Current development of CBP/p300 inhibitors in the last decade

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. (c) 2020 Elsevier Masson SAS. All rights reserved.

Automated summary

CBP/p300, as a potential target for treating diseases including malignant tumors, has attracted interest in the development of small-molecule inhibitors. The review focuses on the development of CBP/p300 inhibitors from 2010 to 2020, highlighting their structure-activity relationships, binding modes, selectivity, and pharmacological functions to facilitate rational design and development of potential inhibitors.