HDAC6型
化学
异羟肟酸
组蛋白脱乙酰基酶
组合化学
生物化学
组蛋白
立体化学
DNA
作者
Tim Keuler,Beate König,Nico Bückreiß,Fabian B. Kraft,Philipp König,Linda Schäker‐Hübner,Christian Steinebach,Gerd Bendas,Michael Gütschow,Finn K. Hansen
摘要
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 warhead as ZBG.
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