Impedance measurement: A new method to detect ligand-biased receptor signaling

Biochemical and Biophysical Research Communications

Volumn 412, Issue 3, 2011, Pages 419-424

  Kammermann, M ^a   Denelavas, A ^a   Imbach, A ^a   Grether, U ^b   Dehmlow, H ^b   Apfel, C M ^a   Hertel, C ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b UNIVERSITY OF BASEL   (Switzerland)

Author keywords

Arrestin; GPR109A; Impedance; Ligand biased receptor signaling

Indexed keywords

BETA ARRESTIN; G PROTEIN COUPLED RECEPTOR; GPR109A NIACIN RECEPTOR; UNCLASSIFIED DRUG;

ARTICLE; CELLULAR IMPEDANCE; CONTROLLED STUDY; FLUSHING; HUMAN; HUMAN CELL; IMPEDANCE; PRIORITY JOURNAL; PROTEIN INDUCTION; SIGNAL TRANSDUCTION;

ANIMALS; CELL LINE; ELECTRIC IMPEDANCE; HUMANS; LIGANDS; MICE; NIACIN; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NICOTINIC; SIGNAL TRANSDUCTION; TRIGLYCERIDES;

MUS;

EID: 80052273428     PISSN: 0006291X     EISSN: 10902104     Source Type: Journal    
DOI: 10.1016/j.bbrc.2011.07.087     Document Type: Article

References (24)

