Abstract：
UNASSIGNED: STAT3 is a critical transcription factor that transmits signals from the cell surface to the nucleus, thus influencing the transcriptional regulation of some oncogenes. The inhibition of the activation of STAT3 is considered a promising strategy for cancer therapy. Numerous STAT3 inhibitors bearing different scaffolds have been reported to date, with a few of them having been considered in clinical trials.
UNASSIGNED: This review summarizes the advances on STAT3 inhibitors with different structural skeletons, focusing on the structure-activity relationships in the related patent literature published from 2014 to date.
UNASSIGNED: Since the X-ray crystal structure of STAT3β homo dimer bound to DNA was solved in 1998, the development of STAT3 inhibitors has gone through a boom in recent years. However, none of them have been approved for marketing, probably due to the complex biological functions of the STAT3 signaling pathway, including its character and the poor drug-like physicochemical properties of its inhibitors. Nonetheless, targeting STAT3 continues to be an exciting field for the development of anti-tumor agents along with the emergence of new STAT3 inhibitors with unique mechanisms of action.
UNASSIGNED: This review summarizes the advances on STAT3 inhibitors with different structural skeletons, focusing on the structure-activity relationships in the related patent literature published from 2014 to date.
UNASSIGNED: Since the X-ray crystal structure of STAT3β homo dimer bound to DNA was solved in 1998, the development of STAT3 inhibitors has gone through a boom in recent years. However, none of them have been approved for marketing, probably due to the complex biological functions of the STAT3 signaling pathway, including its character and the poor drug-like physicochemical properties of its inhibitors. Nonetheless, targeting STAT3 continues to be an exciting field for the development of anti-tumor agents along with the emergence of new STAT3 inhibitors with unique mechanisms of action.
摘要：
未经证实：STAT3是将信号从细胞表面传递到细胞核的关键转录因子，从而影响某些癌基因的转录调控。抑制STAT3的激活被认为是癌症治疗的有希望的策略。迄今为止，已经报道了许多带有不同支架的STAT3抑制剂，其中一些已经在临床试验中考虑过。
UNASSIGNED：这篇综述总结了具有不同结构骨架的STAT3抑制剂的研究进展，重点关注2014年至今发表的相关专利文献中的结构-活动关系。
UNASSIGNED：自1998年解决与DNA结合的STAT3β同源二聚体的X射线晶体结构以来，近年来STAT3抑制剂的开发经历了热潮。然而,它们都没有被批准用于营销，可能是由于STAT3信号通路的复杂生物学功能，包括其特性和其抑制剂的不良药物样理化性质。尽管如此，随着具有独特作用机制的新型STAT3抑制剂的出现，靶向STAT3仍然是抗肿瘤药物开发的一个令人兴奋的领域。
UNASSIGNED：这篇综述总结了具有不同结构骨架的STAT3抑制剂的研究进展，重点关注2014年至今发表的相关专利文献中的结构-活动关系。
UNASSIGNED：自1998年解决与DNA结合的STAT3β同源二聚体的X射线晶体结构以来，近年来STAT3抑制剂的开发经历了热潮。然而,它们都没有被批准用于营销，可能是由于STAT3信号通路的复杂生物学功能，包括其特性和其抑制剂的不良药物样理化性质。尽管如此，随着具有独特作用机制的新型STAT3抑制剂的出现，靶向STAT3仍然是抗肿瘤药物开发的一个令人兴奋的领域。
