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Department of Neuroscience, Uppsala University, Uppsala, Sweden (R.F., M.C.L., L.-G.L., H.B.S.); and Department of Animal Breeding and Genetics, Swedish University of Agricultural Sciences, Uppsala, Sweden (R.F.)
The superfamily of G-protein-coupled receptors (GPCRs) is very diverse in structure and function and its members are among the most pursued targets for drug development. We identified more than 800 human GPCR sequences and simultaneously analyzed 342 unique functional nonolfactory human GPCR sequences with phylogenetic analyses. Our results show, with high bootstrap support, five main families, named glutamate, rhodopsin, adhesion, frizzled/taste2, and secretin, forming the GRAFS classification system. The rhodopsin family is the largest and forms four main groups with 13 sub-branches. Positions of the GPCRs in chromosomal paralogons regions indicate the importance of tetraploidizations or local gene duplication events for their creation. We also searched for "fingerprint" motifs using Hidden Markov Models delineating the putative inter-relationship of the GRAFS families. We show several common structural features indicating that the human GPCRs in the GRAFS families share a common ancestor. This study represents the first overall map of the GPCRs in a single mammalian genome. Our novel approach of analyzing such large and diverse sequence sets may be useful for studies on GPCRs in other genomes and divergent protein families.
Received December 23, 2002; accepted March 11, 2003.
Address correspondence to: Helgi B. Schiöth, Department of Neuroscience, Biomedical Center, Box 593, 75 124 Uppsala, Sweden. E-mail: helgis{at}bmc.uu.se
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L. M. F. Leeb-Lundberg, F. Marceau, W. Muller-Esterl, D. J. Pettibone, and B. L. Zuraw International Union of Pharmacology. XLV. Classification of the Kinin Receptor Family: from Molecular Mechanisms to Pathophysiological Consequences Pharmacol. Rev., March 1, 2005; 57(1): 27 - 77. [Abstract] [Full Text] [PDF] |
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B. N. Armbruster and B. L. Roth Mining the Receptorome J. Biol. Chem., February 18, 2005; 280(7): 5129 - 5132. [Full Text] [PDF] |
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T. Mustafa, A. Eckert, T. Klonisch, A. Kehlen, P. Maurer, M. Klintschar, M. Erhuma, R. Zschoyan, O. Gimm, H. Dralle, et al. Expression of the Epidermal Growth Factor Seven-Transmembrane Member CD97 Correlates with Grading and Staging in Human Oral Squamous Cell Carcinomas Cancer Epidemiol. Biomarkers Prev., January 1, 2005; 14(1): 108 - 119. [Abstract] [Full Text] [PDF] |
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M. J. Kwakkenbos, W. Pouwels, M. Matmati, M. Stacey, H.-H. Lin, S. Gordon, R. A. W. van Lier, and J. Hamann Expression of the largest CD97 and EMR2 isoforms on leukocytes facilitates a specific interaction with chondroitin sulfate on B cells J. Leukoc. Biol., January 1, 2005; 77(1): 112 - 119. [Abstract] [Full Text] [PDF] |
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C. J. Dixon, J. F. Hall, T. E. Webb, and M. R. Boarder Regulation of Rat Hepatocyte Function by P2Y Receptors: Focus on Control of Glycogen Phosphorylase and Cyclic AMP by 2-Methylthioadenosine 5'-Diphosphate J. Pharmacol. Exp. Ther., October 1, 2004; 311(1): 334 - 341. [Abstract] [Full Text] [PDF] |
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C. Lefevre, B. Bouadjar, A. Karaduman, F. Jobard, S. Saker, M. Ozguc, M. Lathrop, J.-F. Prud'homme, and J. Fischer Mutations in ichthyin a new gene on chromosome 5q33 in a new form of autosomal recessive congenital ichthyosis Hum. Mol. Genet., October 1, 2004; 13(20): 2473 - 2482. [Abstract] [Full Text] [PDF] |
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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] |
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D. Ramsay, I. C. Carr, J. Pediani, J. F. Lopez-Gimenez, R. Thurlow, M. Fidock, and G. Milligan High-Affinity Interactions between Human {alpha}1A-Adrenoceptor C-Terminal Splice Variants Produce Homo- and Heterodimers but Do Not Generate the {alpha}1L-Adrenoceptor Mol. Pharmacol., August 1, 2004; 66(2): 228 - 239. [Abstract] [Full Text] [PDF] |
