Orphan and other 7TM receptors

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G protein-coupled receptors
Orphan and other 7TM receptors

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Subfamilies
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Overview

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This set contains 'orphan' G protein coupled receptors where the endogenous ligand(s) is not known.

Subfamilies

* Davenport AP, Alexander SP, Sharman JL, Pawson AJ, Benson HE, Monaghan AE, Liew WC, Mpamhanga CP, Bonner TI, Neubig RR et al.. (2013) International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. Pharmacol Rev, 65 (3): 967-86. [PMID:23686350]

de Gasparo M, Catt KJ, Inagami T, Wright JW, Unger T. (2000) International union of pharmacology. XXIII. The angiotensin II receptors. Pharmacol Rev, 52 (3): 415-72. [PMID:10977869]

DeSimone JA, Lyall V. (2006) Taste receptors in the gastrointestinal tract III. Salty and sour taste: sensing of sodium and protons by the tongue. Am J Physiol Gastrointest Liver Physiol, 291 (6): G1005-10. [PMID:16809639]

Ellis B, Li XC, Miguel-Qin E, Gu V, Zhuo JL. (2012) Evidence for a functional intracellular angiotensin system in the proximal tubule of the kidney. Am J Physiol Regul Integr Comp Physiol, 302 (5): R494-509. [PMID:22170616]

Foord SM, Bonner TI, Neubig RR, Rosser EM, Pin JP, Davenport AP, Spedding M, Harmar AJ. (2005) International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev, 57 (2): 279-88. [PMID:15914470]

Fredriksson R, Lagerström MC, Lundin LG, Schiöth HB. (2003) The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol Pharmacol, 63 (6): 1256-72. [PMID:12761335]

* Gilissen J, Jouret F, Pirotte B, Hanson J. (2016) Insight into SUCNR1 (GPR91) structure and function. Pharmacol Ther, 159: 56-65. [PMID:26808164]

* Insel PA, Wilderman A, Zambon AC, Snead AN, Murray F, Aroonsakool N, McDonald DS, Zhou S, McCann T, Zhang L et al.. (2015) G Protein-Coupled Receptor (GPCR) Expression in Native Cells: "Novel" endoGPCRs as Physiologic Regulators and Therapeutic Targets. Mol Pharmacol, 88 (1): 181-7. [PMID:25737495]

* Khan MZ, He L. (2017) Neuro-psychopharmacological perspective of Orphan receptors of Rhodopsin (class A) family of G protein-coupled receptors. Psychopharmacology (Berl.), 234 (8): 1181-1207. [PMID:28289782]

Kinnamon SC. (2012) Taste receptor signalling - from tongues to lungs. Acta Physiol (Oxf), 204 (2): 158-68. [PMID:21481196]

Lagerström MC, Schiöth HB. (2008) Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat Rev Drug Discov, 7 (4): 339-57. [PMID:18382464]

Maceyka M, Harikumar KB, Milstien S, Spiegel S. (2012) Sphingosine-1-phosphate signaling and its role in disease. Trends Cell Biol, 22 (1): 50-60. [PMID:22001186]

MacKenzie A. (2011) Endothelium-derived vasoactive agents, AT1 receptors and inflammation. Pharmacol Ther, 131 (2): 187-203. [PMID:21115037]

* Mackenzie AE, Milligan G. (2017) The emerging pharmacology and function of GPR35 in the nervous system. Neuropharmacology, 113 (Pt B): 661-671. [PMID:26232640]

Meyerhof W. (2005) Elucidation of mammalian bitter taste. Rev Physiol Biochem Pharmacol, 154: 37-72. [PMID:16032395]

Mutoh T, Rivera R, Chun J. (2012) Insights into the pharmacological relevance of lysophospholipid receptors. Br J Pharmacol, 165 (4): 829-44. [PMID:21838759]

* Ngo T, Kufareva I, Coleman JLj, Graham RM, Abagyan R, Smith NJ. (2016) Identifying ligands at orphan GPCRs: current status using structure-based approaches. Br J Pharmacol, 173 (20): 2934-51. [PMID:26837045]

O'Sullivan C, Dev KK. (2013) The structure and function of the S1P1 receptor. Trends Pharmacol Sci, 34 (7): 401-12. [PMID:23763867]

Overington JP, Al-Lazikani B, Hopkins AL. (2006) How many drug targets are there?. Nat Rev Drug Discov, 5 (12): 993-6. [PMID:17139284]

Patel BM, Mehta AA. (2012) Aldosterone and angiotensin: Role in diabetes and cardiovascular diseases. Eur J Pharmacol, 697 (1-3): 1-12. [PMID:23041273]

Putnam K, Shoemaker R, Yiannikouris F, Cassis LA. (2012) The renin-angiotensin system: a target of and contributor to dyslipidemias, altered glucose homeostasis, and hypertension of the metabolic syndrome. Am J Physiol Heart Circ Physiol, 302 (6): H1219-30. [PMID:22227126]

Pyne S, Pyne NJ. (2011) Translational aspects of sphingosine 1-phosphate biology. Trends Mol Med, 17 (8): 463-72. [PMID:21514226]

Renwick AG, Molinary SV. (2010) Sweet-taste receptors, low-energy sweeteners, glucose absorption and insulin release. Br J Nutr, 104 (10): 1415-20. [PMID:20619074]

Ross RA. (2009) The enigmatic pharmacology of GPR55. Trends Pharmacol Sci, 30 (3): 156-63. [PMID:19233486]

Rozengurt E. (2006) Taste receptors in the gastrointestinal tract. I. Bitter taste receptors and alpha-gustducin in the mammalian gut. Am J Physiol Gastrointest Liver Physiol, 291 (2): G171-7. [PMID:16710053]

Rozengurt E, Sternini C. (2007) Taste receptor signaling in the mammalian gut. Curr Opin Pharmacol, 7 (6): 557-62. [PMID:18024184]

Sevá Pessôa B, van der Lubbe N, Verdonk K, Roks AJ, Hoorn EJ, Danser AH. (2013) Key developments in renin-angiotensin-aldosterone system inhibition. Nat Rev Nephrol, 9 (1): 26-36. [PMID:23165302]

Spiegel S, Milstien S. (2011) The outs and the ins of sphingosine-1-phosphate in immunity. Nat Rev Immunol, 11 (6): 403-15. [PMID:21546914]

Temussi PA. (2009) Sweet, bitter and umami receptors: a complex relationship. Trends Biochem Sci, 34 (6): 296-302. [PMID:19443222]

Tepper BJ. (2008) Nutritional implications of genetic taste variation: the role of PROP sensitivity and other taste phenotypes. Annu Rev Nutr, 28: 367-88. [PMID:18407743]

Yarmolinsky DA, Zuker CS, Ryba NJ. (2009) Common sense about taste: from mammals to insects. Cell, 139 (2): 234-44. [PMID:19837029]

Yona S, Lin HH, Siu WO, Gordon S, Stacey M. (2008) Adhesion-GPCRs: emerging roles for novel receptors. Trends Biochem Sci, 33 (10): 491-500. [PMID:18789697]

How to cite this family page

Database page citation:

Orphan and other 7TM receptors. Accessed on 02/07/2025. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=115.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: G protein-coupled receptors. Br J Pharmacol. 176 Issue S1: S21-S141.