Abstract
Novel fluorescence approaches to investigate ligand recognition and structure of G protein-coupled receptors in native membranes have been developed. These methods combine the biosynthetic incorporation of unnatural fluorescent amino acids at known sites in receptors with the technique of fluorescence energy transfer for distance measurement. This permits one to fix the ligand in space and to define the structure of the receptor in a model of ligand–receptor interactions. Subdomains of ligand binding sites on NK1 and NK2 receptors were also characterized using environment-sensitive fluorophores and the techniques of collisional quenching and anisotropy. Antagonists and agonists have different binding sites on NK1 and NK2.
Similar content being viewed by others
References
Watson, S. and Arkinstall, S. (Eds.) The G Protein-Linked Receptor FactsBook, Academic Press, London, 1994.
Turcatti, G., Nemeth, K., Edgerton, M., Meseth, U., Talabot, F., Peitsch, M., Knowles, J., Vogel, H. and Chollet, A., J. Biol. Chem., 271 (1996) 19991.
Chollet, A., Turcatti, G., Ceszkowski, K. and Bradshaw, C., In Findlay, J. (Ed.) Membrane Protein Models, Bios Scientific Publishers, Oxford, 1996, pp. 177–192.
Bradshaw, C.B., Ceszkowski, K., Turcatti, G., Beresford, I.J.M. and Chollet, A., J. Med. Chem., 37 (1994) 1991.
Turcatti, G., Vogel, H. and Chollet, A., Biochemistry, 34 (1995) 3972.
Turcatti, G., Zoffmann, S., Lowe III, J.A., Drozda, S., Schwartz, T.W. and Chollet, A., J. Biol. Chem., 272 (1997) 21167.
Nemeth, K. and Chollet, A., J. Biol. Chem., 270 (1995) 27601.
Turcatti, G., Nemeth, K., Edgerton, M., Knowles, J., Vogel, H. and Chollet, A., Recept. Channels, (1998) in press.
Förster, T., Ann. Phys. (Leipzig), 2 (1948) 55.
Stryer, L., Annu. Rev. Biochem., 47 (1978) 819.
Baldwin, J., EMBO J., 12 (1993) 1693.
Schertler, G., Villa, C. and Henderson, R., Nature, 362 (1993) 770.
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Chollet, A., Turcatti, G. Mapping the binding sites of peptide and non-peptide molecules to G protein-coupled receptors by fluorescence. Letters in Peptide Science 5, 79–82 (1998). https://doi.org/10.1023/A:1008845130209
Issue Date:
DOI: https://doi.org/10.1023/A:1008845130209