The angiotensin II AT1 receptor structure-activity correlations in the light of rhodopsin structure

Physiological Reviews

Volumn 87, Issue 2, 2007, Pages 565-592

  Oliveira, Laerte ^a   Costa Neto, Claudio M ^b   Nakaie, Clovis R ^b   Schreier, Shirley ^b   Shimuta, Suma I ^b   Paiva, Antonio C M ^b  

^a FEDERAL UNIVERSITY OF SÃO PAULO   (Brazil)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

ANGIOTENSIN 1 RECEPTOR; ANGIOTENSIN 2 RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; RETINA S ANTIGEN; RHODOPSIN;

CARDIOVASCULAR EFFECT; CLUSTER ANALYSIS; DESENSITIZATION; DRUG EFFECT; ENZYME ACTIVATION; HUMAN; INTERNALIZATION; LIGAND BINDING; MUTAGENESIS; PHOSPHORYLATION; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN FUNCTION; RECEPTOR BINDING; RENIN ANGIOTENSIN ALDOSTERONE SYSTEM; RESIDUE ANALYSIS; REVIEW; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; TACHYPHYLAXIS; ANIMAL; CHEMISTRY; METABOLISM; PHYSIOLOGY;

ANIMALS; HUMANS; RECEPTOR, ANGIOTENSIN, TYPE 1; RENIN-ANGIOTENSIN SYSTEM; RHODOPSIN; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 34248591811     PISSN: 00319333     EISSN: 15221210     Source Type: Journal    
DOI: 10.1152/physrev.00040.2005     Document Type: Review

References (306)

