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

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E. Y. T. Chien, W. Liu, Q. Zhao, V. Katritch, G. Won Han, M. A. Hanson, L. Shi, A. H. Newman, J. A. Javitch, V. Cherezov, et al. (2010)
Science 330, 1091-1095
   Abstract »    Full Text »    PDF »
Highly conserved tyrosine stabilizes the active state of rhodopsin.
J. A. Goncalves, K. South, S. Ahuja, E. Zaitseva, C. A. Opefi, M. Eilers, R. Vogel, P. J. Reeves, and S. O. Smith (2010)
PNAS 107, 19861-19866
   Abstract »    Full Text »    PDF »
Functional Differences of Invariant and Highly Conserved Residues in the Extracellular Domain of the Glycoprotein Hormone Receptors.
K. Angelova, H. de Jonge, J. C. M. Granneman, D. Puett, and J. Bogerd (2010)
J. Biol. Chem. 285, 34813-34827
   Abstract »    Full Text »    PDF »
Structure-Activity Relationships of GPR120 Agonists Based on a Docking Simulation.
Q. Sun, A. Hirasawa, T. Hara, I. Kimura, T. Adachi, T. Awaji, M. Ishiguro, T. Suzuki, N. Miyata, and G. Tsujimoto (2010)
Mol. Pharmacol. 78, 804-810
   Abstract »    Full Text »    PDF »
Subtle conformational changes between CX3CR1 genetic variants as revealed by resonance energy transfer assays.
K. Darbandi-Tehrani, P. Hermand, S. Carvalho, K. Dorgham, A. Couvineau, J.-J. Lacapere, C. Combadiere, and P. Deterre (2010)
FASEB J 24, 4585-4598
   Abstract »    Full Text »    PDF »
Third Extracellular Loop (EC3)-N Terminus Interaction Is Important for Seven-transmembrane Domain Receptor Function: IMPLICATIONS FOR AN ACTIVATION MICROSWITCH REGION.
S. Rana and T. J. Baranski (2010)
J. Biol. Chem. 285, 31472-31483
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Exploring the Binding Site Crevice of a Family B G Protein-Coupled Receptor, the Type 1 Corticotropin Releasing Factor Receptor.
K. Gkountelias, M. Papadokostaki, J. A. Javitch, and G. Liapakis (2010)
Mol. Pharmacol. 78, 785-793
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Ligand-Supported Purification of the Urotensin-II Receptor.
A. T. Du, D. Onan, D. T. Dinh, M. J. Lew, J. Ziogas, M.-I. Aguilar, L. K. Pattenden, and W. G. Thomas (2010)
Mol. Pharmacol. 78, 639-647
   Abstract »    Full Text »    PDF »
The M1 Muscarinic Receptor Allosteric Agonists AC-42 and 1-[1'-(2-Methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one Bind to a Unique Site Distinct from the Acetylcholine Orthosteric Site.
M. A. Jacobson, C. Kreatsoulas, D. M. Pascarella, J. A. O'Brien, and C. Sur (2010)
Mol. Pharmacol. 78, 648-657
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Contrasting Modes of Evolution of the Visual Pigments in Heliconius Butterflies.
F. Yuan, G. D. Bernard, J. Le, and A. D. Briscoe (2010)
Mol. Biol. Evol. 27, 2392-2405
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Electrostatic Compensation Restores Trafficking of the Autosomal Recessive Retinitis Pigmentosa E150K Opsin Mutant to the Plasma Membrane.
L. P. Pulagam and K. Palczewski (2010)
J. Biol. Chem. 285, 29446-29456
   Abstract »    Full Text »    PDF »
Characterization of the {beta}-D-Glucopyranoside Binding Site of the Human Bitter Taste Receptor hTAS2R16.
T. Sakurai, T. Misaka, M. Ishiguro, K. Masuda, T. Sugawara, K. Ito, T. Kobayashi, S. Matsuo, Y. Ishimaru, T. Asakura, et al. (2010)
J. Biol. Chem. 285, 28373-28378
   Abstract »    Full Text »    PDF »
Evidence that Interaction between Conserved Residues in Transmembrane Helices 2, 3, and 7 Are Crucial for Human VPAC1 Receptor Activation.
A. O. Chugunov, J. Simms, D. R. Poyner, Y. Dehouck, M. Rooman, D. Gilis, and I. Langer (2010)
Mol. Pharmacol. 78, 394-401
   Abstract »    Full Text »    PDF »

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