Note to users. If you're seeing this message, it means that your browser cannot find this page's style/presentation instructions -- or possibly that you are using a browser that does not support current Web standards. Find out more about why this message is appearing, and what you can do to make your experience of our site the best it can be.

Science 4 August 2000:
Vol. 289. no. 5480, pp. 739 - 745
DOI: 10.1126/science.289.5480.739
Prev | Table of Contents | Next

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.).

Read the Full Text


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
The Fifth Transmembrane Domain of Angiotensin II Type 1 Receptor Participates in the Formation of the Ligand-binding Pocket and Undergoes a Counterclockwise Rotation upon Receptor Activation.
I. Domazet, S. S. Martin, B. J. Holleran, M.-E. Morin, P. Lacasse, P. Lavigne, E. Escher, R. Leduc, and G. Guillemette (2009)
J. Biol. Chem. 284, 31953-31961
   Abstract »    Full Text »    PDF »
Bothnia dystrophy is caused by domino-like rearrangements in cellular retinaldehyde-binding protein mutant R234W.
X. He, J. Lobsiger, and A. Stocker (2009)
PNAS 106, 18545-18550
   Abstract »    Full Text »    PDF »
Individual variation in rod absorbance spectra correlated with opsin gene polymorphism in sand goby (Pomatoschistus minutus).
M. Jokela-Maatta, A. Vartio, L. Paulin, and K. Donner (2009)
J. Exp. Biol. 212, 3415-3421
   Abstract »    Full Text »    PDF »
Dual Activities of Odorants on Olfactory and Nuclear Hormone Receptors.
H. Pick, S. Etter, O. Baud, R. Schmauder, L. Bordoli, T. Schwede, and H. Vogel (2009)
J. Biol. Chem. 284, 30547-30555
   Abstract »    Full Text »    PDF »
Lipid Protein Interactions Couple Protonation to Conformation in a Conserved Cytosolic Domain of G Protein-coupled Receptors.
S. Madathil and K. Fahmy (2009)
J. Biol. Chem. 284, 28801-28809
   Abstract »    Full Text »    PDF »
The evolution of irradiance detection: melanopsin and the non-visual opsins.
S. N. Peirson, S. Halford, and R. G. Foster (2009)
Phil Trans R Soc B 364, 2849-2865
   Abstract »    Full Text »    PDF »
Evolution of opsins and phototransduction.
Y. Shichida and T. Matsuyama (2009)
Phil Trans R Soc B 364, 2881-2895
   Abstract »    Full Text »    PDF »
Dual Role of the Second Extracellular Loop of the Cannabinoid Receptor 1: Ligand Binding and Receptor Localization.
K. H. Ahn, A. C. Bertalovitz, D. F. Mierke, and D. A. Kendall (2009)
Mol. Pharmacol. 76, 833-842
   Abstract »    Full Text »    PDF »
Differential Expression of Two Distinct Functional Isoforms of Melanopsin (Opn4) in the Mammalian Retina.
S. S. Pires, S. Hughes, M. Turton, Z. Melyan, S. N. Peirson, L. Zheng, M. Kosmaoglou, J. Bellingham, M. E. Cheetham, R. J. Lucas, et al. (2009)
J. Neurosci. 29, 12332-12342
   Abstract »    Full Text »    PDF »
Activation Induces Structural Changes in the Liganded Angiotensin II Type 1 Receptor.
M. Clement, J. Cabana, B. J. Holleran, R. Leduc, G. Guillemette, P. Lavigne, and E. Escher (2009)
J. Biol. Chem. 284, 26603-26612
   Abstract »    Full Text »    PDF »
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.
L. Ma, M. A. Seager, M. Wittmann, M. Jacobson, D. Bickel, M. Burno, K. Jones, V. K. Graufelds, G. Xu, M. Pearson, et al. (2009)
PNAS 106, 15950-15955
   Abstract »    Full Text »    PDF »
Structural waters define a functional channel mediating activation of the GPCR, rhodopsin.
