Development of the first non-hydroxamate selective HDAC6 degraders

Autor:	Tim Keuler, Beate König, Nico Bückreiß, Fabian B. Kraft, Philipp König, Linda Schäker-Hübner, Christian Steinebach, Gerd Bendas, Michael Gütschow, Finn K. Hansen
Rok vydání:	2022
Předmět:	Histone Deacetylase Inhibitors Oxadiazoles Zinc Materials Chemistry Metals and Alloys Ceramics and Composites General Chemistry Histone Deacetylase 6 Hydroxamic Acids Catalysis Surfaces Coatings and Films Electronic Optical and Magnetic Materials
Zdroj:	Chemical Communications. 58:11087-11090
ISSN:	1364-548X 1359-7345
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5b75b15bd78c147a2b9c09ce7c7113e https://doi.org/10.1039/d2cc03712b Zobrazit plný text záznamu