Identification of a novel small-molecule agonist for human G protein-coupled receptor 3

Journal of Pharmacology and Experimental Therapeutics

Volumn 349, Issue 3, 2014, Pages 437-443

  Ye, Chenli ^a   Zhang, Zhenghong ^a   Wang, Zhilong ^b   Hua, Qiuhong ^a   Zhang, Ru ^a   Xie, Xin ^a,b,c  

^a TONGJI UNIVERSITY   (China)

^b SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^c NONE   (China)

Author keywords

[No Author keywords available]

Indexed keywords

ADENYLATE CYCLASE; BETA ARRESTIN 2; CYCLIC AMP; DIPHENYLIODONIUM SALT; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR 3; SPHINGOSINE 1 PHOSPHATE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG DETERMINATION; DRUG IDENTIFICATION; DRUG SELECTIVITY; DRUG STRUCTURE; EMBRYO; ENZYME ACTIVATION; HEK293 CELL LINE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; INTERNALIZATION; INTRACELLULAR SIGNALING; MEMBRANE TRANSPORT; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN LOCALIZATION; RECEPTOR DOWN REGULATION; SIGNAL TRANSDUCTION;

CALCIUM SIGNALING; CELL CULTURE TECHNIQUES; CELL MEMBRANE; CYCLIC AMP; GTP-BINDING PROTEIN ALPHA SUBUNITS, GS; HEK293 CELLS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MOLECULAR STRUCTURE; ONIUM COMPOUNDS; RECEPTORS, G-PROTEIN-COUPLED; SMALL MOLECULE LIBRARIES; TRANSFECTION;

EID: 84901188421     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.114.213082     Document Type: Article

References (27)

