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Science 4 August 2000:
Vol. 289. no. 5480, pp. 739 - 745
DOI: 10.1126/science.289.5480.739

Research Articles

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}spring8.or.jp (M.M.); palczews{at}u.washington.edu (K.P.); stenkamp{at}u.washington.edu (R.E.S.).


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Expression of a Functional G Protein-Coupled Receptor 54-Kisspeptin Autoregulatory System in Hypothalamic Gonadotropin-Releasing Hormone Neurons.
S. Quaynor, L. Hu, P. K. Leung, H. Feng, N. Mores, L. Z. Krsmanovic, and K. J. Catt (2007)
Mol. Endocrinol. 21, 3062-3070
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Roof and Floor of the Muscarinic Binding Pocket: Variations in the Binding Modes of Orthosteric Ligands.
J. A. Goodwin, E. C. Hulme, C. J. Langmead, and B. G. Tehan (2007)
Mol. Pharmacol. 72, 1484-1496
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High-Resolution Crystal Structure of an Engineered Human 2-Adrenergic G Protein Coupled Receptor.
V. Cherezov, D. M. Rosenbaum, M. A. Hanson, S. G. F. Rasmussen, F. S. Thian, T. S. Kobilka, H.-J. Choi, P. Kuhn, W. I. Weis, B. K. Kobilka, et al. (2007)
Science 318, 1258-1265
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Isolation and characterization of melanopsin (Opn4) from the Australian marsupial Sminthopsis crassicaudata (fat-tailed dunnart).
S. S Pires, J. Shand, J. Bellingham, C. Arrese, M. Turton, S. Peirson, R. G Foster, and S. Halford (2007)
Proc R Soc B 274, 2791-2799
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Functional Analysis of Transmembrane Domain 2 of the M1 Muscarinic Acetylcholine Receptor.
M. S. Bee and E. C. Hulme (2007)
J. Biol. Chem. 282, 32471-32479
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Inhibitory role of CXCR4 glycan in CD4-independent X4-tropic human immunodeficiency virus type 1 infection and its abrogation in CD4-dependent infection.
Y. Kubo, M. Yokoyama, H. Yoshii, C. Mitani, C. Tominaga, Y. Tanaka, H. Sato, and N. Yamamoto (2007)
J. Gen. Virol. 88, 3139-3144
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Assessment of the Roles of Serines 5.43(239) and 5.46(242) for Binding and Potency of Agonist Ligands at the Human Serotonin 5-HT2A Receptor.
M. R. Braden and D. E. Nichols (2007)
Mol. Pharmacol. 72, 1200-1209
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Transmembrane Segment IV Contributes a Functionally Important Interface for Oligomerization of the Class II G Protein-coupled Secretin Receptor.
K. G. Harikumar, D. I. Pinon, and L. J. Miller (2007)
J. Biol. Chem. 282, 30363-30372
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Identification of Residues Important for Agonist Recognition and Activation in GPR40.
C. S. Sum, I. G. Tikhonova, S. Neumann, S. Engel, B. M. Raaka, S. Costanzi, and M. C. Gershengorn (2007)
J. Biol. Chem. 282, 29248-29255
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Pituitary-Thyroid Setpoint and Thyrotropin Receptor Expression in Consomic Rats.
L. C. Moeller, M. Alonso, X. Liao, V. Broach, A. Dumitrescu, J. Van Sande, L. Montanelli, S. Skjei, C. Goodwin, H. Grasberger, et al. (2007)
Endocrinology 148, 4727-4733
   Abstract »    Full Text »    PDF »
Structures of the CCR5 N Terminus and of a Tyrosine-Sulfated Antibody with HIV-1 gp120 and CD4.
C.-c. Huang, S. N. Lam, P. Acharya, M. Tang, S.-H. Xiang, S. S.-u. Hussan, R. L. Stanfield, J. Robinson, J. Sodroski, I. A. Wilson, et al. (2007)
Science 317, 1930-1934
   Abstract »    Full Text »    PDF »
Mechanism of Activation of a G Protein-coupled Receptor, the Human Cholecystokinin-2 Receptor.
