title: A potent integrin antagonist from a small library of cyclic RGD pentapeptide mimics including benzyl-substituted azabicycloalkane amino acids.
abstract: A small library of cyclic RGD pentapeptide mimics, including benzyl-substituted azabicycloalkane amino acids, was synthesized with the aim of developing active and selective integrin antagonists. In vitro binding assays established one particular compound with affinity for both the alpha(v)beta(3) and the alpha(v)beta(5) integrins. The synthesis in solution and the in vitro screening of these RGD derivatives, as well as the determination of the conformational properties of the integrin ligands by spectroscopic and computational methods are described.
authors.affiliation: Istituto di Scienze e Tecnologie Molecolari, Consiglio Nazionale delle Ricerche, Via Fantoli 16/15, 20138 Milano, Italy.
authors.forename: Daniela
authors.initials: D
authors.lastname: Arosio
authors.forename: Laura
authors.initials: L
authors.lastname: Belvisi
authors.forename: Lino
authors.initials: L
authors.lastname: Colombo
authors.forename: Matteo
authors.initials: M
authors.lastname: Colombo
authors.forename: Donatella
authors.initials: D
authors.lastname: Invernizzi
authors.forename: Leonardo
authors.initials: L
authors.lastname: Manzoni
authors.forename: Donatella
authors.initials: D
authors.lastname: Potenza
authors.forename: Massimo
authors.initials: M
authors.lastname: Serra
authors.forename: Massimo
authors.initials: M
authors.lastname: Castorina
authors.forename: Claudio
authors.initials: C
authors.lastname: Pisano
authors.forename: Carlo
authors.initials: C
authors.lastname: Scolastico
mesh_terms: D053961:Azabicyclo Compounds / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D001665:Binding Sites; D002448:Cell Adhesion / Q000187:drug effects; D002478:Cells, Cultured; D042783:Endothelial Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D016023:Integrins / Q000037:antagonists & inhibitors* / Q000187:drug effects / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000378:metabolism; D054852:Small Molecule Libraries
chemical_list: D053961:Azabicyclo Compounds; D016023:Integrins; D010456:Peptides, Cyclic; D054852:Small Molecule Libraries; C507169:cyclic arginine-glycine-aspartic acid peptide