The agonist SR 146131 and the antagonist SR 27897 occupy different sites on the human CCK1 receptor

European Journal of Pharmacology

Volumn 400, Issue 2-3, 2000, Pages 185-194

  Gouldson, Paul ^a   Legoux, Pascale ^a   Carillon, Christine ^a   Delpech, Bruno ^a   Le Fur, Gérard ^a   Ferrara, Pascual ^a   Shire, David ^a  

^a SANOFI   (France)

Author keywords

Binding site; CCK1 receptor; Modelling; SR 146131; SR 27897

Indexed keywords

2 [4 (4 CHLORO 2,5 DIMETHOXYPHENYL) 5 (2 CYCLOHEXYL ETHYL)THIAZOL 2 YLCARBAMOYL] 5,7 DIMETHYL INDOYL 1 YL 1 ACETIC ACID; 2 [4 (4 CHLORO 2,5 DIMETHOXYPHENYL) 5 (2 CYCLOHEXYLETHYL)THIAZOL 2 YLCARBAMOYL] 5,7 DIMETHYLINDOL 1 YLACETIC ACID; CHOLECYSTOKININ OCTAPEPTIDE; CHOLECYSTOKININ RECEPTOR; CHOLECYSTOKININ RECEPTOR BLOCKING AGENT; LINTITRIPT; MUTANT PROTEIN; RECEPTOR SUBTYPE; RECOMBINANT PROTEIN; UNCLASSIFIED DRUG;

AMINO ACID COMPOSITION; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; CELL STRAIN COS1; CONTROLLED STUDY; DRUG RECEPTOR BINDING; HUMAN; IN VITRO STUDY; MODEL; MUTANT; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; STRUCTURE ACTIVITY RELATION;

AMINO ACID SEQUENCE; ANIMALS; BINDING SITES; BINDING, COMPETITIVE; COS CELLS; HORMONE ANTAGONISTS; HUMANS; INDOLEACETIC ACIDS; INDOLES; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; POINT MUTATION; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY; RECEPTORS, CHOLECYSTOKININ; THIAZOLES;

EID: 0034698260     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(00)00414-3     Document Type: Article

References (26)

