Ying Xiong, Mingming Zhang* and Yingxia Li* Pages 5583 - 5598 ( 16 )
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.
CBP/p300, bromodomain, histone acetyltransferases, genes, inhibitors, drug discovery.
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203