This Article Full Text Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Citation Map Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Request Copyright Permission Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Gether, U. Search for Related Content PubMed PubMed Citation Articles by Gether, U.

Uncovering Molecular Mechanisms Involved in Activation of G Protein-Coupled Receptors

Division of Cellular and Molecular Physiology, Department of Medical Physiology, The Panum Institute, University of Copenhagen, DK-2200 Copenhagen, Denmark

G protein-coupled, seven-transmembrane segment receptors (GPCRs or 7TM receptors), with more than 1000 different members, comprise the largest superfamily of proteins in the body. Since the cloning of the first receptors more than a decade ago, extensive experimental work has uncovered multiple aspects of their function and challenged many traditional paradigms. However, it is only recently that we are beginning to gain insight into some of the most fundamental questions in the molecular function of this class of receptors. How can, for example, so many chemically diverse hormones, neurotransmitters, and other signaling molecules activate receptors believed to share a similar overall tertiary structure? What is the nature of the physical changes linking agonist binding to receptor activation and subsequent transduction of the signal to the associated G protein on the cytoplasmic side of the membrane and to other putative signaling pathways? The goal of the present review is to specifically address these questions as well as to depict the current awareness about GPCR structure-function relationships in general.

This article has been cited by other articles:

				D. Sohy, H. Yano, P. de Nadai, E. Urizar, A. Guillabert, J. A. Javitch, M. Parmentier, and J.-Y. Springael Hetero-oligomerization of CCR2, CCR5, and CXCR4 and the Protean Effects of "Selective" Antagonists J. Biol. Chem., November 6, 2009; 284(45): 31270 - 31279. [Abstract] [Full Text] [PDF]

				H. Tsukamoto, D. L. Farrens, M. Koyanagi, and A. Terakita The Magnitude of the Light-induced Conformational Change in Different Rhodopsins Correlates with Their Ability to Activate G Proteins J. Biol. Chem., July 31, 2009; 284(31): 20676 - 20683. [Abstract] [Full Text] [PDF]

				M. Duran-Prado, M. D. Gahete, A. J. Martinez-Fuentes, R. M. Luque, A. Quintero, S. M. Webb, P. Benito-Lopez, A. Leal, S. Schulz, F. Gracia-Navarro, et al. Identification and Characterization of Two Novel Truncated but Functional Isoforms of the Somatostatin Receptor Subtype 5 Differentially Present in Pituitary Tumors J. Clin. Endocrinol. Metab., July 1, 2009; 94(7): 2634 - 2643. [Abstract] [Full Text] [PDF]

				H. A. Ghofrani, R. J. Barst, R. L. Benza, H. C. Champion, K. A. Fagan, F. Grimminger, M. Humbert, G. Simonneau, D. J. Stewart, C. Ventura, et al. Future perspectives for the treatment of pulmonary arterial hypertension. J. Am. Coll. Cardiol., June 30, 2009; 54(1 Suppl): S108 - S117. [Abstract] [Full Text] [PDF]

				Y.-L. Zhang, J. A. Frangos, and M. Chachisvilis Mechanical stimulus alters conformation of type 1 parathyroid hormone receptor in bone cells Am J Physiol Cell Physiol, June 1, 2009; 296(6): C1391 - C1399. [Abstract] [Full Text] [PDF]

				E. Schepers, G. Glorieux, A. Dhondt, L. Leybaert, and R. Vanholder Role of symmetric dimethylarginine in vascular damage by increasing ROS via store-operated calcium influx in monocytes Nephrol. Dial. Transplant., May 1, 2009; 24(5): 1429 - 1435. [Abstract] [Full Text] [PDF]

				J.-P. Vilardaga, M. Bunemann, T. N. Feinstein, N. Lambert, V. O. Nikolaev, S. Engelhardt, M. J. Lohse, and C. Hoffmann Minireview: GPCR and G Proteins: Drug Efficacy and Activation in Live Cells Mol. Endocrinol., May 1, 2009; 23(5): 590 - 599. [Abstract] [Full Text] [PDF]

				A. Zurn, U. Zabel, J.-P. Vilardaga, H. Schindelin, M. J. Lohse, and C. Hoffmann Fluorescence Resonance Energy Transfer Analysis of {alpha}2a-Adrenergic Receptor Activation Reveals Distinct Agonist-Specific Conformational Changes Mol. Pharmacol., March 1, 2009; 75(3): 534 - 541. [Abstract] [Full Text] [PDF]

				J. Antony, K. Kellershohn, M. Mohr-Andra, A. Kebig, S. Prilla, M. Muth, E. Heller, T. Disingrini, C. Dallanoce, S. Bertoni, et al. Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity FASEB J, February 1, 2009; 23(2): 442 - 450. [Abstract] [Full Text] [PDF]

