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

被引:6
|
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
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
收藏
页码:11349 / 11351
页数:3
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