Uncovering Molecular Mechanisms Involved in Activation of G Protein-Coupled Receptors
Ulrik Gether1
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 (GPCRsor 7TM
receptors), with more than 1000 different members, comprisethe largest
superfamily of proteins in the body. Since the cloningof the first
receptors more than a decade ago, extensive experimentalwork has
uncovered multiple aspects of their function and challengedmany
traditional paradigms. However, it is only recently thatwe are
beginning to gain insight into some of the most fundamentalquestions
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 toshare a
similar overall tertiary structure? What is the natureof the physical
changes linking agonist binding to receptoractivation and subsequent
transduction of the signal to theassociated G protein on the
cytoplasmic side of the membraneand to other putative signaling
pathways? The goal of the presentreview is to specifically address
these questions as well asto depict the current awareness about GPCR
structure-functionrelationships in general.
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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
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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
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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
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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
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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
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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
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H. Tsukamoto, A. Terakita, and Y. Shichida A rhodopsin exhibiting binding ability to agonist all-trans-retinal
PNAS,
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[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,
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[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
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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
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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;
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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
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E. Buck, H. Bourne, and J. A. Wells Site-specific Disulfide Capture of Agonist and Antagonist Peptides on the C5a Receptor
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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
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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
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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
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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
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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
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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
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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
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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
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J. A. Javitch The Ants Go Marching Two by Two: Oligomeric Structure of G-Protein-Coupled Receptors
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