2. Academic Validation
  3. Current development of CBP/p300 inhibitors in the last decade

Current development of CBP/p300 inhibitors in the last decade

  • Eur J Med Chem. 2021 Jan 1:209:112861. doi: 10.1016/j.ejmech.2020.112861.
Zhang-Xu He 1,  Bing-Fei Wei 1,  Xin Zhang 1,  Yun-Peng Gong 1,  Li-Ying Ma 2,  Wen Zhao 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Esophageal Cancer Prevention and Treatment, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, China.
  • 2 State Key Laboratory of Esophageal Cancer Prevention and Treatment, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, China. Electronic address: maliying@zzu.edu.cn.
  • 3 State Key Laboratory of Esophageal Cancer Prevention and Treatment, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, China. Electronic address: zhaowen100@139.com.
PMID: 33045661 DOI: 10.1016/j.ejmech.2020.112861
Abstract

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.

Keywords

Bromodomain; CBP/p300; HAT; Inhibitors.

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