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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