Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 22, Pages 9831-9837Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm3010515
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Funding
- Canadian Institutes for Health Research
- Canada Foundation for Innovation
- Genome Canada
- Pfizer
- GlaxoSmithKline
- Eli Lilly
- Novartis Research Foundation
- Abbott
- Ontario Ministry of Research and Innovation
- Wellcome Trust
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The posttranslational modification of chromatin through acetylation at selected histone lysine residues is governed by histone acetyltransferases (HATs) and histone deacetylases (HDACs). The Significance of this subset of the epigenetic code, is interrogated and interpreted by an acetyllysine-Specific protein-protein interaction with bromodomain reader modules. Selective inhibition of the brome and extra C-terminal domain (BET) family of bromodomains. with a., small molecule is feasible, and this may represent an opportunity for disease intervention through the recently disclosed antiproliferative and anti inflammatory properties of such inhibitors Herein, we describe the discovery and structure activity relationship (SAR) of a novel; small molecule chemical probe for BET family inhibition that was identified through the application of structure based fragment,assessment and optimization techniques This has yielded a potent, selective compound with cell based activity (PFI-1) that may further add to the understanding of BET family function within the bromodomains.
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