				D. Mustafi and K. Palczewski Topology of Class A G Protein-Coupled Receptors: Insights Gained from Crystal Structures of Rhodopsins, Adrenergic and Adenosine Receptors Mol. Pharmacol., January 1, 2009; 75(1): 1 - 12. [Abstract] [Full Text] [PDF]

				Y. Pei, S. C. Rogan, F. Yan, and B. L. Roth Engineered GPCRs as Tools to Modulate Signal Transduction Physiology, December 1, 2008; 23(6): 313 - 321. [Abstract] [Full Text] [PDF]

				M. J. S. Chee, K. Morl, D. Lindner, N. Merten, G. W. Zamponi, P. E. Light, A. G. Beck-Sickinger, and W. F. Colmers The Third Intracellular Loop Stabilizes the Inactive State of the Neuropeptide Y1 Receptor J. Biol. Chem., November 28, 2008; 283(48): 33337 - 33346. [Abstract] [Full Text] [PDF]

				J. A. Tello, S. Wu, J. E. Rivier, and N. M. Sherwood Four functional GnRH receptors in zebrafish: analysis of structure, signaling, synteny and phylogeny Integr. Comp. Biol., November 1, 2008; 48(5): 570 - 587. [Abstract] [Full Text] [PDF]

				T. R. Mahoney, S. Luo, E. K. Round, M. Brauner, A. Gottschalk, J. H. Thomas, and M. L. Nonet Intestinal signaling to GABAergic neurons regulates a rhythmic behavior in Caenorhabditis elegans PNAS, October 21, 2008; 105(42): 16350 - 16355. [Abstract] [Full Text] [PDF]

				J. Royer, A. Lefevre-Minisini, G. Caltabiano, T. Lacombe, Y. Malthiery, F. Savagner, L. Pardo, and P. Rodien The Cloned Equine Thyrotropin Receptor Is Hypersensitive to Human Chorionic Gonadotropin; Identification of Three Residues in the Extracellular Domain Involved in Ligand Specificity Endocrinology, October 1, 2008; 149(10): 5088 - 5096. [Abstract] [Full Text] [PDF]

				L. Jacob and J.-P. Vert Protein-ligand interaction prediction: an improved chemogenomics approach Bioinformatics, October 1, 2008; 24(19): 2149 - 2156. [Abstract] [Full Text] [PDF]

				T. Voisin, A. El Firar, C. Rouyer-Fessard, V. Gratio, and M. Laburthe A hallmark of immunoreceptor, the tyrosine-based inhibitory motif ITIM, is present in the G protein-coupled receptor OX1R for orexins and drives apoptosis: a novel mechanism FASEB J, June 1, 2008; 22(6): 1993 - 2002. [Abstract] [Full Text] [PDF]

				A. Gupta, R. Rozenfeld, I. Gomes, K. M. Raehal, F. M. Decaillot, L. M. Bohn, and L. A. Devi Post-activation-mediated Changes in Opioid Receptors Detected by N-terminal Antibodies J. Biol. Chem., April 18, 2008; 283(16): 10735 - 10744. [Abstract] [Full Text] [PDF]

				S. Ikeda, K. Nakamura, K. Kogure, Y. Omori, S. Yamashita, K. Kubota, T. Mizutani, K. Miyamoto, and T. Minegishi Effect of Estrogen on the Expression of Luteinizing Hormone-Human Chorionic Gonadotropin Receptor Messenger Ribonucleic Acid in Cultured Rat Granulosa Cells Endocrinology, April 1, 2008; 149(4): 1524 - 1533. [Abstract] [Full Text] [PDF]

				E. Stafflinger, K. K. Hansen, F. Hauser, M. Schneider, G. Cazzamali, M. Williamson, and C. J. P. Grimmelikhuijzen Cloning and identification of an oxytocin/vasopressin-like receptor and its ligand from insects PNAS, March 4, 2008; 105(9): 3262 - 3267. [Abstract] [Full Text] [PDF]

				E. C. Hsiao, B. M. Boudignon, W. C. Chang, M. Bencsik, J. Peng, T. D. Nguyen, C. Manalac, B. P. Halloran, B. R. Conklin, and R. A. Nissenson From the Cover: Osteoblast expression of an engineered Gs-coupled receptor dramatically increases bone mass PNAS, January 29, 2008; 105(4): 1209 - 1214. [Abstract] [Full Text] [PDF]

				N. Spitzer, D. H. Edwards, and D. J. Baro Conservation of structure, signaling and pharmacology between two serotonin receptor subtypes from decapod crustaceans, Panulirus interruptus and Procambarus clarkii J. Exp. Biol., January 1, 2008; 211(1): 92 - 105. [Abstract] [Full Text] [PDF]