T. E. Angel, S. Gupta, B. Jastrzebska, K. Palczewski, and M. R. Chance (2009)
PNAS 106, 14367-14372
   Abstract »    Full Text »    PDF »
The Magnitude of the Light-induced Conformational Change in Different Rhodopsins Correlates with Their Ability to Activate G Proteins.
H. Tsukamoto, D. L. Farrens, M. Koyanagi, and A. Terakita (2009)
J. Biol. Chem. 284, 20676-20683
   Abstract »    Full Text »    PDF »
Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice.
S. Neumann, W. Huang, S. Titus, G. Krause, G. Kleinau, A. T. Alberobello, W. Zheng, N. T. Southall, J. Inglese, C. P. Austin, et al. (2009)
PNAS 106, 12471-12476
   Abstract »    Full Text »    PDF »
Probing the role of the cation-{pi} interaction in the binding sites of GPCRs using unnatural amino acids.
M. M. Torrice, K. S. Bower, H. A. Lester, and D. A. Dougherty (2009)
PNAS 106, 11919-11924
   Abstract »    Full Text »    PDF »
Activation Switch in the Transmembrane Domain of Metabotropic Glutamate Receptor.
M. Yanagawa, T. Yamashita, and Y. Shichida (2009)
Mol. Pharmacol. 76, 201-207
   Abstract »    Full Text »    PDF »
Structural and kinetic modeling of an activating helix switch in the rhodopsin-transducin interface.
P. Scheerer, M. Heck, A. Goede, J. H. Park, H.-W. Choe, O. P. Ernst, K. P. Hofmann, and P. W. Hildebrand (2009)
PNAS 106, 10660-10665
   Abstract »    Full Text »    PDF »
APH1 Polar Transmembrane Residues Regulate the Assembly and Activity of Presenilin Complexes.
R. Pardossi-Piquard, S.-P. Yang, S. Kanemoto, Y. Gu, F. Chen, C. Bohm, J. Sevalle, T. Li, P. C. Wong, F. Checler, et al. (2009)
J. Biol. Chem. 284, 16298-16307
   Abstract »    Full Text »    PDF »
Role of Molecular Chaperones in G Protein {beta}5/Regulator of G Protein Signaling Dimer Assembly and G Protein {beta}{gamma} Dimer Specificity.
A. C. Howlett, A. J. Gray, J. M. Hunter, and B. M. Willardson (2009)
J. Biol. Chem. 284, 16386-16399
   Abstract »    Full Text »    PDF »
Shedding Light on Serpent Sight: The Visual Pigments of Henophidian Snakes.
W. L. Davies, J. A. Cowing, J. K. Bowmaker, L. S. Carvalho, D. J. Gower, and D. M. Hunt (2009)
J. Neurosci. 29, 7519-7525
   Abstract »    Full Text »    PDF »
The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex.
X. J. Yao, G. Velez Ruiz, M. R. Whorton, S. G. F. Rasmussen, B. T. DeVree, X. Deupi, R. K. Sunahara, and B. Kobilka (2009)
PNAS 106, 9501-9506
   Abstract »    Full Text »    PDF »
Selection and characterization of DARPins specific for the neurotensin receptor 1.
P. Milovnik, D. Ferrari, C. A. Sarkar, and A. Pluckthun (2009)
Protein Eng. Des. Sel. 22, 357-366
   Abstract »    Full Text »    PDF »
Elucidation of Binding Sites of Dual Antagonists in the Human Chemokine Receptors CCR2 and CCR5.
S. E. Hall, A. Mao, V. Nicolaidou, M. Finelli, E. L. Wise, B. Nedjai, J. Kanjanapangka, P. Harirchian, D. Chen, V. Selchau, et al. (2009)
Mol. Pharmacol. 75, 1325-1336
   Abstract »    Full Text »    PDF »
Conserved waters mediate structural and functional activation of family A (rhodopsin-like) G protein-coupled receptors.
