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Gene Review

SLC52A1  -  solute carrier family 52 (riboflavin...

Homo sapiens

Synonyms: FLJ10060, GPCR42, GPR172B, PAR2, PERV-A receptor 2, ...
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Disease relevance of GPR172B


Psychiatry related information on GPR172B

  • Many drugs of abuse signal through receptors that couple to G proteins (GPCRs), so the factors that control GPCR signaling are likely to be important to the understanding of drug abuse [6].
  • Given the complexity of neurological disorders such as ischemic stroke, Alzheimer's disease and epilepsy, exploitation mGlu receptor-associated GPCR interactions may prove efficacious in the treatment of such disorders [7].

High impact information on GPR172B

  • Future high-resolution structural studies of rhodopsin and other GPCRs will form a basis to elucidate the detailed molecular mechanism of GPCR-mediated signal transduction [8].
  • Significantly, GPCR-containing CCPs are also functionally distinct, as their surface residence time is regulated locally by GPCR cargo via PDZ-dependent linkage to the actin cytoskeleton [9].
  • Our results reveal a novel function of betaarr1 as a cytoplasm-nucleus messenger in GPCR signaling and elucidate an epigenetic mechanism for direct GPCR signaling from cell membrane to the nucleus through signal-dependent histone modification [10].
  • (2005) provide evidence that beta-arrestin 1 moves to the nucleus in response to GPCR stimulation, where it regulates gene expression by facilitating histone acetylation at specific gene promoters [11].
  • A nuclear function of beta-arrestin1 in GPCR signaling: regulation of histone acetylation and gene transcription [10].

Chemical compound and disease context of GPR172B


Biological context of GPR172B

  • In humans, they reside at the ends of the X and Y chromosomes and encompass roughly 2.7 Mb (PAR1) and 0.33 Mb (PAR2) [17].
  • While PAR2 resembles the overall sequence composition of the X chromosome and exhibits only slightly elevated recombination rates, PAR1 is characterized by a significantly higher GC content and a completely different repeat structure [17].
  • Protease-activated receptor 1 (PAR1), a G protein-coupled receptor (GPCR) for thrombin, has been correlated with cell proliferation [18].
  • The selective activation of each PAR by short synthetic peptides representing these sequences has demonstrated that PAR1, PAR2 and PAR4 play important roles in regulating physiological responses ranging from vasoregulation and cell growth to inflammation and nociception [19].
  • Furthermore, here we demonstrate that activation of PAR-2, as well as PAR-1, rescued astrocytes from ceramide-induced apoptosis via regulating chemokine GRO/CINC-1 release [20].

Anatomical context of GPR172B

  • We herein demonstrated that the contractile responses to the PAR-1 and PAR-2 agonist were markedly enhanced in the rabbit femoral arteries after balloon injury [21].
  • Induction of IL-6 release from human T cells by PAR-1 and PAR-2 agonists [22].
  • An important role could be played by bFGF in the regulation of functional PAR-2 expression in cultured RA synovial fibroblasts [23].
  • This study was conducted to examine whether human conjunctival epithelial cells (HCECs) express functionally active PAR1 and PAR2 using Chang conjunctival epithelial cells as in vitro model [24].
  • Our data suggest that OA1 represents the first example of an exclusively intracellular GPCR and support the hypothesis that GPCR-mediated signal transduction systems also operate at the internal membranes in mammalian cells [25].

Associations of GPR172B with chemical compounds

  • This study is the first to describe a function for a tyrosine-based motif, YXX, in GPCR internalization and reveal novel complexities in the regulation of GPCR trafficking [26].
  • The pre-treatment of cells with thrombin or the PAR-1-specific peptide TRag (Ala-pFluoro-Phe-Arg-Cha-HomoArg-Tyr-NH(2), synthetic thrombin receptor agonist peptide), but not the PAR-2-specific peptide, reduces significantly the mesotrypsin-induced Ca(2+) response [27].
  • Real-time PCR showed that MCP-1 mRNA is up-regulated by the serine proteases tested and by agonist peptides of PAR-1 and PAR-2 [28].
  • The constitutive expression of PAR1 and PAR2, and their activation by thrombin and tryptase, respectively, may have important implications in ocular inflammation [24].
  • We provide here structural evidence that the protein product of the ocular albinism type 1 gene (OA1), a pigment cell-specific integral membrane glycoprotein, represents a novel member of the GPCR superfamily and demonstrate that it binds heterotrimeric G proteins [25].

Regulatory relationships of GPR172B

  • Agonist peptides of PAR-1 and PAR-2 stimulate MCP-1 secretion up to 15- and 12.7-fold, respectively [28].

Other interactions of GPR172B

  • The expression of PAR-1 and PAR-2 slightly increased after the sham operation, whereas it markedly and significantly increased after balloon injury [21].

