Development of a FLIPR assay for the simultaneous identification of MrgD agonists and antagonists from a single screen

Journal of Biomedicine and Biotechnology

Volumn 2010, Issue , 2010, Pages

  Ajit, Seena K ^a,b   Pausch, Mark H ^b   Kennedy, Jeffrey D ^b   Kaftan, Edward J ^b  

^a DREXEL UNIVERSITY COLLEGE OF MEDICINE   (United States)

^b PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 AMINO 1 HYDROXY 2 PYRROLIDINONE; 5,7 DIHYDROXYTRYPTAMINE CREATININE SULFATE; 8 [4 (2 AMINOETHYLCARBAMOYL)METHOXYPHENYL] 1,3 DIPROPYLXANTHINE; BETA ALANINE; CHLORPROMAZINE; G PROTEIN COUPLED RECEPTOR; NERVE PROTEIN; PROPYLNORAPOMORPHINE; PROTEIN MRGD; RECEPTOR BLOCKING AGENT; THIORIDAZINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CALCIUM MOBILIZATION; CONTROLLED STUDY; DRUG IDENTIFICATION; FLUOROMETRY; NERVE CELL; NONHUMAN; NUCLEOTIDE SEQUENCE; PROTEIN DETERMINATION; PROTEIN EXPRESSION;

ANIMALS; CELL LINE; CHO CELLS; CRICETINAE; CRICETULUS; DRUG DISCOVERY; FLUOROMETRY; HUMANS; KINETICS; NOCICEPTORS; RATS; RECEPTORS, G-PROTEIN-COUPLED; RECOMBINANT PROTEINS; SMALL MOLECULE LIBRARIES;

RODENTIA;

EID: 77957836233     PISSN: 11107243     EISSN: 11107251     Source Type: Journal    
DOI: 10.1155/2010/326020     Document Type: Article

References (35)