				K. Angelova, F. Fanelli, and D. Puett Contributions of Intracellular Loops 2 and 3 of the Lutropin Receptor in Gs Coupling Mol. Endocrinol., January 1, 2008; 22(1): 126 - 138. [Abstract] [Full Text] [PDF]

				D. Jager, C. Schmalenbach, S. Prilla, J. Schrobang, A. Kebig, M. Sennwitz, E. Heller, C. Trankle, U. Holzgrabe, H.-D. Holtje, et al. Allosteric Small Molecules Unveil a Role of an Extracellular E2/Transmembrane Helix 7 Junction for G Protein-coupled Receptor Activation J. Biol. Chem., November 30, 2007; 282(48): 34968 - 34976. [Abstract] [Full Text] [PDF]

				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. High-Resolution Crystal Structure of an Engineered Human 2-Adrenergic G Protein Coupled Receptor Science, November 23, 2007; 318(5854): 1258 - 1265. [Abstract] [Full Text] [PDF]

				K. H. Sze, H. Zhou, Y. Yang, M. He, Y. Jiang, and A. O. L. Wong Pituitary Adenylate Cyclase-Activating Polypeptide (PACAP) as a Growth Hormone (GH)-Releasing Factor in Grass Carp: II. Solution Structure of a Brain-Specific PACAP by Nuclear Magnetic Resonance Spectroscopy and Functional Studies on GH Release and Gene Expression Endocrinology, October 1, 2007; 148(10): 5042 - 5059. [Abstract] [Full Text] [PDF]

				L. C. Moeller, M. Alonso, X. Liao, V. Broach, A. Dumitrescu, J. Van Sande, L. Montanelli, S. Skjei, C. Goodwin, H. Grasberger, et al. Pituitary-Thyroid Setpoint and Thyrotropin Receptor Expression in Consomic Rats Endocrinology, October 1, 2007; 148(10): 4727 - 4733. [Abstract] [Full Text] [PDF]

				E. Marco, M. Foucaud, I. Langer, C. Escrieut, I. G. Tikhonova, and D. Fourmy Mechanism of Activation of a G Protein-coupled Receptor, the Human Cholecystokinin-2 Receptor J. Biol. Chem., September 28, 2007; 282(39): 28779 - 28790. [Abstract] [Full Text] [PDF]

				J. H. Li, S.-J. Han, F. F. Hamdan, S.-K. Kim, K. A. Jacobson, L. M. Bloodworth, X. Zhang, and J. Wess Distinct Structural Changes in a G Protein-coupled Receptor Caused by Different Classes of Agonist Ligands J. Biol. Chem., September 7, 2007; 282(36): 26284 - 26293. [Abstract] [Full Text] [PDF]

				E. L. Sharp, H. E. Farrell, K. Borchers, E. C. Holmes, and N. J. Davis-Poynter Sequence analysis of the equid herpesvirus 2 chemokine receptor homologues E1, ORF74 and E6 demonstrates high sequence divergence between field isolates J. Gen. Virol., September 1, 2007; 88(9): 2450 - 2462. [Abstract] [Full Text] [PDF]

				V. A. Avlani, K. J. Gregory, C. J. Morton, M. W. Parker, P. M. Sexton, and A. Christopoulos Critical Role for the Second Extracellular Loop in the Binding of Both Orthosteric and Allosteric G Protein-coupled Receptor Ligands J. Biol. Chem., August 31, 2007; 282(35): 25677 - 25686. [Abstract] [Full Text] [PDF]

				C. S. Lisenbee, K. G. Harikumar, and L. J. Miller Mapping the Architecture of Secretin Receptors with Intramolecular Fluorescence Resonance Energy Transfer Using Acousto-Optic Tunable Filter-Based Spectral Imaging Mol. Endocrinol., August 1, 2007; 21(8): 1997 - 2008. [Abstract] [Full Text] [PDF]

				S. Roy, S. Setlur, R. A. Gadkari, H. N. Krishnamurthy, and R. R. Dighe Translational Fusion of Two {beta}-Subunits of Human Chorionic Gonadotropin Results in Production of a Novel Antagonist of the Hormone Endocrinology, August 1, 2007; 148(8): 3977 - 3986. [Abstract] [Full Text] [PDF]

				H. Grasberger, J. Van Sande, A. Hag-Dahood Mahameed, Y. Tenenbaum-Rakover, and S. Refetoff A Familial Thyrotropin (TSH) Receptor Mutation Provides in Vivo Evidence that the Inositol Phosphates/Ca2+ Cascade Mediates TSH Action on Thyroid Hormone Synthesis J. Clin. Endocrinol. Metab., July 1, 2007; 92(7): 2816 - 2820. [Abstract] [Full Text] [PDF]

