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Probing Integrin Selectivity: Rational Design of Highly Active and Selective Ligands for the α5β1 and αvβ3 Integrin Receptor
Author(s) -
Heckmann Dominik,
Meyer Axel,
Marinelli Luciana,
Zahn Grit,
Stragies Roland,
Kessler Horst
Publication year - 2007
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200700008
Subject(s) - selectivity , rational design , integrin , ligand (biochemistry) , receptor , chemistry , computational biology , homology modeling , microbiology and biotechnology , computer science , stereochemistry , biochemistry , biology , genetics , enzyme , catalysis
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.