摘要
信号传导与活化转录因子3(signal transducers and activators of transcription 3,STAT3)是信号传导活化转录因子家族的重要成员,在细胞中起到传递信号和启动基因转录的双重作用。许多研究已经证明,组成型STAT3在多种人类肿瘤中激活。有证据表明,异常STAT3信号通过抑制凋亡,诱导细胞增殖、血管生成、侵袭和转移,诱发炎症和免疫抑制来促进人类癌症的发生和进展。目前针对STAT3为靶点开发出一些特异性小分子抑制剂,然而还没有药物进入临床阶段。鉴定和开发靶向抑制STAT3激活的新型药物仍然是一个重要的科学和临床挑战。本文介绍了STAT3与肿瘤发生之间的关系及新的STAT3抑制剂的研究进展。
Signal transducers and activators of transcription（STAT3） is an important member of the family of signal transducers and activators of transcription, which plays a dual role in signaling and initiating gene transcription in cells. Numerous studies have demonstrated constitutive activation of STAT3 in a wide variety of human tumors. There is strong evidence to suggest that aberrant STAT3 signaling promotes initiation and progression of human cancers by either inhibition of apoptosis or induction of cell proliferation, angiogenesis, invasion, metastasis, inflammation and immunosuppression. At present, some specific small molecule inhibitors have been developed to target STAT3. However, no drugs have been used in the clinical stage. The identification and development of novel drugs that can target deregulated STAT3 activation effectively remains an important scientific and clinical challenge. This article provides a summary on progress about STAT3 in tumor genesis and new inhibitors of STAT3.
作者
陈越
季鸣
陈晓光
CHEN Yue JI Ming CHEN Xiao-guang(State Key Laboratory of B ioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China)
出处
《药学学报》
CAS
CSCD
北大核心
2017年第9期1351-1358,共8页
Acta Pharmaceutica Sinica
基金
基金项目:中国医学科学院医学与健康科技创新工程(2016-12M-3-008)
