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G Protein-coupled Receptor (GPCR) Reconstitution and Labeling for Solution Nuclear Magnetic Resonance (NMR) Studies of the Structural Basis of Transmembrane Signaling
Authors:Haoyi Ge,Huixia Wang,Benxun Pan,Dandan Feng,Canyong Guo,Lingyun Yang,Dongsheng Liu,Kurt Wü  thrich
Affiliation:1.iHuman Institute, ShanghaiTech University, Shanghai 201210, China; (H.G.); (H.W.); (B.P.); (D.F.); (C.G.); (L.Y.); (D.L.);2.School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China;3.Department of Integrative Structural and Computational Biology, Scripps Research, La Jolla, CA 92037, USA;4.Institute of Molecular Biology and Biophysics, ETH Zürich, Otto-Stern-Weg 5, 8093 Zürich, Switzerland
Abstract:G protein-coupled receptors (GPCRs) are a large membrane protein family found in higher organisms, including the human body. GPCRs mediate cellular responses to diverse extracellular stimuli and thus control key physiological functions, which makes them important targets for drug design. Signaling by GPCRs is related to the structure and dynamics of these proteins, which are modulated by extrinsic ligands as well as by intracellular binding partners such as G proteins and arrestins. Here, we review some basics of using nuclear magnetic resonance (NMR) spectroscopy in solution for the characterization of GPCR conformations and intermolecular interactions that relate to transmembrane signaling.
Keywords:G protein-coupled receptors   19F-NMR   membrane mimetics   stable-isotope labeling   in-membrane chemical modification   amino-acid-specific NMR labeling   sequence-specific NMR labeling
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