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Recent Advances in the Development of CBP/p300 Bromodomain Inhibitors

Author(s):

Ying Xiong, Mingming Zhang* and Yingxia Li*   Pages 1 - 15 ( 15 )

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 and 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, Inhibitors, Drug discovery

Affiliation:

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203



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