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Published on: October 9, 2016
Small molecule inhibitors of STAT3 for cancer therapy
1NO.3 People's Hospital affiliated to Shanghai Jiao-Tong University School of Medicine, Shanghai 201900, China.
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.
Insights
Signal transducer and activator of transcription 3 (STAT3) is a key driver in many cancers. This review covers small molecule inhibitors targeting STAT3 for novel cancer therapies.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Aberrant activation of Signal transducer and activator of transcription 3 (STAT3) is implicated in the pathogenesis of numerous human cancers.
- Constitutive STAT3 activity promotes tumor growth, survival, and immune evasion by regulating target genes involved in proliferation, apoptosis, and angiogenesis.
Purpose of the Study:
- To provide a comprehensive review of small molecular inhibitors targeting STAT3 for cancer therapy.
- To discuss the rationale and current landscape of developing STAT3 as a direct molecular target for anticancer strategies.
Main Methods:
- Literature review of experimental research papers on small molecular inhibitors of STAT3.
- Analysis of studies investigating STAT3 as a cancer therapeutic target.
Main Results:
- STAT3 is a validated molecular target in oncology due to its critical role in tumor development.
- Various small molecular weight compounds have been developed to inhibit STAT3 signaling pathways.
- The review consolidates information on existing inhibitory modalities against STAT3.
Conclusions:
- Targeting STAT3 with small molecule inhibitors represents a promising therapeutic strategy for various cancers.
- Further development of STAT3-targeted agents holds potential for novel anticancer drug discovery.
- Disrupting oncogenic STAT3 signaling offers a direct approach to combat cancer progression.
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