信号转导与转录激活因子3:非多肽类小分子抑制剂

Signal transducers and activators of transcription 3: a small molecule nonpeptide inhibitor

信号转导与转录激活因子(STAT)蛋白家族共有7位成员(STAT1、STAT2、STAT3、STAT4、STAT5a、STAT5b和STAT6),它们在细胞中发挥着信号转导和转录因子的双重作用。其中,STAT3在肿瘤的发生、发展和转移,炎症反应,缺血再灌注损伤等多种病理生理过程中发挥着重要的作用,尤其是STAT3的持续异常激活与肿瘤的生长与转移密切相关。抑制STAT3的过度激活是治疗肿瘤的重要方法之一。目前,靶向STAT3的抑制剂主要分成2类:多肽类和拟肽类,非多肽类小分子抑制剂。大部分用于肿瘤防治的STAT3抑制剂都是非多肽类小分子抑制剂。文章针对目前已报道的STAT3非多肽类小分子抑制剂的研究进展进行综述。

Signal transducers and activators of transcription（ STAT） are proteins that play important roles in both signal transduction and transcription. The STAT family has seven members, i. e. STAT1, STAT2, STAT3, STAT4,STAT5 a, STAT5 b, and STAT6. Among them, STAT3 plays important roles in various pathophysiological processes such as incidence, development and metastasis of cancers, inflammation responses, and ischemia / reperfusion injury. In particular, constant abnormal activation of STAT3 is closely relevant to tumor growth and metastasis. So the inhibition of over activation of STAT3 is an important method for cancer treatment. At present, STAT3-targeted inhibitors can generally be classified into two categories, i. e. peptide and peptidomimetics, and small molecular nonpeptide inhibitors. Most STAT3 inhibitors for cancer prevention are small molecular nonpeptide inhibitors. This paper reviews reported research progresses of STAT3 small molecule nonpeptide inhibitors.