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Current Medicinal Chemistry

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ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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Review Article

Recent Advances in the Development of CBP/p300 Bromodomain Inhibitors

Author(s): Ying Xiong, Mingming Zhang* and Yingxia Li*

Volume 27, Issue 33, 2020

Page: [5583 - 5598] Pages: 16

DOI: 10.2174/0929867326666190731141055

Price: $65

Abstract

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.

Keywords: CBP/p300, bromodomain, histone acetyltransferases, genes, inhibitors, drug discovery.

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