Sartan-AT1 receptor interactions: In vitro evidence for insurmountable antagonism and inverse agonism

Molecular and Cellular Endocrinology

Volumn 302, Issue 2, 2009, Pages 237-243

  Van Liefde, I ^a   Vauquelin, G ^a  

^a VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

Author keywords

AT1 receptors; Cardiomyocytes; G proteins; Insurmountable antagonism; Inverse agonism; Sartans

Indexed keywords

2 BUTYL 4 CHLORO 1 [[2' (1H TETRAZOL 5 YL) 4 BIPHENYLYL]METHYL] 5 IMIDAZOLECARBOXYLIC ACID; ANGIOTENSIN 1 RECEPTOR; CANDESARTAN; GUANINE NUCLEOTIDE BINDING PROTEIN; IRBESARTAN; LOSARTAN; OLMESARTAN; SARTAN DERIVATIVE; TELMISARTAN; VALSARTAN; ANGIOTENSIN RECEPTOR ANTAGONIST;

DRUG ACTIVITY; DRUG ANTAGONISM; DRUG HALF LIFE; DRUG RECEPTOR BINDING; HUMAN; IN VITRO STUDY; MUTATION; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; REVIEW; VASCULAR TISSUE; BINDING COMPETITION; CARDIOMEGALY; DRUG EFFECT; METABOLISM;

ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS; BINDING, COMPETITIVE; CARDIOMEGALY; HUMANS; RECEPTOR, ANGIOTENSIN, TYPE 1;

EID: 62949153839     PISSN: 03037207     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.mce.2008.06.006     Document Type: Review

References (70)

