Abstract
Eph-ephrin system is emerging as a new potential target in several diseases including cancer, diabetes, neurodegenerative diseases and inflammation. In the last decade, several efforts have been made to develop small molecule antagonists of Eph receptors. Both natural and synthetic compounds were discovered with (poly) phenol and steroidal derivatives on one side and the α1 agonist doxazosin, 2,5-dimethylpyrrol- 1-yl-benzoic acids and amino acid conjugates of lithocholic acid on the other. In the present paper we critically present available data for these compounds and discuss their potential usefulness as pharmacological tools or as candidates for a lead-optimization program.
Keywords: Eph, ephrin, drug discovery, small molecules, protein-protein, antagonist.
Current Drug Targets
Title:Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors
Volume: 16 Issue: 10
Author(s): Massimiliano Tognolini and Alessio Lodola
Affiliation:
Keywords: Eph, ephrin, drug discovery, small molecules, protein-protein, antagonist.
Abstract: Eph-ephrin system is emerging as a new potential target in several diseases including cancer, diabetes, neurodegenerative diseases and inflammation. In the last decade, several efforts have been made to develop small molecule antagonists of Eph receptors. Both natural and synthetic compounds were discovered with (poly) phenol and steroidal derivatives on one side and the α1 agonist doxazosin, 2,5-dimethylpyrrol- 1-yl-benzoic acids and amino acid conjugates of lithocholic acid on the other. In the present paper we critically present available data for these compounds and discuss their potential usefulness as pharmacological tools or as candidates for a lead-optimization program.
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Cite this article as:
Tognolini Massimiliano and Lodola Alessio, Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors, Current Drug Targets 2015; 16 (10) . https://dx.doi.org/10.2174/1389450116666150825144457
DOI https://dx.doi.org/10.2174/1389450116666150825144457 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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