				K. Shiraishi and M. Ascoli Lutropin/Choriogonadotropin Stimulate the Proliferation of Primary Cultures of Rat Leydig Cells through a Pathway that Involves Activation of the Extracellularly Regulated Kinase 1/2 Cascade Endocrinology, July 1, 2007; 148(7): 3214 - 3225. [Abstract] [Full Text] [PDF]

				E. L. Maillet, N. Pellegrini, C. Valant, B. Bucher, M. Hibert, J.-J. Bourguignon, and J.-L. Galzi A novel, conformation-specific allosteric inhibitor of the tachykinin NK2 receptor (NK2R) with functionally selective properties FASEB J, July 1, 2007; 21(9): 2124 - 2134. [Abstract] [Full Text] [PDF]

				V. Binet, B. Duthey, J. Lecaillon, C. Vol, J. Quoyer, G. Labesse, J.-P. Pin, and L. Prezeau Common Structural Requirements for Heptahelical Domain Function in Class A and Class C G Protein-coupled Receptors J. Biol. Chem., April 20, 2007; 282(16): 12154 - 12163. [Abstract] [Full Text] [PDF]

				M. Hauser, S. Kauffman, B.-K. Lee, F. Naider, and J. M. Becker The First Extracellular Loop of the Saccharomyces cerevisiae G Protein-coupled Receptor Ste2p Undergoes a Conformational Change upon Ligand Binding J. Biol. Chem., April 6, 2007; 282(14): 10387 - 10397. [Abstract] [Full Text] [PDF]

				L. Oliveira, C. M. Costa-Neto, C. R. Nakaie, S. Schreier, S. I. Shimuta, and A. C. M. Paiva The Angiotensin II AT1 Receptor Structure-Activity Correlations in the Light of Rhodopsin Structure Physiol Rev, April 1, 2007; 87(2): 565 - 592. [Abstract] [Full Text] [PDF]

				M. A. Al-Fulaij, Y. Ren, M. Beinborn, and A. S. Kopin Identification of Amino Acid Determinants of Dopamine 2 Receptor Synthetic Agonist Function J. Pharmacol. Exp. Ther., April 1, 2007; 321(1): 298 - 307. [Abstract] [Full Text] [PDF]

				M. Zhong, B. Parish, D. A. Murtazina, C.-Y. Ku, and B. M. Sanborn Amino acids in the COOH-terminal region of the oxytocin receptor third intracellular domain are important for receptor function Am J Physiol Endocrinol Metab, April 1, 2007; 292(4): E977 - E984. [Abstract] [Full Text] [PDF]

				S. Basu, V. R. Jala, S. Mathis, S. T. Rajagopal, A. Del Prete, P. Maturu, J. O. Trent, and B. Haribabu Critical Role for Polar Residues in Coupling Leukotriene B4 Binding to Signal Transduction in BLT1 J. Biol. Chem., March 30, 2007; 282(13): 10005 - 10017. [Abstract] [Full Text] [PDF]

				N. Makita, J. Sato, K. Manaka, Y. Shoji, A. Oishi, M. Hashimoto, T. Fujita, and T. Iiri An acquired hypocalciuric hypercalcemia autoantibody induces allosteric transition among active human Ca-sensing receptor conformations PNAS, March 27, 2007; 104(13): 5443 - 5448. [Abstract] [Full Text] [PDF]

				M. Scarselli, B. Li, S.-K. Kim, and J. Wess Multiple Residues in the Second Extracellular Loop Are Critical for M3 Muscarinic Acetylcholine Receptor Activation J. Biol. Chem., March 9, 2007; 282(10): 7385 - 7396. [Abstract] [Full Text] [PDF]

				Y. Tenenbaum-Rakover, M. Commenges-Ducos, A. Iovane, C. Aumas, O. Admoni, and N. de Roux Neuroendocrine Phenotype Analysis in Five Patients with Isolated Hypogonadotropic Hypogonadism due to a L102P Inactivating Mutation of GPR54 J. Clin. Endocrinol. Metab., March 1, 2007; 92(3): 1137 - 1144. [Abstract] [Full Text] [PDF]

				A. Gupta, F. M. Decaillot, I. Gomes, O. Tkalych, A. S. Heimann, E. S. Ferro, and L. A. Devi Conformation State-sensitive Antibodies to G-protein-coupled Receptors J. Biol. Chem., February 23, 2007; 282(8): 5116 - 5124. [Abstract] [Full Text] [PDF]