1. 1 receptor and the ligand-binding site. J. Mol. Model. 12 (2006) 325-337
2. 1 receptor activation is dependent upon two juxtaposed asparagine residues on transmembrane helices III and VII. J. Biol. Chem. 272 (1997) 4245-4251
3. Becker B.N., Yasuda T., Kondo S., Vaikunth S., Homma T., and Harris R.C. Mechanical stretch/relaxation stimulates a cellular renin-angiotensin system in cultured rat mesangial cells. Exp. Nephrol. 6 (1998) 57-66
4. 2 angiotensin II receptor antagonists. J. Med. Chem. 48 (2005) 4389-4399
5. Campbell D.J., Alexiou T., Xiao H.D., Fuchs S., McKinley M.J., Corvol P., and Bernstein K.E. Effect of reduced angiotensin-converting enzyme gene expression and angiotensin-converting enzyme inhibition on angiotensin and bradykinin peptide levels in mice. Hypertension 43 (2004) 854-859
6. 1 receptor subtype. Br. J. Pharmacol. 110 (1993) 761-771
7. 1 receptor antagonist, UR-7280. Eur. J. Pharmacol. 318 (1996) 341-347
8. de Gasparo M., Catt K.J., Inagami T., Wright J.W., and Unger T. International Union of Pharmacology. XXIII. The Angiotensin II Receptors. Pharmacol. Rev. 52 (2000) 415-472
9. Dickinson K.E., Cohen R.B., Skwish S., Delaney C.L., Serafino R.P., Poss M.A., Gu Z., Ryono D.E., Moreland S., and Powell J.R. BMS-180560, an insurmountable inhibitor of angiotensin II-stimulated responses: comparison with losartan and EXP3174. Br. J. Pharmacol. 113 (1994) 179-189
10. 1 receptor antagonists: the role of tight antagonist binding. Eur. J. Pharmacol. 372 (1999) 199-206
11. 1 receptor-transfected Chinese hamster ovary cells. Eur. J. Pharmacol. 367 (1999) 413-422
12. 1 receptor differently affects the binding of surmountable and insurmountable non-peptide antagonists. J. Renin-Angiotensin-Aldosterone Syst. 1 (2000) 283-288
13. 3H]candesartan to intact cells and membrane preparations. Biochem. Pharmacol. 63 (2002) 1273-1279
14. Fukunaga T., Yamashiro T., Oya S., Takeshita N., Takigawa M., and Takano-Yamamoto T. Connective tissue growth factor mRNA expression pattern in cartilages is associated with their type I collagen expression. Bone 33 (2003) 911-918
15. Gether U. Uncovering molecular mechanisms involved in activation of G protein-coupled receptors. Endocr. Rev. 21 (2000) 90-113
16. Giraldo J. Agonist induction, conformational selection, and mutant receptors. FEBS Lett. 556 (2004) 13-18
17. 1A angiotensin II receptor induces its constitutive activation. J. Biol. Chem. 272 (1997) 1822-1826
18. Hara M., Tozawa F., Itazaki K., Mihara S., and Fujimoto M. Endothelin ET(B) receptors show different binding profiles in intact cells and cell membrane preparations. Eur. J. Pharmacol. 345 (1998) 339-342
19. Harada K., Komuro I., Shiojima I., Hayashi D., Kudoh S., Mizuno T., Kijima K., Matsubara H., Sugaya T., Murakami K., and Yazaki Y. Pressure overload induces cardiac hypertrophy in angiotensin II type 1A receptor knockout mice. Circulation 97 (1998) 1952-1959
20. Hulme E.C., Lu Z.L., Ward S.D., Allman K., and Curtis C.A. The conformational switch in 7-transmembrane receptors: the muscarinic receptor paradigm. Eur. J. Pharmacol. 375 (1999) 247-260
21. Hunyady L., Vauquelin G., and Vanderheyden P. Agonist induction and conformational selection during activation of a G-protein-coupled receptor. Trends Pharmacol. Sci. 24 (2003) 81-86
22. Iekushi K., Taniyama Y., Azuma J., Katsuragi N., Dosaka N., Sanada F., Koibuchi N., Nagao K., Ogihara T., and Morishita R. Novel mechanisms of valsartan on the treatment of acute myocardial infarction through inhibition of the antiadhesion molecule periostin. Hypertension 49 (2007) 1409-1414
23. Kenakin T. The classification of seven transmembrane receptors in recombinant expression systems. Pharmacol. Rev. 48 (1996) 413-463
24. Kudoh S., Komuro I., Hiroi Y., Zou Y., Harada K., Sugaya T., Takekoshi N., Murakami K., Kadowaki T., and Yazaki Y. Mechanical stretch induces hypertrophic responses in cardiac myocytes of angiotensin II type 1a receptor knockout mice. J. Biol. Chem. 273 (1998) 24037-24043
