Peptide and nonpeptide antagonist interaction with constitutively active human AT1 receptors

Biochemical Pharmacology

Volumn 65, Issue 8, 2003, Pages 1329-1338

  Le, Minh Tam ^a   Vanderheyden, Patrick M L ^a   Szaszák, M árta ^b   Hunyady, L ászló ^b   Kersemans, Veerle ^c   Vauquelin, Georges ^a  

^a VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

^b SEMMELWEIS UNIVERSITY   (Hungary)

^c GHENT UNIVERSITY   (Belgium)

Author keywords

AT1 receptor; CHO cells; Constitutive mutant; Insurmountable; Nonpeptide antagonist; Surmountable

Indexed keywords

2 BUTYL 4 CHLORO 1 [[2' (1H TETRAZOL 5 YL) 4 BIPHENYLYL]METHYL] 5 IMIDAZOLECARBOXYLIC ACID; ALANINE; ANGIOTENSIN; ANGIOTENSIN 1 RECEPTOR; ANGIOTENSIN 1 RECEPTOR ANTAGONIST; ANGIOTENSIN II [1 SARCOSINE 8 ISOLEUCINE]; ANGIOTENSIN II [3-8]; ASPARAGINE; ASPARTIC ACID; CANDESARTAN; GLYCINE; INOSITOL PHOSPHATE; IRBESARTAN; LIGAND; LOSARTAN; MUTANT PROTEIN; SERINE; TRITIUM;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CELL STIMULATION; CELL STRUCTURE; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DISSOCIATION; DOSE RESPONSE; DRUG EFFECT; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; LONG TERM EXPOSURE; MOLECULAR MIMICRY; MUTATION; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN EXPRESSION; PROTEIN INTERACTION; RECEPTOR BINDING; STIMULATION; WILD TYPE;

EID: 0037446353     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(03)00072-8     Document Type: Article

References (32)