1. Schulte G., Levy F.O. Novel aspects of G-protein-coupled receptor signalling - different ways to achieve specificity. Acta Physiologica 2007, 190:33-38.
2. Schwartz T.W., Holst B. Allosteric enhancers, allosteric agonists and ago-allosteric modulators: where do they bind and how do they act?. Trends in Pharmacological Sciences 2007, 28:366-373.
3. Shenoy S.K., McDonald P.H., Kohout T.A., Lefkowitz R.J. Regulation of receptor fate by ubiquitination of activated β2-adrenergic receptor and β-arrestin. Science 2001, 294:1307-1313.
4. Drake M.T., Violin J.D., Whalen E.J., Wisler J.W., Shenoy S.K., Lefkowitz R.J. β-arrestin-biased agonism at the β2-adrenergic receptor. Journal of Biological Chemistry 2008, 283:5669-5676.
5. Wisler J.W., DeWire S.M., Whalen E.J., Violin J.D., Drake M.T., Ahn S., Shenoy S.K., Lefkowitz R.J. A unique mechanism of β-blocker action: carvedilol stimulates β-arrestin signaling. Proceedings of the National Academy of Sciences 2007, 104:16657-16662.
6. Violin J., Lefkowitz R. β-arrestin-biased ligands at seven-transmembrane receptors. Trends in Pharmacological Sciences 2007, 28:416-422.
7. Walters R.W., Shukla A.K., Kovacs J.J., Violin J.D., DeWire S.M., Lam C.M., Chen J.R., Muehlbauer M.J., Whalen E.J., Lefkowitz R.J. β-arrestin1 mediates nicotinic acid-induced flushing but not its antilipolytic effect, in mice. The Journal of Clinical Investigation 2009, 119:1312-1321.
8. Kebig A., Kostenis E., Mohr K., Mohr-Andrae M. An optical dynamic mass redistribution assay reveals biased signaling of dualsteric GPCR activators. Journal of Receptor and Signal Transduction 2009, 29:140-145.
9. Peters M.F., Scott C.W. Evaluating cellular impedance assays for detection of GPCR pleiotropic signaling and functional selectivity. Journal of Biomolecular Screening 2009, 14:246-255.
10. Rocheville M., Jerman J.C. 7TM pharmacology measured by label-free: a holistic approach to cell signalling. Current Opinion in Pharmacology 2009, 9:643-649.
11. Yu N., Atienza J.M., Bernard J., Blanc S., Zhu J., Wang X., Xu X., Abassi Y.A. Real-time monitoring of morphological changes in living cells by electronic cell sensor arrays: an approach to study G protein-coupled receptors. Analytical Chemistry 2006, 78:35-43.
12. Abassi Y.A., Xi B., Zhang W., Ye P., Kirstein S.L., Gaylord M.R., Feinstein S.C., Wang X., Xu X. Kinetic cell-based morphological screening: prediction of mechanism of compound action and off-target effects. Chemistry and Biology 2009, 16:712-723.
13. Schroder R., Janssen N., Schmidt J., Kebig A., Merten N., Hennen S., Muller A., Blattermann S., Mohr-Andra M., Zahn S., Wenzel J., Smith N.J., Gomeza J., Drewke C., Milligan G., Mohr K., Kostenis E. Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements. Nature Biotechnology 2010, 28:943-949.
14. Atienza J.M., Zhu L., Wang X., Xu X., Abassi Y.A. Dynamic monitoring of cell adhesion and spreading on microelectronic sensor arrays. Journal of Biomolecular Screening 2005, 10:795-805.
15. Atienza J.M., Yu N., Wang X., Xu X., Abassi Y.A. Label-free and real-time cell-based assay for screening selective and potent receptor tyrosine kinase inhibitors using microelectronic sensor array. Journal of Biomolecular Screening 2006, 11:634-643.
16. Xing J.Z., Zhu L., Jacson J.O., Gabos S., Sun X.-J., Wang W.-B., Xu X. Dynamic monitoring of cytotoxicity on microelectronic sensors. Chemical Research in Toxicology 2005, 18:114-161.
17. D.P. Behan, D.T. Connolly, J.G. Richman, Compositions for treating flushing and lipid-associated disorders comprising pyrazole compounds as niacin receptor partial agonists, WO 2006052569, 2006.
18. G. Semple, T. Schrader, P.J. Skinner, S.L. Colletti, T. Gharbaoui, J.E. Imbriglio, J.K. Jung, R. Liang, S. Raghavan, D. Schmidt, J.R. Tata, A preparation of tetrazole derivatives, useful as a modulators of RUP25 receptor, WO 2005044816, 2005.
19. Benyó Z., Gille A., Bennett C.L., Clausen B.E., Offermanns S. Nicotinic acid-induced flushing is mediated by activation of epidermal langerhans cells. Molecular Pharmacology 2006, 70:1844-1849.
20. Lad P.M., Nielsen T.B., Rodbell M. A probe for the organization of the [beta]-adrenergic receptor-regulated adenylate cyclase system in turkey erythrocyte membranes by the use of a complementation assay. FEBS Letters 1980, 122:179-183.
21. Katada T., Oinuma M., Kusakabe K., Ui M. A new GTP-binding protein in brain tissues serving as the specific substrate of islet-activating protein Pertussis toxin. FEBS Letters 1987, 213:353-358.
22. Liu W.S., Heckman C.A. The sevenfold way of PKC regulation. Cellular Signalling 1998, 10:529-542.
23. Richman J.G., Kanemitsu-Parks M., Gaidarov I., Cameron J.S., Griffin P., Zheng H., Guerra N.C., Cham L., Maciejewski-Lenoir D., Behan D.P., Boatman D., Chen R., Skinner P., Ornelas P., Waters M.G., Wright S.D., Semple G., Connolly D.T. Nicotinic acid receptor agonists differentially activate downstream effectors. Journal of Biological Chemistry 2007, 282:18028-18036.
24. Semple G., Skinner P.J., Gharbaoui T., Shin Y.-J., Jung J.-K., Cherrier M.C., Webb P.J., Tamura S.Y., Boatman P.D., Sage C.R., Schrader T.O., Chen R., Colletti S.L., Tata J.R., Waters M.G., Cheng K., Taggart A.K., Cai T.-Q., Carballo-Jane E., Behan D.P., Connolly D.T., Richman J.G. 3-(1H-Tetrazol-5-yl)-1, 4, 5, 6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-Protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice. Journal of Medicinal Chemistry 2008, 51:5101-5108.