25. Lal H., Verma S.K., Smith M., Guleria R.S., Lu G., Foster D.M., and Dostal D.E. Stretch-induced MAP kinase activation in cardiac myocytes: differential regulation through beta1-integrin and focal adhesion kinase. J. Mol. Cell. Cardiol. 43 (2007) 137-147
26. 1 receptor activation. J. Biol. Chem. 277 (2002) 23107-23110
27. 1 receptors. Biochem. Pharmacol. 65 (2003) 1329-1335
28. 1 antagonism and insurmountability: comparison of olmesartan and telmisartan. Br. J. Pharmacol. 151 (2007) 952-962
29. 2-like receptors. Can they be classified with the available antagonists?. Br. J. Pharmacol. 88 (1986) 585-593
30. Lindström E., von Mentzer B., Påhlman I., Ahlstedt I., Uvebrant A., Kristensson E., Eriksson R., Novén A., de Verdier J., and Vauquelin G. Neurokinin (NK)1 receptor antagonists: correlation between in vitro receptor interaction and in vivo efficacy. J. Pharmacol. Exp. Ther. 322 (2007) 1286-1293
31. Milligan G. Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective. Mol. Pharmacol. 64 (2003) 1271-1276
32. Miura S., Saku K., and Karnik S.S. Molecular analysis of the structure and function of the angiotensin II type 1 receptor. Hypertens. Res. 26 (2003) 937-943
33. Miura S., Fujino M., Hanzawa H., Kiya Y., Imaizumi S., Matsuo Y., Tomita S., Uehara Y., Karnik S.S., Yanagisawa H., Koike H., Komuro I., and Saku K. Molecular mechanism underlying inverse agonist of angiotensin II type 1 receptor. J. Biol. Chem. 281 (2006) 19288-19295
34. Miura S., Kiya Y., Kanazawa T., Imaizumi S., Fujino M., Matsuo Y., Karnik S.S., and Saku K. Differential bonding interactions of inverse agonists of angiotensin II type 1 receptor in stabilizing the inactive state. Mol. Endocrinol. 22 (2008) 139-146
35. Mochizuki S., Sato T., Furata K., Hase K., Ohkura Y., Fukai C., Kosakai K., Wakabayashi A., and Tomiyama A. Pharmacological properties of KT3-671, a novel nonpeptide angiotensin II receptor antagonist. J. Cardiovasc. Pharmacol. 25 (1995) 22-29
36. 1-dependent signalling in bladder smooth muscle cells. Am. J. Physiol. Cell. Physiol. 279 (2000) C1155-C1167
37. Noda M., Shibouta Y., Inada Y., Ojima M., Wada T., Sanada T., Kubo K., Kohara Y., Naka T., and Nishikawa K. Inhibition of rabbit aoritc angiotensin II (AII) receptor by CV-11974, a new neuropeptide AII antagonist. Biochem. Pharmacol. 46 (1993) 311-318
38. 1 receptor in agonist activation. J. Biol. Chem. 270 (1995) 28511-28514
39. 1 angiotensin receptor is generated by angiotensin II induction. Biochemistry 35 (1996) 16435-16442
40. Norris K., and Vaughn C. The role of renin-angiotensin-aldosterone system inhibition in chronic kidney disease. Expert Rev. Cardiovasc. Ther. 1 (2003) 51-63
41. Oparil S. Newly emerging pharmacologic differences in angiotensin II receptor blockers. Am. J. Hypertens. 13 (2000) 18S-24S
42. Oro C., Qian H., and Thomas W.G. Type 1 angiotensin receptor pharmacology: signalling beyond G proteins. Pharmacol. Ther. 113 (2007) 210-226
43. Packeu A., De Backer J.-P., Van Liefde I., Vanderheyden P., and Vauquelin G. Antagonist-dopamine D2L-receptor interactions in intact cells. Biochem. Pharmacol. 75 (2008) 2192-2203
44. Park J.M., Borer J.G., Freeman M.R., and Peters C.A. Stretch activates heparin-binding EGF-like growth factor expression in bladder smooth muscle cells. Am. J. Physiol. 275 (1998) C1247-C1254
45. Parnot C., Bardin S., Miserey-Lenkei S., Guedin D., Corvol P., and Clauser E. Systematic identification of mutations that constitutively activate the angiotensin II type 1A receptor by screening a randomly mutated cDNA library with an original pharmacological bioassay. Proc. Natl. Acad. Sci. U.S.A. 97 (2000) 7615-7620
46. Sadoshima J., Xu Y., Slayter H.S., and Izumo S. Autocrine release of angiotensin II mediates stretch-induced hypertrophy of cardiac myocytes in vitro. Cell 75 (1993) 977-984
47. Saygili E., Rana O.R., Saygili E., Reuter H., Frank K., Schwinger R.H., Müller-Ehmsen J., and Zobel C. Losartan prevents stretch-induced electrical remodeling in cultured atrial neonatal myocytes. Am. J. Physiol. Heart Circ. Physiol. 292 (2007) H2898-H2905
48. 1 receptor differentiate between closely related insurmountable and competitive angiotensin antagonists. Br. J. Pharmacol. 113 (1994) 331-333
