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.

CBP / p300充当组蛋白乙酰转移酶和转录辅助因子，代表了包括恶性肿瘤在内的各种疾病的诱人靶标。针对CBP / p300的溴结构域和HAT结构域的小分子抑制剂的开发引起了药物化学家的广泛兴趣，期望为抗癌治疗提供新的希望。特别是，目前正在对通过CellCentric鉴定的CBP / p300溴结构域抑制剂CCS1477进行临床评估，以治疗血液系统恶性肿瘤和前列腺癌。在这篇综述中，我们描述了从2010年到2020年报道的CBP / p300抑制剂的发展，特别强调了它们的结构-活性关系（SAR），结合方式，