Current development of CBP/p300 inhibitors in the last decade.

Zhang-Xu He, Bing-Fei Wei, Xin Zhang, Yun-Peng Gong, Li-Ying Ma, Wen Zhao

European journal of medicinal chemistry 2021 Jan 01

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CBP/p300, functioning as histone acetyltransferases and transcriptional co-factors, represents an attractive target for various diseases, including malignant tumor. The development of small-molecule inhibitors targeting the bromodomain and HAT domains of CBP/p300 has aroused broad interests of medicinal chemist in expectation of providing new hope for anti-cancer treatment. In particular, the CBP/p300 bromodomain inhibitor CCS1477, identified by CellCentric, is currently undergone clinical evaluation for the treatment of haematological malignancies and prostate cancer. In this review, we depict the development of CBP/p300 inhibitors reported from 2010 to 2020 and particularly highlight their structure-activity relationships (SARs), binding modes, selectivity and pharmacological functions with the aim to facilitate rational design and development of CBP/p300 inhibitors. Copyright © 2020 Elsevier Masson SAS. All rights reserved.

Citation

Zhang-Xu He, Bing-Fei Wei, Xin Zhang, Yun-Peng Gong, Li-Ying Ma, Wen Zhao. Current development of CBP/p300 inhibitors in the last decade. European journal of medicinal chemistry. 2021 Jan 01;209:112861