Abstract
Stat-3 (Signal Transduction and Activator of Transcription) is a member of the Stat family of latent, cytosolic transcription factors that directly relate signals from the plasma membrane to the nucleus. This protein is constitutively activated by aberrant upstream tyrosine kinase activities in a broad spectrum of human tumors, and it has been identified as a promising target for cancer drug discovery. This review deals with the recent developments of peptides and peptidomimetics or even non-peptidic small molecules, able to bind to the SH2 domain of Stat-3, thus blocking its functions. Moreover, several compounds able to alter the Stat-3 pathway by inhibition of kinases upstream to Stat-3, or even with unknown targets, were reviewed.
Keywords: Antitumor agents, Stat-3, Peptide-based antagonists, Small molecules, Natural compounds
Current Medicinal Chemistry
Title: STAT 3 as a Target for Cancer Drug Discovery
Volume: 15 Issue: 9
Author(s): Luca Costantino and Daniela Barlocco
Affiliation:
Keywords: Antitumor agents, Stat-3, Peptide-based antagonists, Small molecules, Natural compounds
Abstract: Stat-3 (Signal Transduction and Activator of Transcription) is a member of the Stat family of latent, cytosolic transcription factors that directly relate signals from the plasma membrane to the nucleus. This protein is constitutively activated by aberrant upstream tyrosine kinase activities in a broad spectrum of human tumors, and it has been identified as a promising target for cancer drug discovery. This review deals with the recent developments of peptides and peptidomimetics or even non-peptidic small molecules, able to bind to the SH2 domain of Stat-3, thus blocking its functions. Moreover, several compounds able to alter the Stat-3 pathway by inhibition of kinases upstream to Stat-3, or even with unknown targets, were reviewed.
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Cite this article as:
Costantino Luca and Barlocco Daniela, STAT 3 as a Target for Cancer Drug Discovery, Current Medicinal Chemistry 2008; 15 (9) . https://dx.doi.org/10.2174/092986708783955464
DOI https://dx.doi.org/10.2174/092986708783955464 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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