Abstract
Aberrant activation of the signal transducer and activator of transcription (STAT) 3 occurs in many human tumors. Constitutive STAT3 activity induces specific target genes that stimulate cell proliferation, prevent apoptosis, promote angiogenesis and facilitate tumor immune evasion. Thus, STAT3 is an attractive molecular target for the development of novel cancer therapeutics. Targeting and disruption of oncogenic STAT3 signaling may theoretically be accomplished through various approaches, involving direct and indirect strategies. Small molecular weight compounds have been used for this purpose. This review is intended to be full coverage of the small molecular inhibitors to develop direct STAT3 as a target for cancer therapy and will provide a discussion on the inhibitory modalities developed to date. At present, we retrieved related small molecular inhibitors experimental research papers about STAT3 as a cancer therapy target, the rationale to pursue the protein for the discovery and development of novel anticancer strategies and agents.
Keywords: Antitumor therapeutics, molecular targeted therapy, small molecule inhibitors, signal transducer, activator of transcription 3, signal transducer and activator of transcription 3, STAT3 activity
Current Medicinal Chemistry
Title: Small Molecule Inhibitors of STAT3 for Cancer Therapy
Volume: 18 Issue: 26
Author(s): M. Zhao, B. Jiang and F.-H. Gao
Affiliation:
Keywords: Antitumor therapeutics, molecular targeted therapy, small molecule inhibitors, signal transducer, activator of transcription 3, signal transducer and activator of transcription 3, STAT3 activity
Abstract: Aberrant activation of the signal transducer and activator of transcription (STAT) 3 occurs in many human tumors. Constitutive STAT3 activity induces specific target genes that stimulate cell proliferation, prevent apoptosis, promote angiogenesis and facilitate tumor immune evasion. Thus, STAT3 is an attractive molecular target for the development of novel cancer therapeutics. Targeting and disruption of oncogenic STAT3 signaling may theoretically be accomplished through various approaches, involving direct and indirect strategies. Small molecular weight compounds have been used for this purpose. This review is intended to be full coverage of the small molecular inhibitors to develop direct STAT3 as a target for cancer therapy and will provide a discussion on the inhibitory modalities developed to date. At present, we retrieved related small molecular inhibitors experimental research papers about STAT3 as a cancer therapy target, the rationale to pursue the protein for the discovery and development of novel anticancer strategies and agents.
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Cite this article as:
Zhao M., Jiang B. and Gao F.-H., Small Molecule Inhibitors of STAT3 for Cancer Therapy, Current Medicinal Chemistry 2011; 18 (26) . https://dx.doi.org/10.2174/092986711796957284
DOI https://dx.doi.org/10.2174/092986711796957284 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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