				T. Ikemoto and M. K. Park Comparative analysis of the pituitary and ovarian GnRH systems in the leopard gecko: signaling crosstalk between multiple receptor subtypes in ovarian follicles J. Mol. Endocrinol., February 1, 2007; 38(2): 289 - 304. [Abstract] [Full Text] [PDF]

				S. Choi, M. Lee, A. L. Shiu, S. J. Yo, and G. W. Aponte Identification of a protein hydrolysate responsive G protein-coupled receptor in enterocytes Am J Physiol Gastrointest Liver Physiol, January 1, 2007; 292(1): G98 - G112. [Abstract] [Full Text] [PDF]

				H. W. Tedford and G. W. Zamponi Direct G Protein Modulation of Cav2 Calcium Channels Pharmacol. Rev., December 1, 2006; 58(4): 837 - 862. [Abstract] [Full Text] [PDF]

				I. S. Hagemann, K. D. Narzinski, D. H. Floyd, and T. J. Baranski Random Mutagenesis of the Complement Factor 5a (C5a) Receptor N Terminus Provides a Structural Constraint for C5a Docking J. Biol. Chem., December 1, 2006; 281(48): 36783 - 36792. [Abstract] [Full Text] [PDF]

				T. A. Spalding, J.-N. Ma, T. R. Ott, M. Friberg, A. Bajpai, S. R. Bradley, R. E. Davis, M. R. Brann, and E. S. Burstein Structural Requirements of Transmembrane Domain 3 for Activation by the M1 Muscarinic Receptor Agonists AC-42, AC-260584, Clozapine, and N-Desmethylclozapine: Evidence for Three Distinct Modes of Receptor Activation Mol. Pharmacol., December 1, 2006; 70(6): 1974 - 1983. [Abstract] [Full Text] [PDF]

				M. R. Paillasse, C. Deraeve, P. de Medina, L. Mhamdi, G. Favre, M. Poirot, and S. Silvente-Poirot Insights into the Cholecystokinin 2 Receptor Binding Site and Processes of Activation Mol. Pharmacol., December 1, 2006; 70(6): 1935 - 1945. [Abstract] [Full Text] [PDF]

				M. Chachisvilis, Y.-L. Zhang, and J. A. Frangos G protein-coupled receptors sense fluid shear stress in endothelial cells PNAS, October 17, 2006; 103(42): 15463 - 15468. [Abstract] [Full Text] [PDF]

				R. S. Mukherjee, E. W. McBride, M. Beinborn, K. Dunlap, and A. S. Kopin Point Mutations in Either Subunit of the GABAB Receptor Confer Constitutive Activity to the Heterodimer Mol. Pharmacol., October 1, 2006; 70(4): 1406 - 1413. [Abstract] [Full Text] [PDF]

				F. T. Khasawneh, J.-S. Huang, J. W. Turek, and G. C. L. Breton Differential Mapping of the Amino Acids Mediating Agonist and Antagonist Coordination with the Human Thromboxane A2 Receptor Protein J. Biol. Chem., September 15, 2006; 281(37): 26951 - 26965. [Abstract] [Full Text] [PDF]

				J. Van Durme, F. Horn, S. Costagliola, G. Vriend, and G. Vassart GRIS: Glycoprotein-Hormone Receptor Information System Mol. Endocrinol., September 1, 2006; 20(9): 2247 - 2255. [Abstract] [Full Text] [PDF]

				H. Nakamichi and T. Okada Local peptide movement in the photoreaction intermediate of rhodopsin PNAS, August 22, 2006; 103(34): 12729 - 12734. [Abstract] [Full Text] [PDF]

				M. Beinborn Class B GPCRs: A Hidden Agonist Within? Mol. Pharmacol., July 1, 2006; 70(1): 1 - 4. [Abstract] [Full Text] [PDF]

				C. E. Elling, T. M. Frimurer, L.-O. Gerlach, R. Jorgensen, B. Holst, and T. W. Schwartz Metal Ion Site Engineering Indicates a Global Toggle Switch Model for Seven-transmembrane Receptor Activation J. Biol. Chem., June 23, 2006; 281(25): 17337 - 17346. [Abstract] [Full Text] [PDF]

				J.-Y. Springael, P. N. Le Minh, E. Urizar, S. Costagliola, G. Vassart, and M. Parmentier Allosteric Modulation of Binding Properties between Units of Chemokine Receptor Homo- and Hetero-Oligomers Mol. Pharmacol., May 1, 2006; 69(5): 1652 - 1661. [Abstract] [Full Text] [PDF]

