DFMO) warhead as ZBG.
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