1. Overington J. P., Al-Lazikani B., Hopkins A. L., How many drug targets are there? Nature Reviews Drug Discovery 2006 5 12 993 996
2. Civelli O., Saito Y., Wang Z., Nothacker H.-P., Reinscheid R. K., Orphan GPCRs and their ligands Pharmacology and Therapeutics 2006 110 3 525 532
3. Dong X., Han S.-K., Zylka M. J., Simon M. I., Anderson D. J., A diverse family of GPCRs expressed in specific subsets of nociceptive sensory neurons Cell 2001 106 5 619 632
4. Lembo P. M. C., Grazzini E., Groblewski T., O'Donnell D., Roy M.-O., Zhang J., Hoffert C., Cao J., Schmidt R., Pelletier M., Labarre M., Gosselin M., Fortin Y., Banville D., Shen S. H., Strm P., Payza K., Dray A., Walker P., Ahmad S., Proenkephalin A gene products activate a new family of sensory neuron-specific GPCRs Nature Neuroscience 2002 5 3 201 209
5. Zylka M. J., Dong X., Southwell A. L., Anderson D. J., Atypical expansion in mice of the sensory neuron-specific Mrg G protein-coupled receptor family Proceedings of the National Academy of Sciences of the United States of America 2003 100 17 10043 10048
6. Robas N., Mead E., Fidock M., MrgX2 is a high potency cortistatin receptor expressed in dorsal root ganglion The Journal of Biological Chemistry 2003 278 45 44400 44404
7. Grazzini E., Puma C., Roy M.-O., Yu X. H., O'Donnell D., Schmidt R., Dautrey S., Ducharme J., Perkins M., Panetta R., Laird J. M. A., Ahmad S., Lembo P. M. C., Sensory neuron-specific receptor activation elicits central and peripheral nociceptive effects in rats Proceedings of the National Academy of Sciences of the United States of America 2004 101 18 7175 7180
8. Han S.-K., Dong X., Hwang J.-I., Zylka M. J., Anderson D. J., Simon M. I., Orphan G protein-coupled receptors Mrga1 and Mrgc11 are distinctively activated by RF-amide-related peptides through the G q/11 pathway Proceedings of the National Academy of Sciences of the United States of America 2002 99 23 14740 14745
9. Shinohara T., Harada M., Ogi K., Maruyama M., Fujii R., Tanaka H., Fukusumi S., Komatsu H., Hosoya M., Noguchi Y., Watanabe T., Moriya T., Itoh Y., Hinuma S., Identification of a G protein-coupled receptor specifically responsive to -alanine The Journal of Biological Chemistry 2004 279 22 23559 23564
10. Kunapuli P., Lee S., Zheng W., Alberts M., Kornienko O., Mull R., Kreamer A., Hwang J.-I., Simon M. I., Strulovici B., Identification of small molecule antagonists of the human mas-related gene-X1 receptor Analytical Biochemistry 2006 351 1 50 61
11. Zhang R., Yan P.-K., Zhou C.-H., Liao J.-Y., Wang M.-W., Development of a homogeneous calcium mobilization assay for high throughput screening of mas-related gene receptor agonists Acta Pharmacologica Sinica 2007 28 1 125 131
12. Nawoschik S. P., Olsen M., Smith D. L., Khawaja X., Stable expression of adenylyl cyclase 2 leads to the functional rescue of human 5-HT6 receptor in a CHODUKX cell line Journal of Pharmacological and Toxicological Methods 2007 55 3 323 331
13. Zylka M. J., Rice F. L., Anderson D. J., Topographically distinct epidermal nociceptive circuits revealed by axonal tracers targeted to Mrgprd Neuron 2005 45 1 17 25
14. Crozier R. A., Ajit S. K., Kaftan E. J., Pausch M. H., MrgD activation inhibits KCNQ/M-currents and contributes to enhanced neuronal excitability Journal of Neuroscience 2007 27 16 4492 4496
15. Cavanaugh D. J., Lee H., Lo L., Shields S. D., Zylka M. J., Basbaum A. I., Anderson D. J., Distinct subsets of unmyelinated primary sensory fibers mediate behavioral responses to noxious thermal and mechanical stimuli Proceedings of the National Academy of Sciences of the United States of America 2009 106 22 9075 9080
16. Ogita K., Suzuki T., Yoneda Y., Strychnine-insensitive binding of [3H]glycine to synaptic membranes in rat brain, treated with triton X-100 Neuropharmacology 1989 28 11 1263 1270 (Pubitemid 19277042)
17. Pullan L. M., Powel R. J., Comparison of binding at strychnine-sensitive (inhibitory glycine receptor) and strychnine-insensitive (N-methyl-D-aspartate receptor) glycine binding sites Neuroscience Letters 1992 148 1-2 199 201
18. Wu F. S., Gibbs T. T., Farb D. H., Dual activation of GABAA and glycine receptors by beta-alanine: inverse modulation by progesterone and 5 alpha-pregnan-3 alpha-ol-20-one The European Journal of Pharmacology 1993 246 239 246
19. Rajendra S., Lynch J. W., Schofield P. R., The glycine receptor Pharmacology and Therapeutics 1997 73 2 121 146
20. Wang Z., Takahashi T., Saito Y., Nagasaki H., Ly N. K., Nothacker H.-P., Reinscheid R. K., Yang J., Chang J. K., Shichiri M., Civelli O., Salusin is a surrogate ligand of the mas-like G protein-coupled receptor MrgA1 European Journal of Pharmacology 2006 539 3 145 150
21. Marks N., Datta R. K., Lajtha A., Distribution of amino acids and of exo- and endopeptidases along vertebrate and invertebrate nerves Journal of Neurochemistry 1970 17 1 53 63
22. Tallan H. H., Moore S., Stein W. H., Studies on the free amino acids and related compounds in the tissues of the cat The Journal of Biological Chemistry 1954 211 2 927 939
23. Yang Z.-Q., Agonists and antagonists for group III metabotropic glutamate receptors 6, 7 and 8 Current Topics in Medicinal Chemistry 2005 5 9 913 918
24. Yang S.-Y., Kao Yang Y.-H., Chong M.-Y., Yang Y.-H., Chang W.-H., Lai C.-S., Risk of extrapyramidal syndrome in schizophrenic patients treated with antipsychotics: a population-based study Clinical Pharmacology and Therapeutics 2007 81 4 586 594
25. Peroutka S. J., Snyder S. H., Relationship of neuroleptic drug effects at brain dopamine, serotonin, -adrenergic, and histamine receptors to clinical potency American Journal of Psychiatry 1980 137 12 1518 1522
26. Raess B. U., Vincenzi F. F., Calmodulin activation of red blood cell (Ca2++Mg2+)-ATPase and its antagonism by phenothiazines Molecular Pharmacology 1980 18 2 253 258
27. Palacios M., Padron J., Glaria L., Rojas A., Delgado R., Knowles R., Moncada S., Chlorpromazine inhibits both the constitutive nitric oxide synthase and the induction of nitric oxide synthase after LPS challenge Biochemical and Biophysical Research Communications 1993 196 1 280 286
28. Drinkwater C., Twycross R. G., Analgesia in terminal malignant disease British Medical Journal 1979 1 6172 1201 1202
29. Mclver B., Walsh D., Nelson K., The use of chlorpromazine for symptom control in dying cancer patients Journal of Pain and Symptom Management 1994 9 5 341 345
30. Harrigan E. P., Miceli J. J., Anziano R., Watsky E., Reeves K. R., Cutler N. R., Sramek J., Shiovitz T., Middle M., A randomized evaluation of the effects of six antipsychotic agents on QTc, in the absence and presence of metabolic inhibition Journal of Clinical Psychopharmacology 2004 24 1 62 69
31. Reilly J. G., Ayis S. A., Ferrier I. N., Jones S. J., Thomas S. H. L., Thioridazine and sudden unexplained death in psychiatric in-patients British Journal of Psychiatry 2002 180 515 522
32. Drolet B., Vincent F., Rail J., Chahine M., Deschenes D., Nadeau S., Khalifa M., Hamelin B. A., Turgeon J., Thioridazine lengthens repolarization of cardiac ventricular myocytes by blocking the delayed rectifier potassium current Journal of Pharmacology and Experimental Therapeutics 1999 288 3 1261 1268 (Pubitemid 29254167)
33. Tie H., Walker B. D., Singleton C. B., Bursill J. A., Wyse K. R., Campbell T. J., Valenzuela S. M., Breit S. N., Clozapine and sudden death Journal of Clinical Psychopharmacology 2001 21 6 630 632
34. Thanacoody R. H. K., Daly A. K., Reilly J. G., Ferrier I. N., Thomas S. H. L., Factors affecting drug concentrations and QT interval during thioridazine therapy Clinical Pharmacology and Therapeutics 2007 82 5 555 565
35. Foster A. C., Kemp J. A., HA-966 antagonizes N-methyl-D-aspartate receptors through a selective interaction with the glycine modulatory site Journal of Neuroscience 1989 9 6 2191 2196