				A. M. Navratil, T. A. Farmerie, J. Bogerd, T. M. Nett, and C. M. Clay Differential Impact of Intracellular Carboxyl Terminal Domains on Lipid Raft Localization of the Murine Gonadotropin-Releasing Hormone Receptor Biol Reprod, May 1, 2006; 74(5): 788 - 797. [Abstract] [Full Text] [PDF]

				J. M. Klco, G. V. Nikiforovich, and T. J. Baranski Genetic Analysis of the First and Third Extracellular Loops of the C5a Receptor Reveals an Essential WXFG Motif in the First Loop J. Biol. Chem., April 28, 2006; 281(17): 12010 - 12019. [Abstract] [Full Text] [PDF]

				F. J. Troost, R.-J. M. Brummer, G. R. M. M. Haenen, A. Bast, R. I. van Haaften, C. T. Evelo, and W. H. M. Saris Gene expression in human small intestinal mucosa in vivo is mediated by iron-induced oxidative stress Physiol Genomics, April 11, 2006; 25(2): 242 - 249. [Abstract] [Full Text] [PDF]

				F. J. Troost, R.-J. M. Brummer, G. R. M. M. Haenen, A. Bast, R. I. van Haaften, C. T. Evelo, and W. H. M. Saris Gene expression in human small intestinal mucosa in vivo is mediated by iron-induced oxidative stress Physiol Genomics, April 11, 2006; 25(2): 242 - 249. [Abstract] [Full Text] [PDF]

				U. Ringkananont, J. Van Durme, L. Montanelli, F. Ugrasbul, Y. M. Yu, R. E. Weiss, S. Refetoff, and H. Grasberger Repulsive Separation of the Cytoplasmic Ends of Transmembrane Helices 3 and 6 Is Linked to Receptor Activation in a Novel Thyrotropin Receptor Mutant (M626I) Mol. Endocrinol., April 1, 2006; 20(4): 893 - 903. [Abstract] [Full Text] [PDF]

				A. Grossfield, S. E. Feller, and M. C. Pitman A role for direct interactions in the modulation of rhodopsin by {omega}-3 polyunsaturated lipids PNAS, March 28, 2006; 103(13): 4888 - 4893. [Abstract] [Full Text] [PDF]

				M. J. Mahon, T. M. Bonacci, P. Divieti, and A. V. Smrcka A Docking Site for G Protein {beta}{gamma} Subunits on the Parathyroid Hormone 1 Receptor Supports Signaling through Multiple Pathways Mol. Endocrinol., January 1, 2006; 20(1): 136 - 146. [Abstract] [Full Text] [PDF]

				W. Guo, L. Shi, M. Filizola, H. Weinstein, and J. A. Javitch From The Cover: Crosstalk in G protein-coupled receptors: Changes at the transmembrane homodimer interface determine activation PNAS, November 29, 2005; 102(48): 17495 - 17500. [Abstract] [Full Text] [PDF]

				N. G. Sgourakis, P. G. Bagos, and S. J. Hamodrakas Prediction of the coupling specificity of GPCRs to four families of G-proteins using hidden Markov models and artificial neural networks Bioinformatics, November 15, 2005; 21(22): 4101 - 4106. [Abstract] [Full Text] [PDF]

				S. Tunaru, J. Lattig, J. Kero, G. Krause, and S. Offermanns Characterization of Determinants of Ligand Binding to the Nicotinic Acid Receptor GPR109A (HM74A/PUMA-G) Mol. Pharmacol., November 1, 2005; 68(5): 1271 - 1280. [Abstract] [Full Text] [PDF]

				S.-J. Han, F. F. Hamdan, S.-K. Kim, K. A. Jacobson, L. M. Bloodworth, B. Li, and J. Wess Identification of an Agonist-induced Conformational Change Occurring Adjacent to the Ligand-binding Pocket of the M3 Muscarinic Acetylcholine Receptor J. Biol. Chem., October 14, 2005; 280(41): 34849 - 34858. [Abstract] [Full Text] [PDF]

				N. Wettschureck and S. Offermanns Mammalian G Proteins and Their Cell Type Specific Functions Physiol Rev, October 1, 2005; 85(4): 1159 - 1204. [Abstract] [Full Text] [PDF]

				R. I. W. Osmond, A. Sheehan, R. Borowicz, E. Barnett, G. Harvey, C. Turner, A. Brown, M. F. Crouch, and A. R. Dyer GPCR Screening via ERK 1/2: A Novel Platform for Screening G Protein-Coupled Receptors J Biomol Screen, October 1, 2005; 10(7): 730 - 737. [Abstract] [PDF]

