Reassessment of the pharmacology of Sphingosine-1-phosphate S1P3 receptor ligands using the DiscoveRx PathHunter™ and Ca2+ release functional assays

British Journal of Pharmacology

Volumn 167, Issue 4, 2012, Pages 868-880

  Riddy, D M ^a   Stamp, C ^a,b   Sykes, D A ^a   Charlton, S J ^a   Dowling, M R ^a  

^a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^b NEWCASTLE UNIVERSITY   (United Kingdom)

Author keywords

arrestin coupling; agonist efficacy; DiscoveRx PathHunter ; drug discovery; receptor conformation; Sphingosine 1 phosphate

Indexed keywords

2 [4 [5 (3,4 DIETHOXYPHENYL) 1,2,4 OXADIAZOL 3 YL] 2,3 DIHYDRO 1H INDEN 1 YL AMINO]ETHANOL; 2 AMINO 2 [2 (4 OCTYLPHENYL)ETHYL] 1,3 PROPANEDIOL PHOSPHATE; AGENTS INTERACTING WITH TRANSMITTER, HORMONE OR DRUG RECEPTORS; CALCIUM ION; CYM 5442; FTY 720 P; PHOSPHORIC ACID MONO[2 AMINO 3 (4 OCTYL PHENYLAMINO)PROPYL]ESTER; SPHINGOSINE 1 PHOSPHATE; SPHINGOSINE 1 PHOSPHATE 3 RECEPTOR; SPHINGOSINE 1 PHOSPHATE RECEPTOR; UNCLASSIFIED DRUG; VPC 24191;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING COMPETITION; CALCIUM TRANSPORT; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG RESEARCH; DRUG SCREENING; FEMALE; HUMAN; HUMAN CELL; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN STRUCTURE;

ANIMALS; ARRESTINS; BINDING, COMPETITIVE; BIOLOGICAL ASSAY; CALCIUM; CHO CELLS; CRICETINAE; CRICETULUS; HUMANS; INDANS; LIGANDS; ORGANOPHOSPHATES; OXADIAZOLES; PROPYLENE GLYCOLS; RADIOLIGAND ASSAY; RECEPTORS, LYSOSPHINGOLIPID; SPHINGOSINE;

EID: 84867028276     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2012.02032.x     Document Type: Article

References (23)

1. Alexander SPH, Mathie A, Peters JA, (2011). Guide to receptors and channels (GRAC), 5th edition (2011). Br J Pharmacol 164 (Suppl. 1): S1-S324.
2. An S, Zheng Y, Bleu T, (2000). Sphingosine-1-Phosphate-induced cell proliferation, survival, and related signalling events mediated by G Protein-coupled receptors Edg3 and Edg5. J Biol Chem 275: 288-296.
3. Black JW, Leff P, (1983). Operational models of pharmacological agonist. Proc R Soc Lond B Biol Sci 220: 141-162.
4. Brinkmann V, Davis MD, Heise CE, Albert R, Cottens S, Hof R, et al,. (2002). The immune modulator FTY720 targets Sphingosine-1-Phosphate receptors. J Biol Chem 277: 21453-21457.
5. Carter CMS, Leighton-Davis JR, Charlton SJ, (2007). Miniaturized receptor binding assays: complications arising from ligand depletion. J Biomol Screen 12: 255-266.
6. Davis MD, Clemens JJ, Macdonald TL, Lynch KR, (2005). Sphingosine 1-phosphate analogs as receptor antagonists. J Biol Chem 280: 9833-9841.
7. van Der Lee MM, Bras M, van Koppen CJ, Zaman GJ, (2008). β-Arrestin recruitment assay for the identification of agonists of the sphingosine 1-phosphate receptor EDG1. J Biomol Screen 13: 986-998.
8. 3 receptor-induced reorganization of epithelial tight junctions compromises ling barrier integrity and is potentiated by TNF. Proc Natl Acad Sci U S A 102: 9270-9275.
9. Holdsworth G, Slocombe P, Hutchinson G, Milligan G, (2005). Analysis of endogenous S1P and LPA receptor expression in CHO-K1 cells. Gene 350: 59-63.
10. 3). Br J Pharmacol 156: 1305-1311.
11. Kennedy S, Kane KA, Pyne NJ, Pyne S, (2008). Targeting sphingosine-1-phoshate signalling for cardioprotection. Curr Opin Pharmacol 9: 1-8.
12. Lagane B, Chow KY, Balabanian K, Levoye A, Harriague J, Planchenault T, et al,. (2008). CXCR4 dimerization and beta-arrestin-mediated signaling account for the enhanced chemotaxis to CXCL12 in WHIM syndrome. Blood 112: 34-44.
13. Leff P, (1995). The two-state model of receptor activation. Trends Pharmacol Sci 16: 89-97.
14. Lichte K, Rossi R, Danneberg K, ter Braak M, Kurschner U, Jakobs KH, et al,. (2008). Lysophospholipid receptor- mediated calcium signaling in human keratinocytes. J Invest Dermatol 128: 1487-1498.
15. Marsolais D, Rosen H, (2009). Chemical modulators of sphingosine-1- phosphate receptors as barrier-oriented therapeutic molecules. Nat Rev Drug Discov 8: 297-307.
16. Murata N, Sato K, Kon J, Tomura H, Yanagita M, Kuwabara A, et al,. (2000). Interaction of sphingosine 1-phosphate with plasma components, including lipoproteins, regulates the lipid receptor-mediated actions. Biochem J 352: 809-815.
17. Pyne NJ, Pyne S, (2011). Selectivity and specificity of sphingosine-1-phosphate receptor ligands: 'off-targets' or complex pharmacology? Front Pharmacol 2: 1-5.
18. van Rossum J, Ariens EJ, (1962). Receptor-reserve and threshold-phenomena. II. Theories on drug-action and a quantitative approach to spare receptors and threshold values. Arch Int Pharmacodyn Ther 1: 385-413.
19. Salomone S, Potts EM, Tyndall S, Ip PC, Chun J, Brinkmann V, et al,. (2008). Analysis of sphingosine 1-phosphate receptors involved in constriction of isolated cerebral arteries with receptor null mice and pharmacological tools. Br J Pharmacol 153: 140-147.
20. Smith PK, Krohn RI, Hermanson GT, Mallia AK, Gartner FH, Provenzano MD, et al,. (1985). Measurement of protein using bicinchoninic acid. Anal Biochem 150: 76-85.
21. Spiegel S, Milstein S, (2003). Sphingosine-1-phosphate: an enigmatic signalling lipid. Nat Rev Mol Cell Biol 4: 397-407.
22. Strange PG, (1999). G protein coupled receptors: conformations and states. Biochem Pharmacol 58: 1081-1088.
23. Violin JD, Lefkowitz RJ, (2007). β-Arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci 28: 416-422.