BRD4抑制剂抗肿瘤机制研究进展

摘要

BRD4蛋白是溴结构域和超末端家族蛋白(BET)家族中最重要的功能蛋白,含两个溴结构域及一个超末端结构域.BRD4的表达上调与肺癌、乳腺癌、急性髓系淋巴瘤、肝癌等多种肿瘤的发生发展密切相关.针对BRD4已开发出多种抑制剂,且其单药或联合其它肿瘤抑制剂应用均显现出良好的抗肿瘤作用.BRD4抑制剂在不同的肿瘤中作用机制不同,本文主要就BRD4抑制剂在不同类型肿瘤中的抗肿瘤机制研究现状进行综述.%Bromodomain-containing protein 4 (BRD4) is the most important member of the bromodomain and extra-terminal (BET) family proteins. It is comprised of two conserved N-terminal bromodomains and an extraterminal domain. Many recent studies have shown the expression of BRD4 is associated with genesis and development of many kinds of cancers, such as lung cancer, breast cancer, acute myelogenous leukemia (AML) and hepatoma carcinoma. At present, small molecular compound targeting BRD4 have been developed and shown significantly antitumor efficacy. Different anti-tumor mechanisms of BRD4 inhibitors have also been found in different tumors. This review summarized the recent researches on the mechanism of BRD4 inhibitors on different types of cancers.