				F. X. Donadeu and M. Ascoli The Differential Effects of the Gonadotropin Receptors on Aromatase Expression in Primary Cultures of Immature Rat Granulosa Cells Are Highly Dependent on the Density of Receptors Expressed and the Activation of the Inositol Phosphate Cascade Endocrinology, September 1, 2005; 146(9): 3907 - 3916. [Abstract] [Full Text] [PDF]

				Z.-L. Lu, R. Gallagher, R. Sellar, M. Coetsee, and R. P. Millar Mutations Remote from the Human Gonadotropin-releasing Hormone (GnRH) Receptor-binding Sites Specifically Increase Binding Affinity for GnRH II but Not GnRH I: EVIDENCE FOR LIGAND-SELECTIVE, RECEPTOR-ACTIVE CONFORMATIONS J. Biol. Chem., August 19, 2005; 280(33): 29796 - 29803. [Abstract] [Full Text] [PDF]

				S. Shacham, M. N. Cheifetz, M. Fridkin, A. J. Pawson, R. P. Millar, and Z. Naor Identification of Ser153 in ICL2 of the Gonadotropin-releasing Hormone (GnRH) Receptor as a Phosphorylation-independent Site for Inhibition of Gq Coupling J. Biol. Chem., August 12, 2005; 280(32): 28981 - 28988. [Abstract] [Full Text] [PDF]

				V. Pham, M. Dong, J. D. Wade, L. J. Miller, C. J. Morton, H.-l. Ng, M. W. Parker, and P. M. Sexton Insights into Interactions between the {alpha}-Helical Region of the Salmon Calcitonin Antagonists and the Human Calcitonin Receptor using Photoaffinity Labeling J. Biol. Chem., August 5, 2005; 280(31): 28610 - 28622. [Abstract] [Full Text] [PDF]

				B. Karges, G. Krause, J. Homoki, K.-M. Debatin, N. de Roux, and W. Karges TSH receptor mutation V509A causes familial hyperthyroidism by release of interhelical constraints between transmembrane helices TMH3 and TMH5 J. Endocrinol., August 1, 2005; 186(2): 377 - 385. [Abstract] [Full Text] [PDF]

				S.-J. Han, F. F. Hamdan, S.-K. Kim, K. A. Jacobson, L. Brichta, L. M. Bloodworth, J. H. Li, and J. Wess Pronounced Conformational Changes following Agonist Activation of the M3 Muscarinic Acetylcholine Receptor J. Biol. Chem., July 1, 2005; 280(26): 24870 - 24879. [Abstract] [Full Text] [PDF]

				J.-L. Baneres, D. Mesnier, A. Martin, L. Joubert, A. Dumuis, and J. Bockaert Molecular Characterization of a Purified 5-HT4 Receptor: A STRUCTURAL BASIS FOR DRUG EFFICACY J. Biol. Chem., May 27, 2005; 280(21): 20253 - 20260. [Abstract] [Full Text] [PDF]

				H. Tsukamoto, A. Terakita, and Y. Shichida A rhodopsin exhibiting binding ability to agonist all-trans-retinal PNAS, May 3, 2005; 102(18): 6303 - 6308. [Abstract] [Full Text] [PDF]

				S. Paoletti, V. Petkovic, S. Sebastiani, M. G. Danelon, M. Uguccioni, and B. O. Gerber A rich chemokine environment strongly enhances leukocyte migration and activities Blood, May 1, 2005; 105(9): 3405 - 3412. [Abstract] [Full Text] [PDF]

				E. Archer-Lahlou, C. Escrieut, P. Clerc, J. Martinez, L. Moroder, C. Logsdon, A. Kopin, C. Seva, M. Dufresne, L. Pradayrol, et al. Molecular Mechanism Underlying Partial and Full Agonism Mediated by the Human Cholecystokinin-1 Receptor J. Biol. Chem., March 18, 2005; 280(11): 10664 - 10674. [Abstract] [Full Text] [PDF]

				R. Jorgensen, L. Martini, T. W. Schwartz, and C. E. Elling Characterization of Glucagon-Like Peptide-1 Receptor {beta}-Arrestin 2 Interaction: A High-Affinity Receptor Phenotype Mol. Endocrinol., March 1, 2005; 19(3): 812 - 823. [Abstract] [Full Text] [PDF]

				E. Buck and J. A. Wells Disulfide trapping to localize small-molecule agonists and antagonists for a G protein-coupled receptor PNAS, February 22, 2005; 102(8): 2719 - 2724. [Abstract] [Full Text] [PDF]

				B. Li, N. M. Nowak, S.-K. Kim, K. A. Jacobson, A. Bagheri, C. Schmidt, and J. Wess Random Mutagenesis of the M3 Muscarinic Acetylcholine Receptor Expressed in Yeast: IDENTIFICATION OF SECOND-SITE MUTATIONS THAT RESTORE FUNCTION TO A COUPLING-DEFICIENT MUTANT M3 RECEPTOR J. Biol. Chem., February 18, 2005; 280(7): 5664 - 5675. [Abstract] [Full Text] [PDF]

