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信号转导和转录激活因子3(STAT3)为细胞内重要的信号转导蛋白,与肿瘤的发生发展密切相关,抑制STAT3的过度的表达为治疗肿瘤的手段之一。分别从肽和拟肽类、天然产物类以及虚拟筛选技术发现的小分子这几个方面对目前已报道的STAT3抑制剂的抗肿瘤活性及其构效关系的研究进展进行综述。
Signal Transducer and Activator of Transcription 3 (STAT3) is an important intracellular signaling protein and is closely related to tumorigenesis and development. Inhibition of STAT3 overexpression is one of the means to treat tumors. The progress on the antitumor activities of STAT3 inhibitors and their structure-activity relationship have been reviewed respectively from peptides and peptidomimetics, natural products and small molecules found by virtual screening technology.