High-resolution crystal structure of an engineered human β2-adrenergic G protein-coupled receptor

Science

Volumn 318, Issue 5854, 2007, Pages 1258-1265

  Cherezov, Vadim ^a   Rosenbaum, Daniel M ^b   Hanson, Michael A ^a   Rasmussen, Søren G F ^b   Foon, Sun Thian ^b   Kobilka, Tong Sun ^b   Choi, Hee Jung ^b   Kuhn, Peter ^a   Weis, William I ^b   Kobilka, Brian K ^b   Stevens, Raymond C ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

^b STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA 2 ADRENERGIC RECEPTOR; CARAZOLOL; CHOLESTEROL; DISULFIDE; G PROTEIN COUPLED RECEPTOR; LYSOZYME; RHODOPSIN;

CRYSTAL STRUCTURE; LIGAND; MEMBRANE; PROTEIN; RESOLUTION;

ARTICLE; BINDING SITE; CRYSTAL STRUCTURE; CRYSTALLIZATION; DIMERIZATION; DNA MODIFICATION; ELECTRICITY; HUMAN; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN ENGINEERING; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN PURIFICATION; PROTEIN STRUCTURE; TISSUE DISTRIBUTION;

BACTERIOPHAGE T4; BINDING SITES; CELL MEMBRANE; CHOLESTEROL; CRYSTALLIZATION; CRYSTALLOGRAPHY, X-RAY; DRUG INVERSE AGONISM; ELECTROSTATICS; HUMANS; LIGANDS; MODELS, MOLECULAR; MURAMIDASE; PROPANOLAMINES; PROTEIN CONFORMATION; PROTEIN FOLDING; PROTEIN STRUCTURE, SECONDARY; RECEPTORS, ADRENERGIC, BETA-2; RECOMBINANT FUSION PROTEINS; RHODOPSIN;

EUKARYOTA;

EID: 36448995359     PISSN: 00368075     EISSN: 10959203     Source Type: Journal    
DOI: 10.1126/science.1150577     Document Type: Article

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76. 2AR-T4L crystallization, 2.4 Å data collection, structure solution, refinement, structure analysis, and manuscript preparation. Supported by NIH Roadmap Initiative grant P50 GM073197 and Protein Structure Initiative grants U54 GM074961 and P50 GM062411 (R.C.S.), NIH Roadmap Initiative grant R21 GM075811 and National Institute of Neurological Disorders and Stroke grant NS028471 (B.K.K.), NIH grant F32 GM082028 (D.M.R.), the Lundbeck Foundation (S.G.F.R.), and NIH grant R01 GM056169 (H.-J.C. and W.I.W.). The GM/CA-CAT beamline (23-ID) at the Advanced Photon Source is supported by National Cancer Institute grant Y1-CO-1020 and National Institute of General Medical Sciences grant Y1-GM-1104. We thank J. Smith, R. Fischetti, and N. Sanishvili at the GM/CA-CAT beamline for assistance in development and use of the minibeam and beam time; G. Schertler for help with the initial diffraction experiments on LCP crystals, performed at ID-13 at the European Synchrotron Radiation Facility; K. Wüthrich and R. Horst for initial NMR analysis of samples; C. Roth, V.-P. Jaakola, A. Alexandrov, E. Chien, M. Bracey, V. Katritch, I. Wilson, and M. Yeager for careful review of the manuscript; Y. Zheng (Ohio State University) and M. Caffrey (University of Limerick) for use of the in meso robot [built with support from NIH (GM075915), NSF (IIS0308078), and SFI (02-IN1-B266)]; and A. Walker for assistance with manuscript preparation. Coordinates and structure factors have been deposited in the Protein Data Bank with identification code 2RH1.