				E. Buck, H. Bourne, and J. A. Wells Site-specific Disulfide Capture of Agonist and Antagonist Peptides on the C5a Receptor J. Biol. Chem., February 11, 2005; 280(6): 4009 - 4012. [Abstract] [Full Text] [PDF]

				J. Martinez-Pinna, I. S. Gurung, C. Vial, C. Leon, C. Gachet, R. J. Evans, and M. P. Mahaut-Smith Direct Voltage Control of Signaling via P2Y1 and Other G{alpha}q-coupled Receptors J. Biol. Chem., January 14, 2005; 280(2): 1490 - 1498. [Abstract] [Full Text] [PDF]

				A. C. Conner, D. L. Hay, J. Simms, S. G. Howitt, M. Schindler, D. M. Smith, M. Wheatley, and D. R. Poyner A Key Role for Transmembrane Prolines in Calcitonin Receptor-Like Receptor Agonist Binding and Signalling: Implications for Family B G-Protein-Coupled Receptors Mol. Pharmacol., January 1, 2005; 67(1): 20 - 31. [Abstract] [Full Text] [PDF]

				S. Neumann, G. Krause, M. Claus, and R. Paschke Structural Determinants for G Protein Activation and Selectivity in the Second Intracellular Loop of the Thyrotropin Receptor Endocrinology, January 1, 2005; 146(1): 477 - 485. [Abstract] [Full Text] [PDF]

				B. Jastrzebska, T. Maeda, L. Zhu, D. Fotiadis, S. Filipek, A. Engel, R. E. Stenkamp, and K. Palczewski Functional Characterization of Rhodopsin Monomers and Dimers in Detergents J. Biol. Chem., December 24, 2004; 279(52): 54663 - 54675. [Abstract] [Full Text] [PDF]

				B. Holst, N. D. Holliday, A. Bach, C. E. Elling, H. M. Cox, and T. W. Schwartz Common Structural Basis for Constitutive Activity of the Ghrelin Receptor Family J. Biol. Chem., December 17, 2004; 279(51): 53806 - 53817. [Abstract] [Full Text] [PDF]

				S. Granier, S. Terrillon, R. Pascal, H. Demene, M. Bouvier, G. Guillon, and C. Mendre A Cyclic Peptide Mimicking the Third Intracellular Loop of the V2 Vasopressin Receptor Inhibits Signaling through Its Interaction with Receptor Dimer and G Protein J. Biol. Chem., December 3, 2004; 279(49): 50904 - 50914. [Abstract] [Full Text] [PDF]

				S. S. Martin, A. A. Boucard, M. Clement, E. Escher, R. Leduc, and G. Guillemette Analysis of the Third Transmembrane Domain of the Human Type 1 Angiotensin II Receptor by Cysteine Scanning Mutagenesis J. Biol. Chem., December 3, 2004; 279(49): 51415 - 51423. [Abstract] [Full Text] [PDF]

				Y. Liang, D. Fotiadis, T. Maeda, A. Maeda, A. Modzelewska, S. Filipek, D. A. Saperstein, A. Engel, and K. Palczewski Rhodopsin Signaling and Organization in Heterozygote Rhodopsin Knockout Mice J. Biol. Chem., November 12, 2004; 279(46): 48189 - 48196. [Abstract] [Full Text] [PDF]

				J. A. Javitch The Ants Go Marching Two by Two: Oligomeric Structure of G-Protein-Coupled Receptors Mol. Pharmacol., November 1, 2004; 66(5): 1077 - 1082. [Abstract] [Full Text] [PDF]

				V. Capra, A. Veltri, C. Foglia, L. Crimaldi, A. Habib, M. Parenti, and G. E. Rovati Mutational Analysis of the Highly Conserved ERY Motif of the Thromboxane A2 Receptor: Alternative Role in G Protein-Coupled Receptor Signaling Mol. Pharmacol., October 1, 2004; 66(4): 880 - 889. [Abstract] [Full Text] [PDF]

				G. J. Reinhart, Q. Xie, X.-J. Liu, Y.-F. Zhu, J. Fan, C. Chen, and R. S. Struthers Species Selectivity of Nonpeptide Antagonists of the Gonadotropinreleasing Hormone Receptor Is Determined by Residues in Extracellular Loops II and III and the Amino Terminus J. Biol. Chem., August 13, 2004; 279(33): 34115 - 34122. [Abstract] [Full Text] [PDF]