Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 187, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.111922
Keywords
STAT3; Anticancer target; Small molecular inhibitor
Categories
Funding
- National Natural Science Foundation of China [21977128, 81973359]
- Guangdong Natural Science Fund [2018A030313300]
- SYSU startup funding [36000-18831205, 36000-18831113]
- Guangdong Provincial Key Laboratory of Construction Foundation [2017B030314030]
- Jilin Province Science and Technology Development Project [20190304046YY]
- National Major Special Projects for the Creation and Manufacture of New Drugs [2018ZX09301031-001]
- Guangdong Innovative and Entrepreneurial Research Team Program [2016ZT06Y337]
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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. (C) 2019 Elsevier Masson SAS. All rights reserved.
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