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I. Kalatskaya, S. Schussler, A. Blaukat, W. Muller-Esterl, M. Jochum, D. Proud, and A. Faussner Mutation of Tyrosine in the Conserved NPXXY Sequence Leads to Constitutive Phosphorylation and Internalization, but Not Signaling, of the Human B2 Bradykinin Receptor J. Biol. Chem., July 23, 2004; 279(30): 31268 - 31276. [Abstract] [Full Text] [PDF] |
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G. Milligan G Protein-Coupled Receptor Dimerization: Function and Ligand Pharmacology Mol. Pharmacol., July 1, 2004; 66(1): 1 - 7. [Abstract] [Full Text] [PDF] |
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S. Takeda, T. Okada, M. Okamura, T. Haga, J. Isoyama-Tanaka, H. Kuwahara, and N. Minamino The Receptor-G{alpha} Fusion Protein as a Tool for Ligand Screening: a Model Study Using a Nociceptin Receptor-G{alpha}i2 Fusion Protein J. Biochem., May 1, 2004; 135(5): 597 - 604. [Abstract] [Full Text] [PDF] |
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S. L. Kirstein and P. A. Insel Autonomic Nervous System Pharmacogenomics: A Progress Report Pharmacol. Rev., March 1, 2004; 56(1): 31 - 52. [Abstract] [Full Text] [PDF] |
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J. Klovins, T. Haitina, D. Fridmanis, Z. Kilianova, I. Kapa, R. Fredriksson, N. Gallo-Payet, and H. B. Schioth The Melanocortin System in Fugu: Determination of POMC/AGRP/MCR Gene Repertoire and Synteny, As Well As Pharmacology and Anatomical Distribution of the MCRs Mol. Biol. Evol., March 1, 2004; 21(3): 563 - 579. [Abstract] [Full Text] [PDF] |
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J. Gupte, G. Cutler, J.-L. Chen, and H. Tian Elucidation of signaling properties of vasopressin receptor-related receptor 1 by using the chimeric receptor approach PNAS, February 10, 2004; 101(6): 1508 - 1513. [Abstract] [Full Text] [PDF] |
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J. Kniazeff, P.-P. Saintot, C. Goudet, J. Liu, A. Charnet, G. Guillon, and J.-P. Pin Locking the Dimeric GABAB G-Protein-Coupled Receptor in Its Active State J. Neurosci., January 14, 2004; 24(2): 370 - 377. [Abstract] [Full Text] [PDF] |
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C. Goudet, F. Gaven, J. Kniazeff, C. Vol, J. Liu, M. Cohen-Gonsaud, F. Acher, L. Prezeau, and J. P. Pin Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors PNAS, January 6, 2004; 101(1): 378 - 383. [Abstract] [Full Text] [PDF] |
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D. Rosskopf and K. H. Jakobs More Hints on Wnts: Gene Profiling by {beta}2-Adrenergic Receptor-Frizzled Chimeras Mol. Pharmacol., January 1, 2004; 65(1): 12 - 14. [Full Text] [PDF] |
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M. C. Lagerstrom, J. Klovins, R. Fredriksson, D. Fridmanis, T. Haitina, M. K. Ling, M. M. Berglund, and H. B. Schioth High Affinity Agonistic Metal Ion Binding Sites within the Melanocortin 4 Receptor Illustrate Conformational Change of Transmembrane Region 3 J. Biol. Chem., December 19, 2003; 278(51): 51521 - 51526. [Abstract] [Full Text] [PDF] |
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W. K. Kroeze, D. J. Sheffler, and B. L. Roth G-protein-coupled receptors at a glance J. Cell Sci., December 15, 2003; 116(24): 4867 - 4869. [Full Text] [PDF] |
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R. B. Clark and T. C. Rich Probing the Roles of Protein Kinases in G-Protein-Coupled Receptor Desensitization Mol. Pharmacol., November 1, 2003; 64(5): 1015 - 1017. [Full Text] [PDF] |
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D. Kuang, Y. Yao, M. Wang, N. Pattabiraman, L. P. Kotra, and D. R. Hampson Molecular Similarities in the Ligand Binding Pockets of an Odorant Receptor and the Metabotropic Glutamate Receptors J. Biol. Chem., October 24, 2003; 278(43): 42551 - 42559. [Abstract] [Full Text] [PDF] |
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J. J. Carrillo, J. Pediani, and G. Milligan Dimers of Class A G Protein-coupled Receptors Function via Agonist-mediated Trans-activation of Associated G Proteins J. Biol. Chem., October 24, 2003; 278(43): 42578 - 42587. [Abstract] [Full Text] [PDF] |
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D. M. Perez The Evolutionarily Triumphant G-Protein-Coupled Receptor Mol. Pharmacol., June 1, 2003; 63(6): 1202 - 1205. [Full Text] [PDF] |
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