GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

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作者
Ichio Shimada
Takumi Ueda
Yutaka Kofuku
Matthew T. Eddy
Kurt Wüthrich
机构
[1] Graduate School of Pharmaceutical Sciences,Department of Integrative Structural and Computational Biology
[2] The University of Tokyo,Departments of Biological Sciences and Chemistry
[3] Hongo,undefined
[4] Skaggs Institute of Chemical Biology,undefined
[5] The Scripps Research Institute,undefined
[6] Bridge Institute,undefined
[7] USC Michelson Center,undefined
[8] University of Southern California,undefined
[9] Skaggs Institute of Chemical Biology,undefined
[10] The Scripps Research Institute,undefined
[11] Present address: Department of Chemistry,undefined
[12] University of Florida,undefined
[13] Gainesville,undefined
[14] FL,undefined
[15] USA.,undefined
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摘要
Determination of the crystal structures of more than 50 human G protein-coupled receptors (GPCRs) during the past decade has provided a platform for structure-based drug design for this key target class, which is being augmented with cryo-electron microscopy (cryo-EM) structures and nuclear magnetic resonance (NMR) spectroscopy studies of dynamic features. This Review describes the application of NMR techniques to GPCRs and projects where crystal and/or cryo-EM structures have been complemented with NMR studies and discusses the impact of this integrative approach on GPCR biology and drug discovery.
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页码:59 / 82
页数:23
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