BET家族及其抑制剂在肿瘤中的研究进展

Advance of BET family and its inhibitors in tumor

溴结构域和超末端结构域(BET)家族属于溴结构域蛋白家族,在多种肿瘤中BET家族表达上调,其与细胞生长、增殖分化、凋亡坏死等多种生物学过程相关,进而参与调控肿瘤发生发展的过程。BET家族多种抑制剂的Ⅰ期或Ⅱ期临床实验正在进行中,相关研究结果表明,BET抑制剂单药或联合现有药物在治疗多种肿瘤中均有明确的效果,因此,其有望成为肿瘤治疗的新靶点。本文通过复习相关文献对近年来BET家族及其抑制剂在肿瘤研究中的进展进行综述。

Bromodomain and extra terminal domain (BET) family is one of bromodomain proteins, which is up-regulated in various tumors and involved in tumor pathogenesis by regulating cell growth, proliferation and differentiation, apoptosis and necrosis. Several BET inhibitors have been developed and clinically tested, the antitumor efficacy of BET inhibitor alone or in combination with existing drugs has been identified in different tumors types, so it may become a new target for tumor treatment. This paper summarizes the current knowledge of BETs and its inhibitors in tumor.