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Updated: Aug 29, 2025

09:20
Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
Published on: August 10, 2017
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Development of the first non-hydroxamate selective HDAC6 degraders
Tim Keuler1, Beate König1, Nico Bückreiß1
1Pharmaceutical Institute, University of Bonn, An der Immenburg 4, 53121, Bonn, Germany. gbendas@uni-bonn.de.
Abstract:
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.

