title: Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors.
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.
authors: Massimiliano
authors: M
authors: Tognolini
authors: Dipartimento di Farmacia, Universita di Parma, Viale delle Scienze 27/a, 43124 Parma, Italia. alessio.lodola@unipr.it.
authors: Alessio
authors: A
authors: Lodola
mesh_terms: D000818:Animals; D001565:Benzoates / Q000737:chemistry / Q000494:pharmacology; D002793:Cholic Acids / Q000737:chemistry / Q000494:pharmacology; D017292:Doxazosin / Q000737:chemistry / Q000494:pharmacology; D055808:Drug Discovery / Q000379:methods*; D036342:Ephrins / Q000378:metabolism*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D028321:Plant Preparations / Q000737:chemistry / Q000494:pharmacology*; D011485:Protein Binding; D025941:Protein Interaction Mapping; D060066:Protein Interaction Maps; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D036081:Receptors, Eph Family / Q000819:agonists / Q000037:antagonists & inhibitors*; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D001565:Benzoates; D002793:Cholic Acids; D036342:Ephrins; D028321:Plant Preparations; D047428:Protein Kinase Inhibitors; D054852:Small Molecule Libraries; D036081:Receptors, Eph Family; D017292:Doxazosin