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

Heckmann Dominik | Zendy; Meyer Axel | Zendy; Marinelli Luciana | Zendy; Zahn Grit | Zendy; Stragies Roland | Zendy; Kessler Horst | Zendy

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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.

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