Analytical, diagnostic and therapeutic context of GPR172B

  • Immunocytochemistry showed thrombin-sensitive PAR receptors as well as trypsin-sensitive PAR-2 receptors [29].
  • Graded reductions in GPCR expression can be achieved through antisense strategies or total gene ablation or replacement can be achieved through gene targeting strategies, and exogenous expression of wild-type or mutant GPCR isoforms can be accomplished with transgenic technologies [30].
  • Here, we report the molecular cloning of a novel GPCR for LTB(4), designated BLT2, which binds LTB(4) with a Kd value of 23 nM compared with 1.1 nM for BLT1, but still efficiently transduces intracellular signaling [31].
  • Techniques: GPCR assembly, pharmacology and screening by flow cytometry [32].
  • In the present study we demonstrate the formation of an agonist-induced multimeric complex containing a GPCR, betaarrestin 2, and the beta2-adaptin subunit of AP-2. beta2-Adaptin binds betaarrestin 2 in a yeast two-hybrid assay and coimmunoprecipitates with betaarrestins and beta2AR in an agonist-dependent manner in HEK-293 cells [33].


  1. Identification of receptors for pig endogenous retrovirus. Ericsson, T.A., Takeuchi, Y., Templin, C., Quinn, G., Farhadian, S.F., Wood, J.C., Oldmixon, B.A., Suling, K.M., Ishii, J.K., Kitagawa, Y., Miyazawa, T., Salomon, D.R., Weiss, R.A., Patience, C. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  2. Tissue factor deficiency and PAR-1 deficiency are protective against renal ischemia reperfusion injury. Sevastos, J., Kennedy, S.E., Davis, D.R., Sam, M., Peake, P.W., Charlesworth, J.A., Mackman, N., Erlich, J.H. Blood (2007) [Pubmed]
  3. TACE cleavage of proamphiregulin regulates GPCR-induced proliferation and motility of cancer cells. Gschwind, A., Hart, S., Fischer, O.M., Ullrich, A. EMBO J. (2003) [Pubmed]
  4. A central role of EGF receptor transactivation in angiotensin II -induced cardiac hypertrophy. Shah, B.H., Catt, K.J. Trends Pharmacol. Sci. (2003) [Pubmed]
  5. p90 ribosomal S6 kinase 2 exerts a tonic brake on G protein-coupled receptor signaling. Sheffler, D.J., Kroeze, W.K., Garcia, B.G., Deutch, A.Y., Hufeisen, S.J., Leahy, P., Brüning, J.C., Roth, B.L. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  6. Regulators of G protein signaling (RGS proteins): novel central nervous system drug targets. Neubig, R.R. J. Pept. Res. (2002) [Pubmed]
  7. Emerging signalling and protein interactions mediated via metabotropic glutamate receptors. Moldrich, R.X., Beart, P.M. Current drug targets. CNS and neurological disorders. (2003) [Pubmed]
  8. Rhodopsin: structural basis of molecular physiology. Menon, S.T., Han, M., Sakmar, T.P. Physiol. Rev. (2001) [Pubmed]
  9. Cargo regulates clathrin-coated pit dynamics. Puthenveedu, M.A., von Zastrow, M. Cell (2006) [Pubmed]
  10. A nuclear function of beta-arrestin1 in GPCR signaling: regulation of histone acetylation and gene transcription. Kang, J., Shi, Y., Xiang, B., Qu, B., Su, W., Zhu, M., Zhang, M., Bao, G., Wang, F., Zhang, X., Yang, R., Fan, F., Chen, X., Pei, G., Ma, L. Cell (2005) [Pubmed]
  11. Beta-arrestin goes nuclear. Beaulieu, J.M., Caron, M.G. Cell (2005) [Pubmed]
  12. E-selectin permits communication between PAF receptors and TRPC channels in human neutrophils. McMeekin, S.R., Dransfield, I., Rossi, A.G., Haslett, C., Walker, T.R. Blood (2006) [Pubmed]
  13. Lysophosphatidic acid-induced squamous cell carcinoma cell proliferation and motility involves epidermal growth factor receptor signal transactivation. Gschwind, A., Prenzel, N., Ullrich, A. Cancer Res. (2002) [Pubmed]
  14. Pleiotropic coupling of G protein-coupled receptors to the mitogen-activated protein kinase cascade. Role of focal adhesions and receptor tyrosine kinases. Della Rocca, G.J., Maudsley, S., Daaka, Y., Lefkowitz, R.J., Luttrell, L.M. J. Biol. Chem. (1999) [Pubmed]
  15. The synthetic peptide derived from the NH2-terminal extracellular region of an orphan G protein-coupled receptor, GPR1, preferentially inhibits infection of X4 HIV-1. Jinno-Oue, A., Shimizu, N., Soda, Y., Tanaka, A., Ohtsuki, T., Kurosaki, D., Suzuki, Y., Hoshino, H. J. Biol. Chem. (2005) [Pubmed]