1. Asano M., Hatori C., Sawai H., Johki S., Inamura N., Kayakiri H., Satoh S., Abe Y., Inoue T., Sawada Y., Mizutani T., Oku T., Nakahara K. Pharmacological characterisation of a non-peptide bradykinin B2 receptor antagonist, FR165649, and agonist, FR190997. Br. J. Pharmacol. 124:1998;441-446.
2. Bignon E., Bachy A., Boigegrain R., Brodin R., Cottineau M., Gully D., Herbert J.-M., Keane P., Labie C., Molimard J.-C., Olliero D., Oury-Donat F., Petereau C., Prabonneaud V., Rockstroh M.-P., Schaeffer P., Servant O., Thurneyssen O., Soubrié P., Pascal M., Maffrand J.-P., LeFur G. SR146131: a new, potent, orally active and selective non-peptide cholecystokinin subtype I receptor agonist: I. In vitro studies. J. Pharmacol. Exp. Ther. 289:1999;742-751.
3. Crawley J.N., Corwin R.L. Biological actions of cholecystokinin. Peptides. 15:1994;731-755.
4. Gigoux V., Maigret B., Escrieut C., Silvente-Poirot S., Bouisson M., Fehrentz J.A., Moroder L., Gully D., Martinez J., Vaysse N., Fourmy D. Arginine 197 of the cholecystokinin-A receptor binding site interacts with the sulfate of the peptide agonist cholecystokinin. Protein Sci. 8:1999;2347-2354.
5. Gigoux V., Escrieut C., Fehrentz J.A., Poirot S., Maigret B., Moroder L., Gully D., Martinez J., Vaysse N., Fourmy D. Arginine 336 and asparagine 333 of the human cholecystokinin-A receptor binding site interact with the penultimate aspartic acid and the C-terminal amide of cholecystokinin. J. Biol. Chem. 274:1999;20457-20464.
6. 2-adrenergic receptor from the evolutionary trace method. Int. J. Quantum Chem., Biophys. Q. 74:1999;371-379.
7. 2-adrenergic receptors. J. Med. Chem. 38:1995;4080-4086.
8. 2-adrenergic receptor that exploits the domain structure of G-protein-coupled receptors. J. Med. Chem. 40:1997;3871-3886.
9. 1 receptor for antagonist SR 27897 and agonist SR 146131 binding. Eur. J. Pharmacol. 383:1999;341-348.
10. 1 receptor for interactions with SR 146131, SR 27897 and CCK-8S. Eur. J. Pharmacol. 389:2000;115-124.
11. Gully D., Fréhel D., Marcy C., Spinazzé A., Lespy L., Neliat G., Maffrand J.P., Le Fur G. Peripheral biological activity of SR-27, 897: a new potent non-peptide antagonist of CCK-A receptors. Eur. J. Pharmacol. 232:1993;13-19.
12. Horton R.M., Hunt H.D., Ho S.N., Pullen J.K., Pease L.R. Engineering hybrid genes without the use of restriction enzymes: gene splicing by overlap extension. Gene. 77:1989;61-68.
13. Kopin A.S., McBride E.W., Quinn S.M., Kolakowski L.F., Beinborn M. The role of the cholecystokinin-B gastrin receptor transmembrane domains in determining affinity for subtype-selective ligands. J. Biol. Chem. 270:1995;5019-5023.
14. Krebs A., Villa C., Edwards P.C., Schertler G.F.X. Characterisation of an improved two-dimensional p22121 crystal from bovine rhodopsin. J. Mol. Biol. 282:1998;991-1003.
15. Liu S., Crider A.M., Tang C., Ho B., Ankersen M., Stidsen C.E. 2-Pyridylthioureas: novel nonpeptide somatostatin agonists with SST4 selectivity. Curr. Pharm. Des. 5:1999;255-263.
16. Miloux B., Lupker J.H. Rapid isolation of highly productive recombinant Chinese Hamster Ovary cell lines. Gene. 149:1994;341-344.
17. Oliveira L., Paiva A.M., Vriend G. A common motif in G-protein-coupled seven transmembrane helix receptors. J. Comput.-Aided Mol. Des. 7:1993;649-658.
18. 1 ligands: susceptibility to receptor mutations. Mol. Pharmacol. 51:1997;301-311.
19. Silvente-Poirot S., Escrieut C., Wank S.A. Role of the extracellular domains of the cholecystokinin receptor in agonist binding. Mol. Pharmacol. 54:1998;364-371.
20. Vita N., Oury-Donat F., Chalon P., Guillemot M., Kaghad M., Bachy A., Thurneyssen O., Garcia S., Poinot-Chazel C., Casellas P., Keane P., Le Fur G., Maffrand J.P., Soubrie P., Caput D., Ferrara P. Neurotensin is an antagonist of the human neurotensin NT2 receptor expressed in Chinese hamster ovary cells. Eur. J. Pharmacol. 360:1998;265-272.
21. Vriend G. WHATIF: a molecular modelling and drug design program. J. Mol. Graphics. 8:1990;52-56.
22. Wank S.A. Cholecystokinin receptors. Am. J. Physiol. 32:1995;G628-G646.
23. Wank S.A. G protein-coupled receptors in gastrointestinal physiology: I. CCK receptors - an exemplary family. Am. J. Physiol. 37:1998;G607-G613.
24. Wank S.A., Harkins R.T., Jensen R.T., Shapira H., De Weerth A., Slattery T. Purification, molecular cloning, and functional expression of the cholecystokinin receptor from rat pancreas. Proc. Natl. Acad. Sci. U. S. A. 89:1992;3125-3129.
25. Wank S.A., Pisegna J.R., De Weerth A. Brain and gastrointestinal cholecystokinin receptor family: structure and functional expression. Proc. Natl. Acad. Sci. U. S. A. 89:1992;8691-8695.
26. Yang L., Berk S.C., Rohrer S.P., Mosley R.T., Guo L., Underwood D.J., Arison B.H., Birzin E.T., Hayes E.C., Mitra S.W., Parmar R.M., Cheng K., Wu T.J., Butler B.S., Foor F., Pasternak A., Pan Y., Silva M., Freidinger R.M., Smith R.G., Chapman K., Schaeffer J.M., Patchett A.A. Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. Proc. Natl. Acad. Sci. U. S. A. 95:1998;10836-10841.