T. E. Angel, M. R. Chance, and K. Palczewski (2009)
PNAS 106, 8555-8560
   Abstract »    Full Text »    PDF »
Thyroid stimulating autoantibody M22 mimics TSH binding to the TSH receptor leucine rich domain: a comparative structural study of protein-protein interactions.
R Nunez Miguel, J Sanders, D Y Chirgadze, J Furmaniak, and B Rees Smith (2009)
J. Mol. Endocrinol. 42, 381-395
   Abstract »    Full Text »    PDF »
Minireview: GPCR and G Proteins: Drug Efficacy and Activation in Live Cells.
J.-P. Vilardaga, M. Bunemann, T. N. Feinstein, N. Lambert, V. O. Nikolaev, S. Engelhardt, M. J. Lohse, and C. Hoffmann (2009)
Mol. Endocrinol. 23, 590-599
   Abstract »    Full Text »    PDF »
Multifaceted Approach to Determine the Antagonist Molecular Mechanism and Interaction of Ibodutant ([1-(2-Phenyl-1R-{[1-(tetrahydropyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide) at the Human Tachykinin NK2 Receptor.
S. Meini, F. Bellucci, C. Catalani, P. Cucchi, A. Giolitti, P. Santicioli, and S. Giuliani (2009)
J. Pharmacol. Exp. Ther. 329, 486-495
   Abstract »    Full Text »    PDF »
Helix 8 of leukotriene B4 type-2 receptor is required for the folding to pass the quality control in the endoplasmic reticulum.
D. Yasuda, T. Okuno, T. Yokomizo, T. Hori, N. Hirota, T. Hashidate, M. Miyano, T. Shimizu, and M. Nakamura (2009)
FASEB J 23, 1470-1481
   Abstract »    Full Text »    PDF »
The Second Transmembrane Domain of the Human Type 1 Angiotensin II Receptor Participates in the Formation of the Ligand Binding Pocket and Undergoes Integral Pivoting Movement during the Process of Receptor Activation.
I. Domazet, B. J. Holleran, S. S. Martin, P. Lavigne, R. Leduc, E. Escher, and G. Guillemette (2009)
J. Biol. Chem. 284, 11922-11929
   Abstract »    Full Text »    PDF »
Thyrotropin and Homologous Glycoprotein Hormone Receptors: Structural and Functional Aspects of Extracellular Signaling Mechanisms.
G. Kleinau and G. Krause (2009)
Endocr. Rev. 30, 133-151
   Abstract »    Full Text »    PDF »
Conformational Toggle Switches Implicated in Basal Constitutive and Agonist-Induced Activated States of 5-Hydroxytryptamine-4 Receptors.
L. P. Pellissier, J. Sallander, M. Campillo, F. Gaven, E. Queffeulou, M. Pillot, A. Dumuis, S. Claeysen, J. Bockaert, and L. Pardo (2009)
Mol. Pharmacol. 75, 982-990
   Abstract »    Full Text »    PDF »
Identification of two distinct inactive conformations of the {beta}2-adrenergic receptor reconciles structural and biochemical observations.
R. O. Dror, D. H. Arlow, D. W. Borhani, M. O. Jensen, S. Piana, and D. E. Shaw (2009)
PNAS 106, 4689-4694
   Abstract »    Full Text »    PDF »
Into the blue: Gene duplication and loss underlie color vision adaptations in a deep-sea chimaera, the elephant shark Callorhinchus milii.
W. L. Davies, L. S. Carvalho, B.-H. Tay, S. Brenner, D. M. Hunt, and B. Venkatesh (2009)
Genome Res. 19, 415-426
   Abstract »    Full Text »    PDF »
Fluorescence Resonance Energy Transfer Analysis of {alpha}2a-Adrenergic Receptor Activation Reveals Distinct Agonist-Specific Conformational Changes.
