| LATEST PAIRINGS |
| The following are reports of recent pairings of receptors with endogenous or synthetic ligands, which in most cases are a single publication. |
| CMKOR1 & CXC chemokines CXCL11 and CXCL12/SDF-1 |
| Statement by NC-IUPHAR on CMKOR1 |
| "A molecule listed in the IUPHAR orphan receptor database as CMKOR1, and originally named RDC1, is now commonly referred to in the literature as CXCR7, on the basis of its clear ability to bind the CXC chemokines CXCL11 and CXCL12/SDF-1 with high affinity. Although reports have suggested that this molecule is able to mediate cellular responses, including chemotaxis and Akt activation, this has not been consistently shown in primary cells. In transfection systems, CXCR7 was reported to form heterodimers with CXCR4 and to modulate CXCL12 signaling. Several studies suggest a role for this receptor in cell growth and survival, and in tumorigenesis, but the underlying signaling pathways remain unknown. The mouse homologue is clearly involved in cardiac valve development and has minor effects on marginal zone B cell localization, but the signaling mechanisms are not defined. The zebrafish homologue is clearly involved in primordial germ cell migration, where the mechanism appears to involve scavenging of CXCL12 leading to formation of CXCL12 gradients. The NC-IUPHAR sub-committee on chemokine receptor nomenclature has concluded that use of the systematic chemokine receptor nomenclature name CXCR7 for this molecule shall remain unofficial until clear evidence of signal transduction mechanisms can be obtained." |
| For database entry click here |
| GPR92/LPA5 & lysophosphatidic acid receptor. |
| Lee CW, Rivera R, Gardell S, Dubin AE, Chun J. (2006) GPR92 as a new G12/13- and Gq-coupled lysophosphatidic acid receptor that increases cAMP, LPA5J Biol Chem. 281, 23589-97 [PMID: 16774927] |
| Kotarsky K, Boketoft A, Bristulf J, Nilsson NE, Norberg A, Hansson S, Owman C, Sillard R, Leeb-Lundberg LM, Olde B (2006) Lysophosphatidic acid binds to and activates GPR92, a G protein-coupled receptor highly expressed in gastrointestinal lymphocytes.J Pharmacol Exp Ther. 318, 619-28 [PMID: 16651401] |
| GPR17 & cysteinyl-leukotrienes (CysLTs)/ uracil nucleotides. |
| Ciana P, Fumagalli M, Trincavelli ML, Verderio C, Rosa P, Lecca D, Ferrario S, Parravicini C, Capra V, Gelosa P, Guerrini U, Belcredito S, Cimino M, Sironi L,Tremoli E, Rovati GE, Martini C, Abbracchio MP (2006) The orphan receptor GPR17 identified as a new dual uracil nucleotides/cysteinyl-leukotrienes receptor.EMBO J. 25, 4615-27 [PMID: 16990797] |
| GPR23/LPA4 & lysophosphatidic acid receptor. |
| Ignatov, A., Robert, J., Gregory-Evans, C., Schaller, H. C. (2006) GPR23 is a lysophosphatidic acid (LPA) receptor utilizing G(s)-,G(q)/G(i)-mediated calcium signaling and G(12/13)-mediated Rho activation.J Biol Chem. 282, 4310-7. [PMID: 17166850] |
| GPR75 & RANTES |
| Ignatov, A., Robert, J., Gregory-Evans, C., Schaller, H. C. (2006) RANTES stimulates Ca(2+) mobilization and inositol triphosphate (IP(3)) formation in cells transfected with G protein-coupled receptor 75. Br J Pharmacol. [Epub ahead of print] [PMID: 17001303] |
| See also: |
| Pease, J. E. (2006) Tails of the unexpected - an atypical receptor for the chemokine RANTES/CCL5 expressed in brain. Br J Pharmacol. [Epub ahead of print] [PMID: 17001302] |
| GPR35 & Kynurenic acid. |
| Wang, J., Simonavicius, N., Wu, X., Swaminath, G., Reagan, J., Tian, H., Ling, L. (2006) Kynurenic acid as a ligand for orphan G protein-coupled receptor GPR35. J Biol Chem. 281, 22021-22028. [PMID: 16754668] |
| GPR120 & Free Fatty Acids. |
| Hirasawa, A., Tsumaya, K., Awaji, T., Katsuma, S., Adachi, T., Yamada, M., Sugimoto, Y., Miyazaki, S. and Tsujimoto, G. (2005) Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120. Nat Med. 11, 90-94. [PMID: 15619630] |
