Probing integrin selectivity:: Rational design of highly active and selective ligands for the α5β1 and αvβ3 integrin receptor

被引：81
作者：
Heckmann, Dominik
Meyer, Axel
Marinelli, Luciana
Zahn, Grit
Stragies, Roland
Kessler, Horst
机构：
[1] Tech Univ Munich, Dept Chem, D-85747 Garching, Germany
[2] Univ Naples Federico II, Dipartimento Chim Farmaceut & Tossicol, I-80131 Naples, Italy
[3] Jerini AG, D-10115 Berlin, Germany
来源：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2007年 / 46卷 / 19期
关键词：
antitumor agents; drug design; integrin ligands; receptors; structure-activity relationships;
D O I：
10.1002/anie.200700008
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
(Chemical Equation Presented) 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. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码：3571 / 3574
页数：4
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