A. Zurn, U. Zabel, J.-P. Vilardaga, H. Schindelin, M. J. Lohse, and C. Hoffmann (2009)
Mol. Pharmacol. 75, 534-541
   Abstract »    Full Text »    PDF »
Ribosomal S6 Kinase 2 Directly Phosphorylates the 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptor, Thereby Modulating 5-HT2A Signaling.
R. T. Strachan, D. J. Sheffler, B. Willard, M. Kinter, J. G. Kiselar, and B. L. Roth (2009)
J. Biol. Chem. 284, 5557-5573
   Abstract »    Full Text »    PDF »
Two Arginine-Glutamate Ionic Locks Near the Extracellular Surface of FFAR1 Gate Receptor Activation.
C. S. Sum, I. G. Tikhonova, S. Costanzi, and M. C. Gershengorn (2009)
J. Biol. Chem. 284, 3529-3536
   Abstract »    Full Text »    PDF »
Isolation and functional characterization of a stable complex between photoactivated rhodopsin and the G protein, transducin.
B. Jastrzebska, M. Golczak, D. Fotiadis, A. Engel, and K. Palczewski (2009)
FASEB J 23, 371-381
   Abstract »    Full Text »    PDF »
The C-terminal Tail of CRTH2 Is a Key Molecular Determinant That Constrains G{alpha}i and Downstream Signaling Cascade Activation.
R. Schroder, N. Merten, J. M. Mathiesen, L. Martini, A. Kruljac-Letunic, F. Krop, A. Blaukat, Y. Fang, E. Tran, T. Ulven, et al. (2009)
J. Biol. Chem. 284, 1324-1336
   Abstract »    Full Text »    PDF »
PROKR2 missense mutations associated with Kallmann syndrome impair receptor signalling activity.
C. Monnier, C. Dode, L. Fabre, L. Teixeira, G. Labesse, J.-P. Pin, J.-P. Hardelin, and P. Rondard (2009)
Hum. Mol. Genet. 18, 75-81
   Abstract »    Full Text »    PDF »
Functional Characterization and Structural Modeling of Obesity Associated Mutations in the Melanocortin 4 Receptor.
K. Tan, I. D. Pogozheva, G. S. H. Yeo, D. Hadaschik, J. M. Keogh, C. Haskell-Leuvano, S. O'Rahilly, H. I. Mosberg, and I. S. Farooqi (2009)
Endocrinology 150, 114-125
   Abstract »    Full Text »    PDF »
Topology of Class A G Protein-Coupled Receptors: Insights Gained from Crystal Structures of Rhodopsins, Adrenergic and Adenosine Receptors.
D. Mustafi and K. Palczewski (2009)
Mol. Pharmacol. 75, 1-12
   Abstract »    Full Text »    PDF »
An Intracellular Loop 2 Amino Acid Residue Determines Differential Binding of Arrestin to the Dopamine D2 and D3 Receptors.
H. Lan, M. M. Teeter, V. V. Gurevich, and K. A. Neve (2009)
Mol. Pharmacol. 75, 19-26
   Abstract »    Full Text »    PDF »
SuperScent--a database of flavors and scents.
M. Dunkel, U. Schmidt, S. Struck, L. Berger, B. Gruening, J. Hossbach, I. S. Jaeger, U. Effmert, B. Piechulla, R. Eriksson, et al. (2009)
Nucleic Acids Res. 37, D291-D294
   Abstract »    Full Text »    PDF »
Inactivation of G-protein-coupled Receptor 48 (Gpr48/Lgr4) Impairs Definitive Erythropoiesis at Midgestation through Down-regulation of the ATF4 Signaling Pathway.
H. Song, J. Luo, W. Luo, J. Weng, Z. Wang, B. Li, D. Li, and M. Liu (2008)
J. Biol. Chem. 283, 36687-36697
   Abstract »    Full Text »    PDF »
Linking Non-peptide Ligand Binding Mode to Activity at the Human Cholecystokinin-2 Receptor.