1. De Gasparo M., Catt K.J., Inagami T., Wright J.W., Unger T. International Union of Pharmacology. XXIII. The angiotensin II receptors. Pharmacol. Rev. 52:2000;15-72.
2. Wong P.C., Price W.A., Chiu A.T., Thoolen M.J.M.C., Duncia J.V., Carini D.J., Wexler R.R., Johnson A.L., Timmermans P.B.M.W.M. Nonpeptide angiotensin II receptor antagonists. IX. Pharmacology of EXP3174: an active metabolite of DuP 753, an orally active antihypertensive agent. J. Pharmacol. Exp. Ther. 255:1990;211-217.
3. Timmermans P.B., Wong P.C., Chiu A.T., Herblin W.F., Benfield P., Carini D.J., Lee R.J., Wexler R.R., Saye J.A., Smith R.D. Angiotensin II receptors and angiotensin II receptor antagonists. Pharmacol. Rev. 45:1993;205-251.
4. Burnier M., Brunner H.R. Angiotensin II receptor antagonists. Lancet. 355:2000;637-645.
5. 1 receptors. Br. J. Pharmacol. 126:1999;1057-1065.
6. 1 receptor antagonist. The role of tight antagonist binding. Eur. J. Pharmacol. 372:1999;199-206.
7. Vauquelin G., Morsing P., Fierens F.L., De Backer J.-P., Vanderheyden P.M. A two-state receptor model for the interaction between angiotensin II type 1 receptors and nonpeptide antagonists. Biochem. Pharmacol. 61:2001;277-284.
8. 1 receptor activation. J. Biol. Chem. 277:2002;2310723110.
9. 1 receptor in agonist activation. J. Biol. Chem. 270:1995;28511-28514.
10. 199 mutation of the human angiotensin type 1 receptor differential affects the binding of surmountable and insurmountable nonpeptide antagonists. J. Renin Angiotensin Aldosterone Syst. 1:2000;283-288.
11. 1 receptor-transfected Chinese hamster ovary cells Eur. J. Pharmacol. 367:1999;413-422.
12. 1 angiotensin receptor is generated by angiotensin II induction. Biochemistry. 35:1996;16435-16442.
13. 1 receptor activation is dependent upon two juxtaposed asparagine residues on transmembranz helices III and VII. J. Biol. Chem. 272:1997;4245-4251.
14. 1A angiotensin II receptor induces its constitutive activation. J. Biol. Chem. 272:1997;1822-1826.
15. 1 receptor. J. Biol. Chem. 274:1999;7103-7110.
16. Robinson P.R., Cohen G.B., Zhukovsky E.A., Oprian D.D. Constitutively active mutants of rhodopsin. Neuron. 9:1992;719-725.
17. Perez D.M., Hwa J., Gaivin R., Mathur M., Brown F., Graham R.M. Constitutive activation of a single effector pathway: evidence for multiple activation states of a G protein-coupled receptor. Mol. Pharmacol. 49:1996;112-122.
18. Strader C.D., Sigal I.S., Dixon R.A. Structural basis of beta-adrenergic receptor function. FASEB J. 3:1989;1825-1832.
19. Marie J., Koch C., Pruneau D., Paquet J.L., Groblewski T., Larguier R., Lombard C., Deslauriers B., Maigret B., Bonnafous J.C. Constitutive activation of the human bradykinin B2 receptor induced by mutation in transmembrane helices III and VI. Mol. Pharmacol. 55:1999;92-101.
20. Zhang W.B., Navenot J.M., Haribabu B., Tamamura H., Hiramatu K., Omagari A., Pei G., Manfredi J.P., Fujii N., Broach J.R., Peiper S.C. A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse and that AMD3100 and ALX40-4C are weak partial agonists. J. Biol. Chem. 277:2002;24515-24521.
21. Ishii I., Izumi T., Tsukamoto H., Umeyama H., Ui M., Shimizu T. Alanine exchanges of polar amino acids in the transmembrane domains of a platelet-activating factor receptor generate both constitutively active and inactive mutants. J. Biol. Chem. 272:1997;7846-7854.
22. Monnot C., Bihoreau C., Conchon S., Curnow K.M., Corvol P., Clauser E. Polar residues in the transmembrane domains of the type 1 angiotensin II receptor are required for binding and coupling. Reconstitution of the binding site by co-expression of two deficient mutants. J. Biol. Chem. 271:1996;1507-1513.
23. Groblewski T., Maigret B., Nouet S., Larguier R., Lombard C., Bonnafous J.C., Marie J. Amino acids of the third transmembrane domain of the AT1A angiotensin II receptor are involved in the differential recognition of peptide and nonpeptide ligands. Biochem. Biophys. Res. Commun. 209:1995;153-160.
24. 1 angiotensin receptor. Br. J. Pharmacol. 119:1996;1505-1507.
25. Vauquelin G., Fierens F.L.P., Gáborik Z., Le M.T., De Backer J.-P., Hunyady L., Vanderheyden P.M.L. Role of basic amino acids of the human angiotensin type 1 receptor in the binding of the non-peptide antagonist candesartan. J. Renin Angiotensin Aldosterone Syst. 2:2001;32-36.
26. 1). J. Biol. Chem. 270:1995;14024-14030.
27. Schambye H.T., Hjorth S.A., Bergsma D.J., Sathe G., Schwartz T.W. Differentiation between binding sites for angiotensin II and nonpeptide antagonists on the angiotensin II type 1 receptors. Proc. Natl. Acad. Sci. U.S.A. 91:1994;7046-7050.
28. 1 angiotensin receptor. Identification of amino acid residues that determine binding of the antihypertensive drug losartan. J. Biol. Chem. 269:1994;16533-16536.
29. 1 angiotensin receptor function on adjacent asparagine residues in the seventh transmembrane helix. Mol. Pharmacol. 54:1998;427-434.
30. Vanderheyden P.M.L., Fierens F.L.P., De Backer J.-P., Vauquelin G. Reversible and syntopic interaction between angiotensin receptor antagonists on Chinese hamster ovary cells expressing human angiotensin II type 1 receptors. Biochem. Pharmacol. 59:2000;927-935.
31. 1 receptor is essential for full agonism. J. Biol. Chem. 270:1995;12846-12850.
32. Cheng Y., Prusoff W.H. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 22:1973;3099-3108.