A different molecular interaction of bradykinin and the synthetic agonist FR190997 with the human B 2 receptor: Evidence from mutational analysis

British Journal of Pharmacology

Volumn 140, Issue 3, 2003, Pages 500-506

  Bellucci, Francesca ^a   Meini, Stefania ^a   Cucchi, Paola ^a   Catalani, Claudio ^a   Reichert, Wolfgang ^b   Zappitelli, Sabrina ^a   Rotondaro, Luigi ^a   Quartara, Laura ^a   Giolitti, Alessandro ^a   Maggi, Carlo Alberto ^a  

^a Menarini Ricerche SpA   (Italy)

^b IMMUNDIAGNOSTIK AG   (Germany)

Author keywords

B 2 receptor; Binding; Bradykinin; Efficacy; FR190997; Mutagenesis; Nonpeptide

Indexed keywords

8 [2,6 DICHLORO 3 [N [4 (N METHYLCARBAMOYL)CINNAMAMIDOACETYL] N METHYLAMINO]BENZYLOXY] 2 METHYL 4 (2 PYRIDYLMETHOXY)QUINOLINE; BRADYKININ; INOSITOL PHOSPHATE;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; CHO CELL; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; FEMALE; HORMONE RECEPTOR INTERACTION; MOLECULAR INTERACTION; MUTATIONAL ANALYSIS; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; WILD TYPE;

ANIMALS; BRADYKININ; CHO CELLS; CRICETINAE; DNA MUTATIONAL ANALYSIS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MUTATION; PROTEIN BINDING; QUINOLINES; RECEPTOR, BRADYKININ B2;

EID: 10744222336     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0705454     Document Type: Article

References (37)

