JAK/STAT3信号通路及其抑制剂在肿瘤治疗领域的研究进展

JAK/STAT3 Signaling Pathway and Its Inhibitors in Tumor Therapy

信号转导及转录激活因子3(signal transducers and activators of transcription 3,STAT3)是一种细胞内重要的转录因子,在体内可被其最常见的上游激酶JAK激酶(Janus kinase)磷酸化激活。众所周知,异常激活的STAT3促进肿瘤的发生发展,因此研究人员一直致力于研究一类靶向JAK/STAT3信号通路的抗肿瘤药物。笔者收集了近年来文献中报道的靶向JAK/STAT3信号通路的抑制剂研究及临床试验进展,对于部分抑制剂已经报道的靶点、作用机制和药效活性进行总结。

Signal transducers and activators of transcription 3 generally located in cytoplasm is a key intra-cellular transcription.So far,STAT3 has been known that could be activated by several different upstream kinase within cell,the most common one of which is Janus kinase.The aberrant activation of STAT3 induces tumorigenesis and promotes tumor development.Consequently,researchers have always been committed to developing novel anti-tumor drugs targeting JAK/STAT3 pathway signaling.In this review,researches as well as clinical trials of JAK/STAT3 inhibitors published over the past several years are collected and the targets,mechanism and pharmacological properties of certain inhibitors are summarized.