An integrated fragment based screening approach for the discovery of small molecule modulators of the VWF-GPIbα interaction

被引：7

作者：

Jose, Rani A. ^{[1
]}

Voet, Arnout ^{[2
,3
]}

Broos, Katleen ^{[4
]}

Jakobi, Arjen J. ^{[5
]}

Bruylants, Gilles ^{[6
]}

Egle, Brecht ^{[1
]}

Zhang, Kam Y. J. ^{[3
]}

De Maeyer, Marc ^{[2
]}

Deckmyn, Hans ^{[4
]}

De Borggraeve, Wim M. ^{[1
]}

机构：

[1] Katholieke Univ Leuven, Dept Chem, B-3001 Heverlee, Belgium

[2] Katholieke Univ Leuven, Div Biochem Mol & Struct Biol, Dept Chem, Lab Biomol Modelling, B-3001 Heverlee, Belgium

[3] RIKEN, Adv Sci Inst, Zhang Initiat Res Unit, Wako, Saitama 3510198, Japan

[4] KU Leuven Campus Kortrijk, Lab Thrombosis Res, B-8500 Kortrijk, Belgium

[5] Univ Utrecht, Dept Chem, Bijvoet Ctr Biomol Res, NL-3584 CH Utrecht, Netherlands

[6] Univ Libre Bruxelles, B-1050 Brussels, Belgium

来源：

CHEMICAL COMMUNICATIONS | 2012年 / 48卷 / 92期

关键词：

VON-WILLEBRAND-FACTOR; PROTEIN-PROTEIN INTERACTIONS; TRANSFER DIFFERENCE NMR; LESSONS; LIGAND; DOMAIN;

D O I：

10.1039/c2cc35269a

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

An integrated approach comprising STD NMR screening, pharmacophore based analogue selection and a bioassay is presented for the discovery of a stabilizer of the clinically relevant VWF-GPIb alpha protein-protein interaction.

引用

页码：11349 / 11351

页数：3

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