2. Academic Validation
  3. Revisiting signal transducer and activator of transcription 3 (STAT3) as an anticancer target and its inhibitor discovery: Where are we and where should we go?

Revisiting signal transducer and activator of transcription 3 (STAT3) as an anticancer target and its inhibitor discovery: Where are we and where should we go?

  • Eur J Med Chem. 2020 Feb 1:187:111922. doi: 10.1016/j.ejmech.2019.111922.
Qiuyao Huang 1,  Yan Zhong 2,  Hui Dong 1,  Qiyao Zheng 2,  Shuo Shi 2,  Kai Zhu 3,  Xinming Qu 3,  Wenhao Hu 1,  Xiaolei Zhang 4,  Yuanxiang Wang 5
Affiliations

Affiliations

  • 1 Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
  • 2 Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
  • 3 Innovation Practice Center, Changchun University of Chinese Medicine, Changchun, 130117, China.
  • 4 Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China. Electronic address: zhangxlei5@mail.sysu.edu.cn.
  • 5 Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China. Electronic address: wangyx95@mail.sysu.edu.cn.
PMID: 31810784 DOI: 10.1016/j.ejmech.2019.111922
Abstract

As a transcription factor, STAT3 protein transduces extracellular signals to the nucleus and then activates transcription of target genes. STAT3 has been well validated as an attractive Anticancer target due to its important roles in Cancer initiation and progression. Identification of specific and potent STAT3 inhibitors has attracted much attention, while there has been no STAT3 targeted drug approved for clinical application. In this review, we will briefly introduce STAT3 protein and review its role in multiple aspects of Cancer, and systematically summarize the recent advances in discovery of STAT3 inhibitors, especially the ones discovered in the past five years. In the last part of the review, we will discuss the possible new strategies to overcome the difficulties of developing potent and specific STAT3 inhibitors and hope to shed light on future drug design and inhibitor optimization.

Keywords

Anticancer target; STAT3; Small molecular inhibitor.

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