Affiliation:
1. Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Soochow University, Suzhou
215123, P.R. China
Abstract
Background:
STAT3 (signal transducer and activator of transcription 3) is a
member of the STAT family of proteins that function as signal transducers and transcription
factors. Previous research has demonstrated its importance in cell proliferation, differentiation,
apoptosis, and immunological and inflammatory responses. Targeting the
STAT3 protein has recently been hailed as a viable cancer therapeutic method. Even
though none of these inhibitors have yet been exploited in clinical cancer therapy, a
small number have made them into clinical trials, leading researchers to explore more
promising inhibitors.
Methods:
Based on the mechanism of STAT3 activation, several types of STAT3 inhibitors
were described and summarized according to their origins, structures, bioactivity and
mechanism of action. Direct inhibition of STAT3 mainly targeted one of the three distinct
structural regions of the protein, namely the SH2 domain, the DNA binding domain,
and the coiled-coil domain.
Results:
The progress in STAT3 inhibitor discovery from 2010 to 2021 is comprehensively
summarized in this review. STAT3 inhibitors are mainly classified into small
molecule inhibitors, natural product inhibitors, and peptides/peptidomimetics. Moreover,
it also covers relevant analogues, as well as their core framework.
Conclusion:
Small-molecule inhibitors of STAT3 like BP-1-102 and BTP analogues displayed
great potential against various cancers, while natural products, as well as peptide
and peptidomimetics, also showed promising application. Therefore, STAT3 has become
a promising target with great research value, and the development of STAT3 inhibitors
may provide more therapeutic strategies for STAT3-related diseases.
Funder
Natural Science Foundation of Jiangsu Province
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology,Molecular Medicine,Drug Discovery,Biochemistry,Organic Chemistry
Cited by
2 articles.
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