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Science 289 (5480): 739-745

Copyright © 2000 by the American Association for the Advancement of Science

Crystal Structure of Rhodopsin: A G Protein-Coupled Receptor

Krzysztof Palczewski,123* Takashi Kumasaka,7 Tetsuya Hori,78 Craig A. Behnke,46 Hiroyuki Motoshima,7 Brian A. Fox,46 Isolde Le Trong,56 David C. Teller,46 Tetsuji Okada,1 Ronald E. Stenkamp,56* Masaki Yamamoto,7 Masashi Miyano7*

Heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs) respond to a variety of different external stimuli and activate G proteins. GPCRs share many structural features, including a bundle of seven transmembrane alpha  helices connected by six loops of varying lengths. We determined the structure of rhodopsin from diffraction data extending to 2.8 angstroms resolution. The highly organized structure in the extracellular region, including a conserved disulfide bridge, forms a basis for the arrangement of the seven-helix transmembrane motif. The ground-state chromophore, 11-cis-retinal, holds the transmembrane region of the protein in the inactive conformation. Interactions of the chromophore with a cluster of key residues determine the wavelength of the maximum absorption. Changes in these interactions among rhodopsins facilitate color discrimination. Identification of a set of residues that mediate interactions between the transmembrane helices and the cytoplasmic surface, where G-protein activation occurs, also suggests a possible structural change upon photoactivation.

1 Department of Ophthalmology,
2 Department of Pharmacology,
3 Department of Chemistry,
4 Department of Biochemistry,
5 Department of Biological Structure, and
6 Biomolecular Structure Center, University of Washington, Seattle, WA 98195, USA.
7 Structural Biophysics Laboratory, RIKEN Harima Institute, 1-1-1 Kouto, Mikazuki-cho, Sayo-gun, Hyogo 679-5148, Japan.
8 Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology, 4259 Nagatsuta, Midori-ku, Yokohama 226-8501, Japan
*   To whom correspondence should be addressed. E-mail: miyano{at} (M.M.); palczews{at} (K.P.); stenkamp{at} (R.E.S.).

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Toward Selective Drug Development for the Human 5-Hydroxytryptamine 1E Receptor: A Comparison of 5-Hydroxytryptamine 1E and 1F Receptor Structure-Affinity Relationships.
M. T. Klein, M. Dukat, R. A. Glennon, and M. Teitler (2011)
J. Pharmacol. Exp. Ther. 337, 860-867
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International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B).
S. Offermanns, S. L. Colletti, T. W. Lovenberg, G. Semple, A. Wise, and A. P. IJzerman (2011)
Pharmacol. Rev. 63, 269-290
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Role of Bulk Water in Hydrolysis of the Rhodopsin Chromophore.
B. Jastrzebska, K. Palczewski, and M. Golczak (2011)
J. Biol. Chem. 286, 18930-18937
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Differential Regulation of Two Palmitoylation Sites in the Cytoplasmic Tail of the {beta}1-Adrenergic Receptor.
D. M. Zuckerman, S. W. Hicks, G. Charron, H. C. Hang, and C. E. Machamer (2011)
J. Biol. Chem. 286, 19014-19023
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Two distinct conformations of helix 6 observed in antagonist-bound structures of a {beta}1-adrenergic receptor.
R. Moukhametzianov, T. Warne, P. C. Edwards, M. J. Serrano-Vega, A. G. W. Leslie, C. G. Tate, and G. F. X. Schertler (2011)
PNAS 108, 8228-8232
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Solid-state 2H NMR relaxation illuminates functional dynamics of retinal cofactor in membrane activation of rhodopsin.
A. V. Struts, G. F. J. Salgado, and M. F. Brown (2011)
PNAS 108, 8263-8268
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Disease-causing Mutation in PKR2 Receptor Reveals a Critical Role of Positive Charges in the Second Intracellular Loop for G-protein Coupling and Receptor Trafficking.
Z. Peng, Y. Tang, H. Luo, F. Jiang, J. Yang, L. Sun, and J.-D. Li (2011)
J. Biol. Chem. 286, 16615-16622
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Docking-based virtual screening of potential human P2Y12 receptor antagonists.
H. Chen, X. Dong, M. Zhou, H. Shi, and X. Luo (2011)
Acta Biochim Biophys Sin 43, 400-408
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