E. Marco, M. Foucaud, I. Langer, C. Escrieut, I. G. Tikhonova, and D. Fourmy (2007)
J. Biol. Chem. 282, 28779-28790
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Small Molecule Receptor Agonists and Antagonists of CCR3 Provide Insight into Mechanisms of Chemokine Receptor Activation.
E. L. Wise, C. Duchesnes, P. C. A. da Fonseca, R. A. Allen, T. J. Williams, and J. E. Pease (2007)
J. Biol. Chem. 282, 27935-27943
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Distinct Structural Changes in a G Protein-coupled Receptor Caused by Different Classes of Agonist Ligands.
J. H. Li, S.-J. Han, F. F. Hamdan, S.-K. Kim, K. A. Jacobson, L. M. Bloodworth, X. Zhang, and J. Wess (2007)
J. Biol. Chem. 282, 26284-26293
   Abstract »    Full Text »    PDF »
Functional characterization, tuning, and regulation of visual pigment gene expression in an anadromous lamprey.
W. L. Davies, J. A. Cowing, L. S. Carvalho, I. C. Potter, A. E. O. Trezise, D. M. Hunt, and S. P. Collin (2007)
FASEB J 21, 2713-2724
   Abstract »    Full Text »    PDF »
Gene Duplication Is an Evolutionary Mechanism for Expanding Spectral Diversity in the Long-Wavelength Photopigments of Butterflies.
F. D. Frentiu, G. D. Bernard, M. P. Sison-Mangus, A. Van Zandt Brower, and A. D. Briscoe (2007)
Mol. Biol. Evol. 24, 2016-2028
   Abstract »    Full Text »    PDF »
Critical Role for the Second Extracellular Loop in the Binding of Both Orthosteric and Allosteric G Protein-coupled Receptor Ligands.
V. A. Avlani, K. J. Gregory, C. J. Morton, M. W. Parker, P. M. Sexton, and A. Christopoulos (2007)
J. Biol. Chem. 282, 25677-25686
   Abstract »    Full Text »    PDF »
Crystal structure of the incretin-bound extracellular domain of a G protein-coupled receptor.
C. Parthier, M. Kleinschmidt, P. Neumann, R. Rudolph, S. Manhart, D. Schlenzig, J. Fanghanel, J.-U. Rahfeld, H.-U. Demuth, and M. T. Stubbs (2007)
PNAS 104, 13942-13947
   Abstract »    Full Text »    PDF »
Helix 8 Leu in the CB1 Cannabinoid Receptor Contributes to Selective Signal Transduction Mechanisms.
S. Anavi-Goffer, D. Fleischer, D. P. Hurst, D. L. Lynch, J. Barnett-Norris, S. Shi, D. L. Lewis, S. Mukhopadhyay, A. C. Howlett, P. H. Reggio, et al. (2007)
J. Biol. Chem. 282, 25100-25113
   Abstract »    Full Text »    PDF »
Trapping of a Nonpeptide Ligand by the Extracellular Domains of the Gonadotropin-Releasing Hormone Receptor Results in Insurmountable Antagonism.
T. A. Kohout, Q. Xie, S. Reijmers, K. J. Finn, Z. Guo, Y.-F. Zhu, and R. S. Struthers (2007)
Mol. Pharmacol. 72, 238-247
   Abstract »    Full Text »    PDF »
Receptor-Mediated Activation of Heterotrimeric G-Proteins: Current Structural Insights.
C. A. Johnston and D. P. Siderovski (2007)
Mol. Pharmacol. 72, 219-230
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Molecular Approximations between Residues 21 and 23 of Secretin and Its Receptor: Development of a Model for Peptide Docking with the Amino Terminus of the Secretin Receptor.
M. Dong, P. C.-H. Lam, F. Gao, K. Hosohata, D. I. Pinon, P. M. Sexton, R. Abagyan, and L. J. Miller (2007)
Mol. Pharmacol. 72, 280-290
   Abstract »    Full Text »    PDF »
Molecular Interaction of a Potent Nonpeptide Agonist with the Chemokine Receptor CCR8.
P. C. Jensen, R. Nygaard, S. Thiele, A. Elder, G. Zhu, R. Kolbeck, S. Ghosh, T. W. Schwartz, and M. M. Rosenkilde (2007)
Mol. Pharmacol. 72, 327-340
   Abstract »    Full Text »    PDF »
Statistical prediction of protein chemical interactions based on chemical structure and mass spectrometry data.
N. Nagamine and Y. Sakakibara (2007)
Bioinformatics 23, 2004-2012
   Abstract »    Full Text »    PDF »



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