Studying Ligand Efficacy at G Protein-Coupled Receptors Using FRET

Methods in Molecular Biology

Volumn 756, Issue , 2011, Pages 133-148

  Vilardaga, Jean Pierre ^a  

^a UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE   (United States)

Author keywords

Conformational changes; FlAsH labeling; F rster resonance energy transfer; G protein coupled receptor; GPCR heterodimer; GPCR polymorphisms; Heterotrimeric G proteins; Ligand efficacy; 2A Adrenergic receptor; 1 Adrenergic receptor

Indexed keywords

G PROTEIN COUPLED RECEPTOR; LIGAND;

ANIMAL; ARTICLE; CELL LINE; DRUG DEVELOPMENT; DRUG POTENTIATION; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMAN; METABOLISM; METHODOLOGY; PROTEIN MULTIMERIZATION;

ANIMALS; CELL LINE; DRUG DISCOVERY; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMANS; LIGANDS; PROTEIN MULTIMERIZATION; RECEPTORS, G-PROTEIN-COUPLED;

EID: 80054775036     PISSN: 10643745     EISSN: 19406029     Source Type: Book Series    
DOI: 10.1007/978-1-61779-160-4_6     Document Type: Chapter

References (17)

1. Kendall, R.T., and Luttrell, L.M. (2009) Diversity in arrestin function. Cell Mol Life Sci 66, 2953–73.
2. Neubig, R.R., Spedding, M., Kenakin, T., and Christopoulos, A. (2003) International union of pharmacology nomemclature and rug classification. Upadate on tgerms and symbols in quantitative pharmacology. Pharmcol Rev 55, 597–606.
3. Ciccarelli, E., Vilardaga, J.-P., De Neef, P., DiPaolo, E., Waelbroeck, M., Bollen, A., and Robberecht, P. (1994) Properties of the VIP-PACAP type II receptor stably expressed in CHO cells. Regulatory Peptides 54, 397–407.
4. Perrin, J. Théorie quantique des transferts d’activation entre molécules de même espèce. (1932) Cas des solutions fluorescentes. Ann Chim Phys 17, 283–313.
5. Förster, T. (1948) Zwischenmolekulare Energiewanderung und Fluoreszenz. Ann Physik (Leipzig) 2, 55–75.
6. Vilardaga, J.-P., Bünemann, M., Feinstein, T.N., Lambert, N., Nikolaev, V.O., Engelhardt, S., Lohse, M.J., and Hoffmann, C. (2009) GPCR and G proteins: drug efficacy and activation in live cells. Mol Endocrinol 23, 590–99.
7. Balla, T. (2009) Green light to illuminate signal transduction events. Trends Cell Biol 19, 575–86
8. Vilardaga, J.-P., Bünemann, M., Krasel, C., Castro, M., and Lohse, M.J. (2003) A millisecond activation switch for G protein-coupled receptors in living cells. Nat Biotechnology 21, 807–12.
9. Hoffmann, C., Gaietta,. G., Bünemann, M., Adams, R.S., Oberforff-Maas, S., Behr, B., Vilardaga. J.-P., Tsien, R.Y., Ellisman, M.H., and Lohse, M.J. (2005) A FLASH-based approach to determine G protein-coupled receptor activation in living cells. Nature Methods 2, 171–76.
10. Ferrandon, S., Feinstein, T.N., Castro, C., Bouley, R., Potts, J.T., Gardella, T.J., and Vilardaga, J.-P. (2009) Sustained cyclic AMP production by parathyroid hormone receptor endocytosis. Nat Chem Biol 5, 734–42.
11. Vilardaga, J.-P.,, Steinmeyer, R., Harms, G., and Lohse M.J. (2005) Molecular basis of inverse agonism in a G protein-coupled receptor. Nat Chem Biol 1, 25–8.
12. i-protein heterotrimer. J. Biol. Chem. 281, 24506–11.
13. 2A-adrenergic and m-opioid receptors. Nat Chem Biol 4, 126–31.
14. 1-adrenergic receptor activation reveals supersensitivity of the Arg389 variant to carvedilol. (2007) J Clin Invest 117, 229–35.
15. Xia, Z., and Liu, Y. (2001) Reliable and global measurement of fluorescence resonance energy transfer using fluorescence microscopes. (2001) Biophys. J. 81, 2395–02.
16. Ausubel, F. M., Brent, R., Kingston, R. E., Moore, D. D., Seidman, J. G., Smith, J. A., and Struhl, K. (1997) Current Protocols in Molecular Biology. Wiley, New York
17. Hein, P., Frank, M., Hoffmann, C., Lohse, M.J, and Bünemann, M. (2005) Dynamic of receptor/G protein coupling in living cells. EMBO J 24, 4106–14.