1. Aldieri E, Riganti C, Polimeni M, Gazzano E, Lussiana C, Campia I, and Ghigo D (2008) Classical inhibitors of NOX NAD(P)H oxidases are not specific. Curr Drug Metab 9:686-696.
2. Bjursell M, Gerdin AK, Jönsson M, Surve VV, Svensson L, Huang XF, Törnell J, and Bohlooly-Y M (2006) G protein-coupled receptor 12 deficiency results in dys-lipidemia and obesity in mice. Biochem Biophys Res Commun 348:359-366.
3. Deng J, Lang S, Wylie C, and Hammes SR (2008) The Xenopus laevis isoform of G protein-coupled receptor 3 (GPR3) is a constitutively active cell surface receptor that participates in maintaining meiotic arrest in X. laevis oocytes. Mol Endocrinol 22:1853-1865.
4. Ferguson SS, Barak LS, Zhang J, and Caron MG (1996) G-protein-coupled receptor regulation: role of G-protein-coupled receptor kinases and arrestins. Can J Physiol Pharmacol 74:1095-1110.
5. Ignatov A, Lintzel J, Hermans-Borgmeyer I, Kreienkamp HJ, Joost P, Thomsen S, Methner A, and Schaller HC (2003a) Role of the G-protein-coupled receptor GPR12 as high-Affinity receptor for sphingosylphosphorylcholine and its expression and function in brain development. J Neurosci 23:907-914.
6. Ignatov A, Lintzel J, Kreienkamp HJ, and Schaller HC (2003b) Sphingosine-1-phosphate is a high-Affinity ligand for the G protein-coupled receptor GPR6 from mouse and induces intracellular Ca21 release by activating the sphingosine-kinase pathway. Biochem Biophys Res Commun 311:329-336.
7. Iismaa TP, Kiefer J, Liu ML, Baker E, Sutherland GR, and Shine J (1994) Isolation and chromosomal localization of a novel human G-protein-coupled receptor (GPR3) expressed predominantly in the central nervous system. Genomics 24:391-394.
8. Kleniewska P, Piechota A, Skibska B, and Gora̧ca A (2012) The NADPH oxidase family and its inhibitors. Arch Immunol Ther Exp (Warsz) 60:277-294.
9. Kovanci E, Simpson JL, Amato P, Rohozinski J, Heard MJ, Bishop CE, and Carson SA (2008) Oocyte-specific G-protein-coupled receptor 3 (GPR3): no perturbations found in 82 women with premature ovarian failure (first report). Fertil Steril 90: 1269-1271.
10. Ledent C, Demeestere I, Blum D, Petermans J, Hämäläinen T, Smits G, and Vassart G (2005) Premature ovarian aging in mice deficient for Gpr3. Proc Natl Acad Sci USA 102:8922-8926.
11. Lefkowitz RJ and Shenoy SK (2005) Transduction of receptor signals by beta-Arrestins. Science 308:512-517.
12. Lobo MK, Cui Y, Ostlund SB, Balleine BW, and Yang XW (2007) Genetic control of instrumental conditioning by striatopallidal neuron-specific S1P receptor Gpr6. Nat Neurosci 10:1395-1397.
13. Lowther KM, Uliasz TF, Götz KR, Nikolaev VO, and Mehlmann LM (2013) Regulation of Constitutive GPR3 Signaling and Surface Localization by GRK2 and b-Arrestin-2 Overexpression in HEK293 Cells. PLoS ONE 8:e65365.
14. Luttrell LM and Lefkowitz RJ (2002) The role of beta-Arrestins in the termination and transduction of G-protein-coupled receptor signals. J Cell Sci 115:455-465.
15. Mehlmann LM (2005) Oocyte-specific expression of Gpr3 is required for the maintenance of meiotic arrest in mouse oocytes. Dev Biol 288:397-404.
16. Mehlmann LM, Saeki Y, Tanaka S, Brennan TJ, Evsikov AV, Pendola FL, Knowles BB, Eppig JJ, and Jaffe LA (2004) The Gs-linked receptor GPR3 maintains meiotic arrest in mammalian oocytes. Science 306:1947-1950.
17. Ruiz-Medina J, Ledent C, and Valverde O (2011) GPR3 orphan receptor is involved in neuropathic pain after peripheral nerve injury and regulates morphine-induced antinociception. Neuropharmacology 61:43-50.
18. Siehler S and Manning DR (2002) Pathways of transduction engaged by sphingosine 1-phosphate through G protein-coupled receptors. Biochim Biophys Acta 1582: 94-99.
19. Tanaka S, Ishii K, Kasai K, Yoon SO, and Saeki Y (2007) Neural expression of G protein-coupled receptors GPR3, GPR6, and GPR12 up-regulates cyclic AMP levels and promotes neurite outgrowth. J Biol Chem 282:10506-10515.
20. Tanaka S, Shaikh IM, Chiocca EA, and Saeki Y (2009) The Gs-linked receptor GPR3 inhibits the proliferation of cerebellar granule cells during postnatal development. PLoS ONE 4:e5922.
21. Thathiah A, Horré K, Snellinx A, Vandewyer E, Huang Y, Ciesielska M, De Kloe G, Munck S, and De Strooper B (2013) b-Arrestin 2 regulates Ab generation and g-secretase activity in Alzheimer's disease. Nat Med 19:43-49.
22. Thathiah A, Spittaels K, Hoffmann M, Staes M, Cohen A, Horré K, Vanbrabant M, Coun F, Baekelandt V, and Delacourte A, et al. (2009) The orphan G protein-coupled receptor 3 modulates amyloid-beta peptide generation in neurons. Science 323:946-951.
23. Uhlenbrock K, Gassenhuber H, and Kostenis E (2002) Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors. Cell Signal 14:941-953.
24. Valverde O, Célérier E, Baranyi M, Vanderhaeghen P, Maldonado R, Sperlagh B, Vassart G, and Ledent C (2009) GPR3 receptor, a novel actor in the emotional-like responses. PLoS ONE 4:e4704.
25. Yin H, Chu A, Li W, Wang B, Shelton F, Otero F, Nguyen DG, Caldwell JS, and Chen YA (2009) Lipid G protein-coupled receptor ligand identification using beta-Arrestin PathHunter assay. J Biol Chem 284:12328-12338.
26. Zhang R and Xie X (2012) Tools for GPCR drug discovery. Acta Pharmacol Sin 33:372-384.
27. Zhou S, Wang B, Ni F, Wang J, Cao Y, and Ma X (2010) GPR3 may not be a potential candidate gene for premature ovarian failure. Reprod Biomed Online 20:53-55.