M. Foucaud, E. Marco, C. Escrieut, C. Low, B. Kalindjian, and D. Fourmy (2008)
J. Biol. Chem. 283, 35860-35868
   Abstract »    Full Text »    PDF »
Residue 17 of Sauvagine Cross-links to the First Transmembrane Domain of Corticotropin-releasing Factor Receptor 1 (CRFR1).
I. Assil-Kishawi, T. A. Samra, D. F. Mierke, and A. B. Abou-Samra (2008)
J. Biol. Chem. 283, 35644-35651
   Abstract »    Full Text »    PDF »
A Low-Molecular-Weight Antagonist for the Human Thyrotropin Receptor with Therapeutic Potential for Hyperthyroidism.
S. Neumann, G. Kleinau, S. Costanzi, S. Moore, J.-k. Jiang, B. M. Raaka, C. J. Thomas, G. Krause, and M. C. Gershengorn (2008)
Endocrinology 149, 5945-5950
   Abstract »    Full Text »    PDF »
The Third Intracellular Loop Stabilizes the Inactive State of the Neuropeptide Y1 Receptor.
M. J. S. Chee, K. Morl, D. Lindner, N. Merten, G. W. Zamponi, P. E. Light, A. G. Beck-Sickinger, and W. F. Colmers (2008)
J. Biol. Chem. 283, 33337-33346
   Abstract »    Full Text »    PDF »
The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist.
V.-P. Jaakola, M. T. Griffith, M. A. Hanson, V. Cherezov, E. Y. T. Chien, J. R. Lane, A. P. IJzerman, and R. C. Stevens (2008)
Science 322, 1211-1217
   Abstract »    Full Text »    PDF »
Two protonation switches control rhodopsin activation in membranes.
M. Mahalingam, K. Martinez-Mayorga, M. F. Brown, and R. Vogel (2008)
PNAS 105, 17795-17800
   Abstract »    Full Text »    PDF »
Complement Component 5a Receptor Oligomerization and Homologous Receptor Down-regulation.
M.-J. Rabiet, E. Huet, and F. Boulay (2008)
J. Biol. Chem. 283, 31038-31046
   Abstract »    Full Text »    PDF »
A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity: MUSCARINIC PARTIAL AGONIST McN-A-343 AS A BITOPIC ORTHOSTERIC/ALLOSTERIC LIGAND.
C. Valant, K. J. Gregory, N. E. Hall, P. J. Scammells, M. J. Lew, P. M. Sexton, and A. Christopoulos (2008)
J. Biol. Chem. 283, 29312-29321
   Abstract »    Full Text »    PDF »
Phenylalanine 169 in the Second Extracellular Loop of the Human Histamine H4 Receptor Is Responsible for the Difference in Agonist Binding between Human and Mouse H4 Receptors.
H. D. Lim, A. Jongejan, R. A. Bakker, E. Haaksma, I. J. P. de Esch, and R. Leurs (2008)
J. Pharmacol. Exp. Ther. 327, 88-96
   Abstract »    Full Text »    PDF »
The Cloned Equine Thyrotropin Receptor Is Hypersensitive to Human Chorionic Gonadotropin; Identification of Three Residues in the Extracellular Domain Involved in Ligand Specificity.
J. Royer, A. Lefevre-Minisini, G. Caltabiano, T. Lacombe, Y. Malthiery, F. Savagner, L. Pardo, and P. Rodien (2008)
Endocrinology 149, 5088-5096
   Abstract »    Full Text »    PDF »
Structural Motifs of Importance for the Constitutive Activity of the Orphan 7TM Receptor EBI2: Analysis of Receptor Activation in the Absence of an Agonist.
T. Benned-Jensen and M. M. Rosenkilde (2008)
Mol. Pharmacol. 74, 1008-1021
   Abstract »    Full Text »    PDF »
Engineering G protein-coupled receptor expression in bacteria.
G. Skretas and G. Georgiou (2008)
PNAS 105, 14747-14748
   Full Text »    PDF »
From the Cover: Directed evolution of a G protein-coupled receptor for expression, stability, and binding selectivity.
