Journal
CURRENT MEDICINAL CHEMISTRY
Volume 27, Issue 33, Pages 5583-5598Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867326666190731141055
Keywords
CBP/p300; bromodomain; histone acetyltransferases; genes; inhibitors; drug discovery
Funding
- National Natural Science Foundation of China [81773576]
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CBP and p300 are two closely related Histone Acetyltransferases (HATs) that interact with numerous transcription factors and act to increase the expression of their target genes. Both proteins contain a bromodomain flanking the HAT catalytic domain that is important in binding of CBP/p300 to chromatin, which offers an opportunity to develop protein-protein interaction inhibitors. Since their discovery in 2006, CBP/p300 bromodomains have attracted much interest as promising new epigenetic targets for diverse human diseases, including inflammation, cancer, autoimmune disorders, and cardiovascular disease. Herein, we present a comprehensive review of the structure, function, and inhibitors of CBP/p300 bromodomains developed in the last several years, which is expected to be beneficial to relevant studies.
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