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A Potent Integrin Antagonist from a Small Library of Cyclic RGD Pentapeptide Mimics Including Benzyl‐Substituted Azabicycloalkane Amino Acids
Author(s) -
Arosio Daniela,
Belvisi Laura,
Colombo Lino,
Colombo Matteo,
Invernizzi Donatella,
Manzoni Leonardo,
Potenza Donatella,
Serra Massimo,
Castorina Massimo,
Pisano Claudio,
Scolastico Carlo
Publication year - 2008
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200800143
Subject(s) - pentapeptide repeat , integrin , in vitro , chemistry , cyclic peptide , amino acid , antagonist , combinatorial chemistry , stereochemistry , lead compound , biochemistry , peptide , receptor
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 α v β 3 and the α v β 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.