期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 56, 期 24, 页码 10183-10187出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm401582c
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资金
- UK Biotechnology and Biological Sciences Research Council (BBSRC) [BB/J001201/1, BB/G023123/1]
- BBSRC
- Canadian Institutes for Health Research
- Canada Foundation for Innovation
- Genome Canada
- GlaxoSmithKline
- Pfizer
- Eli Lilly
- Novartis Research Foundation
- Takeda
- Ontario Ministry of Research and Innovation
- Wellcome Trust
- Biotechnology and Biological Sciences Research Council [BB/G023123/1, 980607, BB/J001201/1] Funding Source: researchfish
- BBSRC [BB/G023123/1, BB/J001201/1] Funding Source: UKRI
Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower pockets. We describe successful targeting of the challenging BAZ2B bromodomain using biophysical fragment screening and structure-based optimization of high ligand-efficiency fragments into a novel series of low-micromolar inhibitors. Our results provide attractive leads for development of BAZ2B chemical probes and indicate the whole family may be tractable.
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