Probing Integrin Selectivity: Rational Design of Highly Active and Selective Ligands for the α5β1 and αvβ3 Integrin Receptor

Try and fit in: A strategy for the rational design of α5β1 ligands for the purpose of lead generation and biochemical studies on integrin selectivity is based α5β1 homology modeling. Ligand 1 can bind α5β1 with activities in the subnanomolar range and high selectivity. Minor changes can result in a ligand with a high selectivity for the related αvβ3 receptor.