49. 1 receptor antagonists. Clinical implications of active metabolites. J. Med. Chem. 46 (2003) 2261-2270
50. Timmermans P.B. Angiotensin II receptor antagonists: an emerging new class of cardiovascular therapeutics. Hypertens. Res. 22 (1999) 147-153
51. van Kesteren C.A., Saris J.J., Dekkers D.H., Lamers J.M., Saxena P.R., Schalekamp M.A., and Danser A.H. Cultured neonatal rat cardiac myocytes and fibroblasts do not synthesize renin or angiotensinogen: evidence for stretch-induced cardiomyocyte hypertrophy independent of angiotensin II. Cardiovasc. Res. 43 (1999) 148-156
52. 1 receptors expressed in CHO-K1 cells. Biochem. Pharmacol. 59 (2000) 927-935
53. 3H]irbesartan to human recombinant angiotensin II type 1 receptors. J. Renin-Angiotensin-Aldosterone Syst. 1 (2000) 159-165
54. 1 receptors. Brit. J. Pharmacol. 126 (1999) 1057-1065
55. Vauquelin G., and Szczuka A. Kinetic versus allosteric mechanisms to explain insurmountable antagonism and delayed ligand dissociation. Neurochem. Int. 51 (2007) 254-260
56. Vauquelin G., and Van Liefde I. G protein-coupled receptors: a count of 1001 conformations. Fundam. Clin. Pharmacol. 19 (2005) 45-56
57. Vauquelin G., and Van Liefde I. From slow antagonist dissociation to long- lasting receptor protection. Trends Pharmacol. Sci. 27 (2006) 355-359
58. 1 receptor antagonists. J. Renin-Angiotensin-Aldosterone Syst. 2 (2001) S24-S31
59. Vauquelin G., Morsing P., Fierens F.L., De Backer J.P., and Vanderheyden P.M. A two-state receptor model for the interaction between angiotensin II type 1 receptors and non-peptide antagonists. Biochem. Pharmacol. 61 (2001) 277-284
60. Vauquelin G., Fierens F., Verheijen I., and Vanderheyden P. Insurmountable AT(1) receptor antagonism: the need for different antagonist binding states of the receptor. Trends Pharmacol. Sci. 22 (2001) 343-344
61. Vauquelin G., Fierens F.L.P., Gáborik Z., Le Minh T., De Backer J.-P., Hunyady L., and Vanderheyden P.M.L. Role of basic amino acids of the human angiotensin type1 receptor in the binding of the non-peptide antagonist candesartan. J. Renin-Angiotensin-Aldosterone Syst. 2 (2001) S32-S36
62. Vauquelin G., Van Liefde I., and Vanderheyden P.M.L. Models and methods for studying insurmountable antagonism. Trends Pharmacol. Sci. 23 (2002) 514-518
63. 1 receptor binding and protection by candesartan: comparison to other biphenyl-tetrazole sartans. J. Hypertens. 24 (2006) S23-S30
64. Verheijen I., Fierens F.L.P., De Backer J.-P., Vauquelin G., and Vanderheyden P.M.L. Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors. Fundam. Clin. Pharmacol. 14 (2000) 577-585
65. 1 receptors in intact cells. Biochem. Pharmacol. 67 (2004) 601-606
66. Wienen W., Maunz A.B., Van Meel J.C., and Entzeroth M. Different types of receptor interaction of peptide and nonpeptide angiotensin II antagonists revealed by receptor binding and functional studies. Mol. Pharmacol. 41 (1992) 1081-1088
67. Wienen W., Hauel N., Van Meel J.C., Narr B., Ries U., and Entzeroth M. Pharmacological characterization of the novel nonpeptide angiotensin II receptor antagonist, BIBR 277. Br. J. Pharmacol. 110 (1993) 245-252
68. Yamazaki T., Komuro I., Kudoh S., Zou Y., Shiojima I., Mizuno T., Takano H., Hiroi Y., Ueki K., Tobe K., Kadowaki T., Nagai R., and Yazaki Y. Angiotensin II partly mediates mechanical stress-induced cardiac hypertrophy. Circ. Res. 77 (1995) 258-265
69. Yamazaki T., Komuro I., Shiojima I., Mizuno T., Kudoh S., Zou Y., Takano H., Hiroi Y., Ueki K., Tobe K., Kadowaki T., Nagai R., and Yazaki Y. Mechanical stress activates protein kinase cascade of phosphorylation in neonatal rat cardiac myocytes. J. Clin. Invest. 96 (1995) 438-446
70. Zou Y., Akazawa H., Qin Y., Sano M., Takano H., Minamino T., Makita N., Iwanaga K., Zhu W., Kudoh S., Toko H., Tamura K., Kihara M., Nagai T., Fukamizu A., Umemura S., Iiri T., Fujita T., and Komuro I. Mechanical stress activates angiotensin II type 1 receptor without the involvement of angiotensin II. Nat. Cell Biol. 6 (2004) 499-506