Drug Design for G-Protein-Coupled Receptors by a Ligand-Based NMR Method

被引：28

作者：

Bartoschek, Stefan ^{[1
]}

Klabunde, Thomas ^{[1
]}

Defossa, Elisabeth ^{[1
]}

Dietrich, Viktoria ^{[1
]}

Stengelin, Siegfried ^{[1
]}

Griesinger, Christian ^{[2
]}

Carlomagno, Teresa ^{[3
]}

Focken, Ingo ^{[1
]}

Wendt, K. Ulrich ^{[1
]}

机构：

[1] Sanofi Aventis Deutschland GmbH, R&D Dept Chem & Analyt Sci Struct Biol TD Metab B, D-65926 Frankfurt, Germany

[2] Max Planck Inst Biophys Chem, Dept NMR Based Struct Biol, D-37033 Gottingen, Germany

[3] EMBL, Struct & Computat Biol Unit, D-69117 Heidelberg, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2010年 / 49卷 / 08期

关键词：

drug design; G-protein-coupled receptors; NMR spectroscopy; structure-activity relationships; TRANSFER DIFFERENCE NMR; INTEGRIN ALPHA(IIB)BETA(3); BINDING; SPECTROSCOPY; CELLS; GPR40;

D O I：

10.1002/anie.200905102

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

(Figure Presented) A nonradioactive binding assay relying on NMR methods has been devised for a G-protein-coupled receptor; in addition the INPHARMA methods give access to the relative orientation of multiple ligands and supports ligand-based drug design (see picture of superimposed ligands). The method is fast and does not require any structural information from protein crystal structures. © 2010 Wiley-VCH Verlag GmbH &. Co. KGaA.

引用

页码：1426 / 1429

页数：4

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