C. A. Sarkar, I. Dodevski, M. Kenig, S. Dudli, A. Mohr, E. Hermans, and A. Pluckthun (2008)
PNAS 105, 14808-14813
   Abstract »    Full Text »    PDF »
From the Cover: Elucidation of phenotypic adaptations: Molecular analyses of dim-light vision proteins in vertebrates.
S. Yokoyama, T. Tada, H. Zhang, and L. Britt (2008)
PNAS 105, 13480-13485
   Abstract »    Full Text »    PDF »
FSH and TSH binding to their respective receptors: similarities, differences and implication for glycoprotein hormone specificity.
R Nunez Miguel, J Sanders, D Y Chirgadze, T L Blundell, J Furmaniak, and B Rees Smith (2008)
J. Mol. Endocrinol. 41, 145-164
   Abstract »    Full Text »    PDF »
Mutational Analysis of the Conserved Asp2.50 and ERY Motif Reveals Signaling Bias of the Urotensin II Receptor.
C. D. Proulx, B. J. Holleran, A. A. Boucard, E. Escher, G. Guillemette, and R. Leduc (2008)
Mol. Pharmacol. 74, 552-561
   Abstract »    Full Text »    PDF »
Co-evolving stability and conformational homogeneity of the human adenosine A2a receptor.
F. Magnani, Y. Shibata, M. J. Serrano-Vega, and C. G. Tate (2008)
PNAS 105, 10744-10749
   Abstract »    Full Text »    PDF »
A Novel Adrenocorticotropin Receptor Mutation Alters Its Structure and Function, Causing Familial Glucocorticoid Deficiency.
R. A. Artigas, A. Gonzalez, E. Riquelme, C. A. Carvajal, A. Cattani, A. Martinez-Aguayo, A. M. Kalergis, T. Perez-Acle, and C. E. Fardella (2008)
J. Clin. Endocrinol. Metab. 93, 3097-3105
   Abstract »    Full Text »    PDF »
Evidence for cooperative signal triggering at the extracellular loops of the TSH receptor.
G. Kleinau, H. Jaeschke, S. Mueller, B. M. Raaka, S. Neumann, R. Paschke, and G. Krause (2008)
FASEB J 22, 2798-2808
   Abstract »    Full Text »    PDF »
How vision begins: An odyssey.
D.-G. Luo, T. Xue, and K.-W. Yau (2008)
PNAS 105, 9855-9862
   Abstract »    Full Text »    PDF »
In silico identified CCR4 antagonists target regulatory T cells and exert adjuvant activity in vaccination.
J. Bayry, E. Z. Tchilian, M. N. Davies, E. K. Forbes, S. J. Draper, S. V. Kaveri, A. V. S. Hill, M. D. Kazatchkine, P. C. L. Beverley, D. R. Flower, et al. (2008)
PNAS 105, 10221-10226
   Abstract »    Full Text »    PDF »
A High-Throughput Screening Method for Small-Molecule Pharmacologic Chaperones of Misfolded Rhodopsin.
S. M. Noorwez, D. A. Ostrov, J. H. McDowell, M. P. Krebs, and S. Kaushal (2008)
Invest. Ophthalmol. Vis. Sci. 49, 3224-3230
   Abstract »    Full Text »    PDF »
Extended Hormone Binding Site of the Human Thyroid Stimulating Hormone Receptor: DISTINCTIVE ACIDIC RESIDUES IN THE HINGE REGION ARE INVOLVED IN BOVINE THYROID STIMULATING HORMONE BINDING AND RECEPTOR ACTIVATION.
S. Mueller, G. Kleinau, H. Jaeschke, R. Paschke, and G. Krause (2008)
J. Biol. Chem. 283, 18048-18055
   Abstract »    Full Text »    PDF »
Crystal Structure of Squid Rhodopsin with Intracellularly Extended Cytoplasmic Region.
