EP300作为癌症潜在治疗靶标的研究进展

Research Progress of EP300 as a Potential Therapeutic Target for Cancer

癌症的发生发展是一个长期的、多种因素参与的过程。EP300是组蛋白乙酰转移酶,越来越多的研究表明,EP300的表达和突变与癌症的发生发展密切相关,它能通过乙酰化组蛋白、非组蛋白,或者作为转录辅助因子,将转录因子募集到目标基因的启动子区域促基因转录,来发挥其对癌症的双重作用。本文就EP300对癌症发生发展影响机制的研究进展进行综述。

The occurrence and development of cancer is a long-term process involving many factors. EP300 is a histone acetyltransferase. More and more studies have shown that the expression and mutation of EP300 are closely related to the occurrence and development of tumors. It can play its dual role in tumor by acetylation of histones, non-histones, or as a transcription co-factor, recruiting transcrip-tion factors to the promoter region of the target gene to promote gene transcription. The develop-ment of EP300 highly selective small molecule inhibitors is also a hot spot in drug research and de-velopment. In this paper, the mechanism of EP300 on tumor development and its inhibitors were reviewed.