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Gene Review

P2RY14  -  purinergic receptor P2Y, G-protein coupled...

Homo sapiens

Synonyms: BPR105, G-protein coupled receptor 105, GPR105, KIAA0001, P2Y purinoceptor 14, ...
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Disease relevance of P2RY14

  • GPR105 is widely expressed throughout many brain regions and peripheral tissues of human and rodents, and couples to a pertussis toxin-sensitive G protein [1].
  • In conclusion, we have shown that although UDP-glucose inhibits forskolin-stimulated cAMP accumulation in human U373 MG astrocytoma cells, we did not detect P2Y14 receptor mRNA in these cells [2].
  • Therefore, the primary aim of this study was to investigate the effects of uridine 5'-diphosphoglucose (UDP-glucose) on forskolin-stimulated cyclic AMP (cAMP) accumulation in two cell lines that reportedly express P2Y14 receptor mRNA, namely human neuroblastoma SH-SY5Y cells and human astrocytoma U373 MG cells [2].

High impact information on P2RY14


Biological context of P2RY14

  • Cloning, pharmacology, and tissue distribution of G-protein-coupled receptor GPR105 (KIAA0001) rodent orthologs [8].
  • Mutagenesis of the entire UDP-glucose receptor gene yielded receptors with increased activity but similar ligand specificities, while random mutagenesis of residues in the immediate vicinity of the ligand-binding pocket yielded mutants with altered ligand specificity [9].

Anatomical context of P2RY14

  • To further characterise the role of GPR105, we demonstrate by immunohistochemistry with receptor-specific antiserum that GPR105 protein is widely distributed throughout the post mortem human brain where it is localised to glial cells, and specifically co-localises with astrocytes [1].
  • Using quantitative RT-PCR we also show that GPR105 mRNA exhibits a restricted expression profile in an array of human cell lines and primary cells, with prominent expression detected in immune cells including neutrophils, lymphocytes, and megakaryocytic cells [1].
  • Prediction of the coding sequences of unidentified human genes. I. The coding sequences of 40 new genes (KIAA0001-KIAA0040) deduced by analysis of randomly sampled cDNA clones from human immature myeloid cell line KG-1 [10].
  • P2Y14 mRNA was weakly expressed by putative microglia [11].
  • Schwann cells expressed P2Y2 mRNA, and the nonneuronal cells around the DRG neurons, perhaps the satellite cells, expressed P2Y12 and P2Y14 mRNAs [11].

Associations of P2RY14 with chemical compounds

  • Finally, we show that expression of GPR105 mRNA in the rat brain is up-regulated by immunologic challenge with lipopolysaccharide [1].
  • To investigate the G protein selectivity of GPR105, we used chimeric Galpha subunits (Galpha(qi5), Galpha(qo5), and Galpha(qs5)) and an intracellular Ca(2+) mobilisation assay to demonstrate that GPR105 couples to Galpha subunits of the G(i/o) family but not to G(s) family proteins or to endogenous G(q/11) proteins in HEK-293 cells [1].
  • It has recently been shown that UDP-glucose is a potent agonist of the orphan G-protein-coupled receptor (GPCR) KIAA0001 [8].

Other interactions of P2RY14


Analytical, diagnostic and therapeutic context of P2RY14

  • By first sensitizing the P2Y14 receptor and then redirecting ligand specificity, we were able to create mutant receptors suitable for a simple biosensor [9].


  1. GPR105, a novel Gi/o-coupled UDP-glucose receptor expressed on brain glia and peripheral immune cells, is regulated by immunologic challenge: possible role in neuroimmune function. Moore, D.J., Murdock, P.R., Watson, J.M., Faull, R.L., Waldvogel, H.J., Szekeres, P.G., Wilson, S., Freeman, K.B., Emson, P.C. Brain Res. Mol. Brain Res. (2003) [Pubmed]
  2. Pharmacological effects mediated by UDP-glucose that are independent of P2Y14 receptor expression. Scrivens, M., Dickenson, J.M. Pharmacol. Res. (2005) [Pubmed]
  3. P2Y-like receptor, GPR105 (P2Y14), identifies and mediates chemotaxis of bone-marrow hematopoietic stem cells. Lee, B.C., Cheng, T., Adams, G.B., Attar, E.C., Miura, N., Lee, S.B., Saito, Y., Olszak, I., Dombkowski, D., Olson, D.P., Hancock, J., Choi, P.S., Haber, D.A., Luster, A.D., Scadden, D.T. Genes Dev. (2003) [Pubmed]
  4. Human immature monocyte-derived dendritic cells express the G protein-coupled receptor GPR105 (KIAA0001, P2Y14) and increase intracellular calcium in response to its agonist, uridine diphosphoglucose. Skelton, L., Cooper, M., Murphy, M., Platt, A. J. Immunol. (2003) [Pubmed]
  5. P2 receptors activated by uracil nucleotides--an update. Brunschweiger, A., Müller, C.E. Current medicinal chemistry. (2006) [Pubmed]
  6. Pharmacological profiles of cloned mammalian P2Y-receptor subtypes. von Kügelgen, I. Pharmacol. Ther. (2006) [Pubmed]
  7. The P2Y14 receptor of airway epithelial cells: coupling to intracellular Ca2+ and IL-8 secretion. Müller, T., Bayer, H., Myrtek, D., Ferrari, D., Sorichter, S., Ziegenhagen, M.W., Zissel, G., Virchow, J.C., Luttmann, W., Norgauer, J., Di Virgilio, F., Idzko, M. Am. J. Respir. Cell Mol. Biol. (2005) [Pubmed]
  8. Cloning, pharmacology, and tissue distribution of G-protein-coupled receptor GPR105 (KIAA0001) rodent orthologs. Freeman, K., Tsui, P., Moore, D., Emson, P.C., Vawter, L., Naheed, S., Lane, P., Bawagan, H., Herrity, N., Murphy, K., Sarau, H.M., Ames, R.S., Wilson, S., Livi, G.P., Chambers, J.K. Genomics (2001) [Pubmed]
  9. Creation of GPCR-based chemical sensors by directed evolution in yeast. Ault, A.D., Broach, J.R. Protein Eng. Des. Sel. (2006) [Pubmed]
  10. Prediction of the coding sequences of unidentified human genes. I. The coding sequences of 40 new genes (KIAA0001-KIAA0040) deduced by analysis of randomly sampled cDNA clones from human immature myeloid cell line KG-1. Nomura, N., Miyajima, N., Sazuka, T., Tanaka, A., Kawarabayasi, Y., Sato, S., Nagase, T., Seki, N., Ishikawa, K., Tabata, S. DNA Res. (1994) [Pubmed]
  11. Neurons and glial cells differentially express P2Y receptor mRNAs in the rat dorsal root ganglion and spinal cord. Kobayashi, K., Fukuoka, T., Iyamanaka, H., Dai, Y., Obata, K., Tokunaga, A., Noguchi, K. J. Comp. Neurol. (2006) [Pubmed]
  12. A sequence-ready map of the Usher syndrome type III critical region on chromosome 3q. Joensuu, T., Hämäläinen, R., Lehesjoki, A.E., de la Chapelle, A., Sankila, E.M. Genomics (2000) [Pubmed]
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