STAT3抗肿瘤抑制剂的研究进展

Advances on anti-neoplastic STAT3 inhibitors

信号转导与转录激活因子3 (Signal transducer and activator of transcription 3, STAT3)是一种在细胞中参与大量细胞因子及生长因子应答的信号转导蛋白,负责调控细胞的生长、增殖、分化以及凋亡等一系列重要的生理过程。研究发现,STAT3的持续性活化与肿瘤的发生发展密切相关。抑制STAT3信号通路的异常活化已成为抗肿瘤药物研发的热门靶点之一。本文从作用于STAT3蛋白的N末端结构域、DNA结合域、SH2结构域以及C末端转录活化结构域的角度,总结了近年来STAT3抗肿瘤抑制剂的研究进展。

Signal transducer and activator of transcription 3（STAT3） is a kind of signal transduction protein involved in cell proliferation, differentiation, apoptosis and other important physiological processes in response to a large number of cytokines and growth factors in cells. It has been shown that constitutive activation of STAT3 is closely associated with oncogenesis and tumorigenesis. Inhibition of aberrant STAT3 signaling has been one of promising strategies for the development of anti-neoplastic therapeutics. The review summarizes the latest progress of STAT3 inhibitors in recent years from the perspective of targeting N-terminal domain, DNA binding domain, SH2 domain and C-terminal transactivation domain of STAT3.