Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors

Author(s): Massimiliano Tognolini, Alessio Lodola

Journal Name: Current Drug Targets

Volume 16 , Issue 10 , 2015

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Graphical 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.

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Article Details

Year: 2015
Page: [1048 - 1056]
Pages: 9
DOI: 10.2174/1389450116666150825144457
Price: $65

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