  16. Differential regulation of estrogen receptor alpha, glucocorticoid receptor and retinoic acid receptor alpha transcriptional activity by melatonin is mediated via different G proteins. Kiefer, T.L., Lai, L., Yuan, L., Dong, C., Burow, M.E., Hill, S.M. J. Pineal Res. (2005) [Pubmed]
  17. The pseudoautosomal regions, SHOX and disease. Blaschke, R.J., Rappold, G. Curr. Opin. Genet. Dev. (2006) [Pubmed]
  18. Negative regulation of protease-activated receptor 1-induced Src kinase activity by the association of phosphocaveolin-1 with Csk. Lu, T.L., Kuo, F.T., Lu, T.J., Hsu, C.Y., Fu, H.W. Cell. Signal. (2006) [Pubmed]
  19. Proteinase-mediated cell signalling: targeting proteinase-activated receptors (PARs) by kallikreins and more. Oikonomopoulou, K., Hansen, K.K., Saifeddine, M., Vergnolle, N., Tea, I., Diamandis, E.P., Hollenberg, M.D. Biol. Chem. (2006) [Pubmed]
  20. Proteinase-activated receptor-1 and -2 induce the release of chemokine GRO/CINC-1 from rat astrocytes via differential activation of JNK isoforms, evoking multiple protective pathways in brain. Wang, Y., Luo, W., Reiser, G. Biochem. J. (2007) [Pubmed]
  21. Upregulation of proteinase-activated receptors and hypercontractile responses precede development of arterial lesions after balloon injury. Fukunaga, R., Hirano, K., Hirano, M., Niiro, N., Nishimura, J., Maehara, Y., Kanaide, H. Am. J. Physiol. Heart Circ. Physiol. (2006) [Pubmed]
  22. Induction of IL-6 release from human T cells by PAR-1 and PAR-2 agonists. Li, T., He, S. Immunol. Cell Biol. (2006) [Pubmed]
  23. Up-regulation of protease-activated receptor-2 by bFGF in cultured human synovial fibroblasts. Abe, K., Aslam, A., Walls, A.F., Sato, T., Inoue, H. Life Sci. (2006) [Pubmed]
  24. Constitutive expression of functionally active protease-activated receptors 1 and 2 in human conjunctival epithelial cells. Nickel, T.J., Kabir, M.H., Talreja, J., Stechschulte, D.J., Dileepan, K.N. Mediators Inflamm. (2006) [Pubmed]
  25. Ocular albinism: evidence for a defect in an intracellular signal transduction system. Schiaffino, M.V., d'Addio, M., Alloni, A., Baschirotto, C., Valetti, C., Cortese, K., Puri, C., Bassi, M.T., Colla, C., De Luca, M., Tacchetti, C., Ballabio, A. Nat. Genet. (1999) [Pubmed]
  26. A tyrosine-based sorting signal regulates intracellular trafficking of protease-activated receptor-1: multiple regulatory mechanisms for agonist-induced G protein-coupled receptor internalization. Paing, M.M., Temple, B.R., Trejo, J. J. Biol. Chem. (2004) [Pubmed]
  27. Mesotrypsin, a brain trypsin, activates selectively proteinase-activated receptor-1, but not proteinase-activated receptor-2, in rat astrocytes. Wang, Y., Luo, W., Wartmann, T., Halangk, W., Sahin-T??th, M., Reiser, G. J. Neurochem. (2006) [Pubmed]
  28. Induction of monocyte chemoattractant protein-1 release from A549 cells by agonists of protease-activated receptor-1 and -2. Wang, H., Yi, T., Zheng, Y., He, S. Eur. J. Cell Biol. (2007) [Pubmed]
  29. Thrombin inhibits intercellular calcium wave propagation in corneal endothelial cells by modulation of hemichannels and gap junctions. D'hondt, C., Ponsaerts, R., Srinivas, S.P., Vereecke, J., Himpens, B. Invest. Ophthalmol. Vis. Sci. (2007) [Pubmed]
  30. G protein-coupled receptors: functional and mechanistic insights through altered gene expression. Rohrer, D.K., Kobilka, B.K. Physiol. Rev. (1998) [Pubmed]
  31. A second leukotriene B(4) receptor, BLT2. A new therapeutic target in inflammation and immunological disorders. Yokomizo, T., Kato, K., Terawaki, K., Izumi, T., Shimizu, T. J. Exp. Med. (2000) [Pubmed]
  32. Techniques: GPCR assembly, pharmacology and screening by flow cytometry. Waller, A., Simons, P.C., Biggs, S.M., Edwards, B.S., Prossnitz, E.R., Sklar, L.A. Trends Pharmacol. Sci. (2004) [Pubmed]
  33. The beta2-adrenergic receptor/betaarrestin complex recruits the clathrin adaptor AP-2 during endocytosis. Laporte, S.A., Oakley, R.H., Zhang, J., Holt, J.A., Ferguson, S.S., Caron, M.G., Barak, L.S. Proc. Natl. Acad. Sci. U.S.A. (1999) [Pubmed]
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