T. Shimamura, K. Hiraki, N. Takahashi, T. Hori, H. Ago, K. Masuda, K. Takio, M. Ishiguro, and M. Miyano (2008)
J. Biol. Chem. 283, 17753-17756
   Abstract »    Full Text »    PDF »
Me-Talnetant and Osanetant Interact within Overlapping but Not Identical Binding Pockets in the Human Tachykinin Neurokinin 3 Receptor Transmembrane Domains.
P. Malherbe, C. Bissantz, A. Marcuz, C. Kratzeisen, M.-T. Zenner, J. G. Wettstein, H. Ratni, C. Riemer, and W. Spooren (2008)
Mol. Pharmacol. 73, 1736-1750
   Abstract »    Full Text »    PDF »
From the Cover: High-resolution distance mapping in rhodopsin reveals the pattern of helix movement due to activation.
C. Altenbach, A. K. Kusnetzow, O. P. Ernst, K. P. Hofmann, and W. L. Hubbell (2008)
PNAS 105, 7439-7444
   Abstract »    Full Text »    PDF »
Rhodopsin's active state is frozen like a DEER in the headlights.
T. Huber and T. P. Sakmar (2008)
PNAS 105, 7343-7344
   Full Text »    PDF »
Crystal Structure of D351A and P312A Mutant Forms of the Mammalian Sarcoplasmic Reticulum Ca2+-ATPase Reveals Key Events in Phosphorylation and Ca2+ Release.
A. Marchand, A.-M. L. Winther, P. J. Holm, C. Olesen, C. Montigny, B. Arnou, P. Champeil, J. D. Clausen, B. Vilsen, J. P. Andersen, et al. (2008)
J. Biol. Chem. 283, 14867-14882
   Abstract »    Full Text »    PDF »
The Cannabinoid Receptors Are Required for Ultraviolet-Induced Inflammation and Skin Cancer Development.
D. Zheng, A. M. Bode, Q. Zhao, Y.-Y. Cho, F. Zhu, W.-Y. Ma, and Z. Dong (2008)
Cancer Res. 68, 3992-3998
   Abstract »    Full Text »    PDF »
The Thyrotropin Receptor Hinge Region Is Not Simply a Scaffold for the Leucine-Rich Domain but Contributes to Ligand Binding and Signal Transduction.
Y. Mizutori, C.-R. Chen, S. M. McLachlan, and B. Rapoport (2008)
Mol. Endocrinol. 22, 1171-1182
   Abstract »    Full Text »    PDF »
Crystallizing Thinking about the {beta}2-Adrenergic Receptor.
A. K. Shukla, J.-P. Sun, and R. J. Lefkowitz (2008)
Mol. Pharmacol. 73, 1333-1338
   Abstract »    Full Text »    PDF »
Allosteric Ligands for the Corticotropin Releasing Factor Type 1 Receptor Modulate Conformational States Involved in Receptor Activation.
S. R. J. Hoare, B. A. Fleck, R. S. Gross, P. D. Crowe, J. P. Williams, and D. E. Grigoriadis (2008)
Mol. Pharmacol. 73, 1371-1380
   Abstract »    Full Text »    PDF »
Acceleration of Cardiovascular Disease by a Dysfunctional Prostacyclin Receptor Mutation: Potential Implications for Cyclooxygenase-2 Inhibition.
E. Arehart, J. Stitham, F. W. Asselbergs, K. Douville, T. MacKenzie, K. M. Fetalvero, S. Gleim, Z. Kasza, Y. Rao, L. Martel, et al. (2008)
Circ. Res. 102, 986-993
   Abstract »    Full Text »    PDF »
Post-activation-mediated Changes in Opioid Receptors Detected by N-terminal Antibodies.
A. Gupta, R. Rozenfeld, I. Gomes, K. M. Raehal, F. M. Decaillot, L. M. Bohn, and L. A. Devi (2008)
J. Biol. Chem. 283, 10735-10744
   Abstract »    Full Text »    PDF »
Multiple Roles for the C-terminal Tail of the Chemokine Scavenger D6.