| GPR30 & Estrogen |
| Several groups have confirmed that estrogen is an agonist of this receptor, for database entry click here. |
| For review see: Filardo, E. J. and Thomas, P. (2005) GPR30: a seven-transmembrane-spanning estrogen receptor that triggers EGF release. Trends Endocrinol Metab. 16, 362-367. [PMID: 16125968] |
| GPR39 & Obestatin |
| Zhang, J. V., Ren, P. G., Avsian-Kretchmer, O., Luo, C. W., Rauch, R., Klein, C. and Hsueh, A. J. (2005) Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intake. Science. 310, 996-999. [PMID: 16284174] |
| Initial pairing could not be repeated |
| Holst, B., Egerod, K. L., Schild, E., Vickers, S. P., Cheetham, S., Gerlach, L. O., Storjohann, L., Stidsen, C. E., Jones, R. Beck-Sickinger, A. G., Schwartz, T. W. (2006) GPR39 signaling is stimulated by zinc ions but not by obestatin. Endocrinology [Epub ahead of print] [PMID: 16959833] |
| Chartrel N, Alvear-Perez R, Leprince J, Iturrioz X, Reaux-Le Goazigo A, Audinot V, Chomarat P, Coge F, Nosjean O, Rodriguez M, Galizzi JP, Boutin JA, Vaudry H, Llorens-Cortes C. (2007) Zhang et al. reported that obestatin, a peptide derived from the ghrelin precursor, activated the orphan G protein-coupled receptor GPR39. However, we found that I125-obestatin does not bind GPR39 and observed no effects of obestatin on GPR39-transfected cells in various functional assays (cyclic adenosine monophosphate production, calcium mobilization, and GPR39 internalization). Our results indicate that obestatin is not the cognate ligand for GPR39. Science 315,766 [PMID: 17289961] |
| GPR37 & The neuropeptide head activator (HA) |
| Rezgaoui, M., Susens, U., Ignatov, A., Gelderblom, M., Glassmeier, G., Franke, I., Urny, J., Imai, Y., Takahashi, R. and Schaller, H. C. (2006)
The neuropeptide head activator is a high-affinity ligand for the orphan G-protein-coupled receptor GPR37. J Cell Sci. 119, 542-549. [PMID: 16443751] |
| CXCR2 & Macrophage Derived lectin MNCF |
| Moreno, A. N., Pereira-da-Silva, G., Oliver, C., Jamur, M. C., Panunto-Castelo, A. and Roque-Barreira, M. C. (2005) The macrophage-derived lectin, MNCF, activates neutrophil migration through a pertussis toxin-sensitive pathway. J. Histochem. Cytochem. 53, 715-723. |
| GPR119 & Oleoylethanolamide (OEA) |
| Overton, H. A., Babbs, A. J., Doel, S. M., Fyfe, M. C., Gardner, L. S., Griffin, G., Jackson, H. C., Procter, M. J., Rasamison, C. M., Tang-Christensen, M., Widdowson, P. S., Williams, G. M. and Reynet, C. (2006)
Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab. 3, 167-175. [PMID: 16517404] |
| CMKLR1 & Resolvin E1 (RvE1) oxygenated product of eicosapentaenoic acid (EPA) |
| Arita, M., Bianchini, F., Aliberti, J., Sher, A., Chiang, N., Hong, S., Yang, R., Petasis, N. A. and Serhan, C. N. (2005)
Stereochemical assignment, antiinflammatory properties, and receptor for the omega-3 lipid mediator resolvin E1. J Exp Med. 201, 713-722. [PMID: 15753205]  |
| TIG2/chermerin found to be an alternative ligand for CMKLR1. |
| Meder, W., Wendland, M., Busmann, A., Kutzleb, C., Spodsberg, N., John, H., Richter, R., Schleuder, D., Meyer, M. and Forssmann, W. G. (2003) Characterization of human circulating TIG2 as a ligand for the orphan receptor ChemR23. FEBS Lett. 555, 495-499. [PMID: 14675762] |
| GPR55: Proposed as a cannabinoid receptor but endogenous ligand not yet known. |
| Drmota, T., Greasley, P. and Groblewski T. (2004)
Screening assays for cannabinoid-ligand-type modulators of GPR55. WIPO patent 074 844 |
| RETRACTED: GPR68 & Sphingosylphosphorylcholine |
| Xu, Y., Zhu, K., Hong, G., Wu, W., Baudhuin, L. M., Xiao, Y. and Damron, D. S. (2006)
Sphingosylphosphorylcholine is a ligand for ovarian cancer G-protein-coupled receptor 1. Nat Cell Biol. 8, 299. [PMID: 10806476] |
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