2. Academic Validation
  3. Development of the first non-hydroxamate selective HDAC6 degraders

Development of the first non-hydroxamate selective HDAC6 degraders

  • Chem Commun (Camb). 2022 Oct 4;58(79):11087-11090. doi: 10.1039/d2cc03712b.
Tim Keuler 1,  Beate König 1,  Nico Bückreiß 1,  Fabian B Kraft 1,  Philipp König 1,  Linda Schäker-Hübner 1,  Christian Steinebach 1,  Gerd Bendas 1,  Michael Gütschow 1,  Finn K Hansen 1
Affiliations

Affiliation

  • 1 Pharmaceutical Institute, University of Bonn, An der Immenburg 4, 53121, Bonn, Germany. gbendas@uni-bonn.de.
PMID: 36098075 DOI: 10.1039/d2cc03712b
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.

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