1. ALTAMURA, M., MEINI, S., QUARTARA, L. & MAGGI, C.A. (1999). Nonpeptide antagonists for kinin receptors. Regul. Pept., 80, 13-26.
2. 2 receptor. Mol. Pharmacol., 52, 16-20.
3. BARTUS, R.T., ELLIOTT, P.J., DEAN, R.L., HAYWARD, N.J., NAGLE, T.L., HUFF, M.R., SNODGRASS, P.A. & BLUNT, D.G. (1996). Controlled modulation of BBB permeability using the bradykinin agonist, RMP-7. Exp. Neurol., 142, 14-28.
4. BAXTER, G.F. & EBRAHIM, Z. (2002). Role of bradykinin in preconditioning and protection of the ischaemic myocardium. Br. J. Pharmacol., 135, 843-854.
5. BEELEY, N.R.A. (2000). Can peptides be mimicked? Drug Discov. Today, 5, 354-363.
6. BLAKER, M., REN, Y., GORDON, M.C., HSU, J.E., BEINBORN, M. & KOPIN, A.S. (1998). Mutations within the cholecystokinin-B/gastrin receptor ligand 'pocket' interconvert the functions of nonpeptide agonists and antagonists. Mol. Pharmacol., 54, 857-863.
7. BLAKER, M., REN, Y., SESHADRI, L., MCBRIDE, E.W., BEINBORN, M. & KOPIN, A.S. (2000). CCK-B/gastrin receptor transmembrane domain mutations selectively alter synthetic agonist efficacy without affecting the activity of endogenous peptides. Mol. Pharmacol., 58, 399-406.
8. 2 receptor in vivo phosphorylation sites and their role in receptor function. J. Biol. Chem., 276, 40431-40440.
9. BRADFORD, M.M. (1976). A rapid and sensitive method for the quantitation of microgram quantities of protein utilising the principle of protein-dye binding. Anal. Biochem., 75, 248-254.
10. COLQUHOUN, D. (1998). Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors. Br. J. Pharmacol., 125, 923-947.
11. CUTHBERT, A.W. (1999). Anion secretory effects of a non-peptide mimic of bradykinin (FR190997) on mouse colon epithelium. Immunopharmacology, 45, 191-198.
12. EGGERICKX, D., RASPE, E., BERTRAND, D., VASSART, G. & PARMENTIER, M. (1992). Molecular cloning, functional expression and pharmacological characterisation of a human bradykinin B2 receptor gene. Biochem. Biophys. Res. Commun., 187, 1306-1313.
13. EMERICH, D.F., DEAN, R.L., OSBORN, C. & BARTUS, R.T. (2001). The development of the bradykinin agonist Labradimil as a means to increase the permeability of the blood-brain barrier. Clin. Pharmacokinet., 40, 105-123.
14. FARMER, S.G., POWELL, S.J., WILKINS, D.E. & GRAHAM, A. (1998). Cloning, sequencing and functional expression of a guinea pig lung bradykinin receptor. Eur. J. Pharmacol., 346, 291-298.
15. GETHER, U. (2000). Uncovering molecular mechanisms involved in activation of G protein-coupled receptors. Endocrine Rev., 21, 90-113.
16. GOBEIL, F., MONTAGNE, M., INAMURA, N. & REGOLI, D. (1999). Characterization of non-peptide bradykinin B2 receptor agonist (FR190997) and antagonist (FR173657). Immunopharmacology, 43, 179-185.
17. HALL, J.M. (1992). Bradykinin receptors: pharmacological properties and biological roles. Pharmacol. Ther., 56, 131-190.
18. HAYASHI, I., ISHIHARA, K., KUMAGAI, Y. & MAJIMA, M. (2001). Proinflammatory characteristics of a nonpeptide bradykinin mimic, FR190997, in vivo. Br. J. Pharmacol., 133, 1296-1306.
19. 2 receptor agonists in the treatment of cardiovascular disease. Expert Opin. Investig. Drugs, 12, 759-770.
20. HESS, J.F., BORKOWSKI, J.A., YOUNG, G.S., STRADER, C.D. & RANSOM, R.W. (1992). Cloning and pharmacological characterization of a human bradykinin (BK-2) receptor. Biochem. Biophys. Res. Commun., 184, 260-268.
21. 1 receptor revealed by G-protein fusions and mutagenesis. J. Biol. Chem., 276, 19793-19799.
22. 2 receptor signalling by increment of regional blood flow around the ischaemic lesions in rats. Br. J. Pharmacol., 138, 225-233.
23. 2 bradykinin receptor reveal a different pattern of contacts for peptidic agonists and peptidic antagonists. J. Biol. Chem., 271, 28277-28286.
24. KENAKIN, T. (1997). Competitive antagonism. Pharmacologic analysis of drug-interaction. 3rd edn., pp. 331-373. Philadelphia: Lippincott-Raven Press Publishers.
25. KENAKIN, T. & ONARAN, O. (2002). The ligand paradox between affinity and efficacy: can you be there and not make a difference? Trends Pharmacol. Sci., 23, 275-280.
26. 2 bradykinin receptor. J. Biol. Chem., 276, 41100-41111.
27. 2 receptor for nonpeptide antagonist ligands recognition. Can. J. Physiol. Pharmacol., 80, 303-309.
28. 2 receptor agonists and antagonists: a reappraisal of their pharmacology in the guinea-pig ileum. Eur. J. Pharmacol., 409, 185-194.
29. MENG, E.C. & BOURNE, H.R. (2001). Receptor activation: what does the rhodopsin structure tell us? Trends Pharmacol. Sci., 22, 587-593.
30. MENKE, J.G., BORKOWSKI, J.A., BIERILO, K.K., MACNEIL, T., DERRICK, A.W., SCHNECK, K.A., RANSOM, R.W., STRADER, C.D., LINEMEYER, D.L. & HESS, J.F. (1994). Expression cloning of a human B1 bradykinin receptor. J. Biol. Chem., 269, 21583-21586.
31. 1 ligands: susceptibility to receptor mutations. Mol. Pharmacol., 51, 301-311.
32. REGOLI, D. & BARABÉ, J. (1980). Pharmacology of bradykinin and related kinins. Pharmacol. Rev., 32, 1-46.
33. 2 receptors. Naunyn-Schmiedeberg's Arch. Pharmacol., 360, 361-367.
34. SANTICIOLI, P., CATALIOTO, R.-M., MEINI, S. & MAGGI, C.A. (2001). Differences in electromechanical coupling between bradykinin and the nonpeptide kinin B2 receptor agonist, FR190997, in the circular muscle of guinea-pig colon. Naunyn-Schmiedeberg's Arch. Pharmacol., 363, 175-181.
35. 1 vascular vasopressin receptor. J. Pharmacol. Exp. Ther., 294, 195-203.
36. UENO, A., NARABA, H., KOJIMA, F., MORITA, E. & OH-ISHI, S. (1999). FR190997, a novel bradykinin B2 agonist, expresses longer action than bradykinin in paw edema formation and hypotensive response. Immunopharmacology, 45, 89-93.
37. 2-antagonists. Jpn. J. Pharmacol., 78, 109-111.