C. V. McCulloch, V. Morrow, S. Milasta, I. Comerford, G. Milligan, G. J. Graham, N. W. Isaacs, and R. J. B. Nibbs (2008)
J. Biol. Chem. 283, 7972-7982
   Abstract »    Full Text »    PDF »
Dimerization and oligomerization of G-protein-coupled receptors: debated structures with established and emerging functions.
L. Szidonya, M. Cserzo, and L. Hunyady (2008)
J. Endocrinol. 196, 435-453
   Abstract »    Full Text »    PDF »
Vertebrate Membrane Proteins: Structure, Function, and Insights from Biophysical Approaches.
D. J. Muller, N. Wu, and K. Palczewski (2008)
Pharmacol. Rev. 60, 43-78
   Abstract »    Full Text »    PDF »
An Intracellular Allosteric Site for a Specific Class of Antagonists of the CC Chemokine G Protein-Coupled Receptors CCR4 and CCR5.
G. Andrews, C. Jones, and K. A. Wreggett (2008)
Mol. Pharmacol. 73, 855-867
   Abstract »    Full Text »    PDF »
Rhodopsin and 9-Demethyl-retinal Analog: EFFECT OF A PARTIAL AGONIST ON DISPLACEMENT OF TRANSMEMBRANE HELIX 6 IN CLASS A G PROTEIN-COUPLED RECEPTORS.
B. Knierim, K. P. Hofmann, W. Gartner, W. L. Hubbell, and O. P. Ernst (2008)
J. Biol. Chem. 283, 4967-4974
   Abstract »    Full Text »    PDF »
Efficient Coupling of Transducin to Monomeric Rhodopsin in a Phospholipid Bilayer.
M. R. Whorton, B. Jastrzebska, P. S.-H. Park, D. Fotiadis, A. Engel, K. Palczewski, and R. K. Sunahara (2008)
J. Biol. Chem. 283, 4387-4394
   Abstract »    Full Text »    PDF »
Characterization of G-Protein Coupled Receptor Kinase Interaction with the Neurokinin-1 Receptor Using Bioluminescence Resonance Energy Transfer.
R. Jorgensen, N. D. Holliday, J. L. Hansen, M. Vrecl, A. Heding, T. W. Schwartz, and C. E. Elling (2008)
Mol. Pharmacol. 73, 349-358
   Abstract »    Full Text »    PDF »
[3H]Org 43553, the First Low-Molecular-Weight Agonistic and Allosteric Radioligand for the Human Luteinizing Hormone Receptor.
L. H. Heitman, J. Oosterom, K. M. Bonger, C. M. Timmers, P. H. G. Wiegerinck, and A. P. IJzerman (2008)
Mol. Pharmacol. 73, 518-524
   Abstract »    Full Text »    PDF »
Conformational thermostabilization of the {beta}1-adrenergic receptor in a detergent-resistant form.
M. J. Serrano-Vega, F. Magnani, Y. Shibata, and C. G. Tate (2008)
PNAS 105, 877-882
   Abstract »    Full Text »    PDF »
Site-specific Incorporation of Keto Amino Acids into Functional G Protein-coupled Receptors Using Unnatural Amino Acid Mutagenesis.
S. Ye, C. Kohrer, T. Huber, M. Kazmi, P. Sachdev, E. C.Y. Yan, A. Bhagat, U. L. RajBhandary, and T. P. Sakmar (2008)
J. Biol. Chem. 283, 1525-1533
   Abstract »    Full Text »    PDF »
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
   Abstract »    Full Text »    PDF »
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
   Abstract »    Full Text »    PDF »
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
   Abstract »    Full Text »    PDF »
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
   Abstract »    Full Text »    PDF »
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
   Abstract »    Full Text »    PDF »
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
   Abstract »    Full Text »    PDF »
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
   Abstract »    Full Text »    PDF »
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
   Abstract »    Full Text »    PDF »


To Advertise     Find Products

Science. ISSN 0036-8075 (print), 1095-9203 (online)