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Allosteric inhibitors of the STAT3 signaling pathway.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-02-07 , DOI: 10.1016/j.ejmech.2020.112122 Junhong Qin 1 , Xiaofei Shen 1 , Jian Zhang 2 , Da Jia 1
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-02-07 , DOI: 10.1016/j.ejmech.2020.112122 Junhong Qin 1 , Xiaofei Shen 1 , Jian Zhang 2 , Da Jia 1
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Over-expression and/or hyperactivation of signal transducer and activator of transcription 3 (STAT3) signaling are found in various human diseases, including cancer, autoimmune disorders, and inflammatory diseases. Therefore, STAT3 represents a highly promising therapeutic target for the treatment of these diseases. However, the traditional orthosteric inhibitors of STAT3 exhibit limited clinical efficacy, with low selectivity, numerous side effects, and emerging acquired resistance. Allosteric inhibitors targeting STAT3 or its upstream molecules have emerged as a promising approach to overcome these barriers. In this review, we summarize the recent advances in the development of these inhibitors as well as their applications.
中文翻译：
STAT3信号通路的变构抑制剂。
在多种人类疾病中发现了信号转导子和转录激活因子3（STAT3）信号的过度表达和/或过度激活，包括癌症，自身免疫性疾病和炎症性疾病。因此，STAT3代表了用于治疗这些疾病的高度有前途的治疗靶标。然而，传统的STAT3正构抑制剂显示出有限的临床疗效，选择性低，副作用多且出现新获得的耐药性。靶向STAT3或其上游分子的变构抑制剂已成为克服这些障碍的一种有前途的方法。在这篇综述中，我们总结了这些抑制剂及其应用的最新进展。
更新日期：2020-02-07
中文翻译：
STAT3信号通路的变构抑制剂。
在多种人类疾病中发现了信号转导子和转录激活因子3（STAT3）信号的过度表达和/或过度激活，包括癌症，自身免疫性疾病和炎症性疾病。因此，STAT3代表了用于治疗这些疾病的高度有前途的治疗靶标。然而，传统的STAT3正构抑制剂显示出有限的临床疗效，选择性低，副作用多且出现新获得的耐药性。靶向STAT3或其上游分子的变构抑制剂已成为克服这些障碍的一种有前途的方法。在这篇综述中，我们总结了这些抑制剂及其应用的最新进展。
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