1. 1-receptor heterodimers show enhanced G-protein activation and altered receptor sequestration. Nature 407: 94-98, 2000.
2. 1 receptor antagonist. J Biol Chem 276: 39721-39726, 2001.
3. AbdAlla S, Lother H, Langer A, el Faramawy Y, Quitterer U. Factor XIIIA transglutaminase crosslinks AT1 receptor dimers of monocytes at the onset of atherosclerosis. Cell 119: 343-354, 2004.
4. + fluxes in vascular smooth muscle cells. Pflügers Arch 415: 230-234, 1989.
5. Albiston AL, McDowall SG, Matsacos D, Sim P, Clune E, Mustafa T, Lee J, Mendelsohn FA, Simpson RJ, Connolly LM, Chai SY. Evidence that the angiotensin IV [AT(4)] receptor is the enzyme insulin-regulated aminopeptidase. J Biol Chem 276: 48623-48626, 2001.
6. Anderson KM, Murahashi T, Dostal DE, Peach MJ. Morphological and biochemical analysis of angiotensin II internalization in cultured rat aortic smooth muscle cells. Am J Physiol Cell Physiol 264: C179-C188, 1993.
7. Angelova K, Fanelli F, Puett D. A model for constitutive lutropin receptor activation based on molecular simulation and engineered mutations in transmembrane helices 6 and 7. J Biol Chem 277: 32202-32213, 2002.
8. Angelova K, Narayan P, Simon JP, Puett D. Functional role of transmembrane helix 7 in the activation of the heptahelical lutropin receptor. Mol Endocrinol 14: 459-471, 2000.
9. Antunes-Rodrigues J, de Castro M, Elias LL, Valenca MM, McCann SM. Neuroendocrine control of body fluid metabolism. Physiol Rev 84: 169-208, 2004.
10. Ardaillou R. Angiotensin II receptors. J Am Soc Nephrol 11: S30-S39, 1999.
11. Arimoto R, Kisselev OG, Makara GM, Marshall GR. Rhodopsin-transducin interface: studies with conformationally constrained peptides. Biophys J 81: 3285-3293, 2001.
12. Auger-Messier M, Clement M, Lanctot PM, Leclerc PC, Leduc R, Escher E, Guillemette G. The constitutively active N111G-AT1 receptor for angiotensin II maintains a high affinity conformation despite being uncoupled from its cognate G protein Gq/11alpha. Endocrinology 144: 5277-5284, 2003.
13. Baldwin JM, Schertler GF, Unger VM. An alpha-carbon template for the transmembrane helices in the rhodopsin family of G-protein-coupled receptors. J Mol Biol 272: 144-164, 1997.
14. Baleanu-Gogonea C, Karnik S. Model of the whole rat AT(1) receptor and the ligand-binding site. J Mol Mod 1-13, 2006.
15. Ballesteros JA, Jensen AD, Liapakis G, Rasmussen SG, Shi L, Gether U, Javitch JA. Activation of the beta 2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6. J Biol Chem 276: 29171-29177, 2001.
16. Ballesteros JA, Shi L, Javitch JA. Structural mimicry in G protein-coupled receptors: implications of the high-resolution structure of rhodopsin for structure-function analysis of rhodopsin-like receptors. Mol Pharmacol 60: 1-19, 2001.
17. Balmforth AJ, Lee AJ, Warburton P, Donnelly D, Ball SG. The conformational change responsible for AT1 receptor activation is dependent upon two juxtaposed asparagine residues on transmembrane helices III and VII. J Biol Chem 272: 4245-4251, 1997.
18. Barbhaiya H, McClain R, Ijzerman A, Rivkees SA. Site-directed mutagenesis of the human A1 adenosine receptor: influences of acidic and hydroxy residues in the first four transmembrane domains on ligand binding. Mol Pharmacol 50: 1635-1642, 1996.
19. Barki-Harrington L, Luttrell LM, Rockman HA. Dual inhibition of beta-adrenergic and angiotensin II receptors by a single antagonist: a functional role for receptor-receptor interaction in vivo. Circulation 108: 1611-1618, 2003.
20. Bartl FJ, Fritze O, Ritter E, Herrmann R, Kuksa V, Palczewski K, Hofmann KP, Ernst OP. Partial agonism in a G protein-coupled receptor: role of the retinal ring structure in rhodopsin activation. J Biol Chem 280: 34259-34267, 2005.
21. Beck M, Sakmar TP, Siebert F. Spectroscopic evidence for interaction between transmembrane helices 3 and 5 in rhodopsin. Biochemistry 37: 7630-7639, 1998.
22. Beukers MW, Kristiansen K, Ijzerman AP, Edvardsen O. TinyGRAP database: a bioinformatics tool to mine G protein-coupled receptor mutant data. Trends Pharmacol Sci 20: 475-477, 1999.
23. Bihoreau C, Monnot C, Davies E, Teutsch B, Bernstein KE, Corvol P, Clauser E. Mutation of Asp74 of the rat angiotensin II receptor confers changes in antagonist affinities and abolishes G-protein coupling. Proc Natl Acad Sci USA 90: 5133-5137, 1993.
24. Bockaert J, Roussignol G, Becamel C, Gavarini S, Joubert L, Dumuis A, Fagni L, Marin P. GPCR-interacting proteins (GIPs): nature and functions. Biochem Soc Trans 32: 851-855, 2004.
25. Boucard AA, Roy M, Beaulieu ME, Lavigne P, Escher E, Guillemette G, Leduc R. Constitutive activation of the angiotensin II type 1 receptor alters the spatial proximity of transmembrane 7 to the ligand-binding pocket. J Biol Chem 278: 36628-36636, 2003.
26. Bovy PR, O'Neal JM, Olins GM, Patton DR, McMahon EG, Palomo M, Koepke JP, Salles KS, Trapani AJ, Smits GJ. Structure-activity relationships for the carboxy-terminus truncated analogues of angiotension II, a new class of angiotensin II antagonists. J Med Chem 33: 1477-1482, 1990.
27. Brock TA, Rittenhouse SE, Powers CW, Ekstein LS, Gimbrone MA Jr, Alexander RW. Phorbol ester and 1-oleoyl-2-acetylglycerol inhibit angiotensin activation of phospholipase C in cultured vascular smooth muscle cells. J Biol Chem 260: 14158-14162, 1985.
28. Bulenger S, Marullo S, Bouvier M. Emerging role of homo- and heterodimerization in G-protein coupled receptor biosynthesis and maturation. Trends Pharmacol Sci 26: 131-137, 2005.
29. Bywater RP. Location and nature of the residues important for ligand recognition in G-protein coupled receptors. J Mol Recognit 18: 60-72, 2005.
30. Cai H, Griendling KK, Harrison DG. The vascular NAD(P)H oxidases as therapeutic targets in cardiovascular diseases. Trends Pharmacol Sci 24: 471-478, 2003.
31. Capponi AM, Catt KJ. Angiotensin II receptors in adrenal cortex and uterus. Binding and activation properties of angiotensin analogues. J Biol Chem 254: 5120-5127, 1979.
32. Carey RM. Cardiovascular and renal regulation by the angiotensin type 2 receptor. The AT2 receptor comes of age. Hypertension 45: 840-844, 2005.
33. Cavalli A, Fanelli F, Taddei C, De Benedetti PG, Cotecchia S. Amino acids of the alpha1B-adrenergic receptor involved in agonist binding: differences in docking catecholamines to receptor subtypes. FEBS Lett 399: 9-13, 1996.
34. Cazaubon C, Gougat J, Bousquet F, Guiraudou P, Gayraud R, Lacour C, Roccon A, Galindo G, Barthelemy G, Gautret B. Pharmacological characterization of SR 47436, a new nonpeptide AT1 subtype angiotensin II receptor antagonist. J Pharmacol Exp Ther 265: 826-834, 1993.
35. Ciarkowski J, Witt M, Slusarz R. A hypothesis for GPCR activation. J Mol Mod 11: 407-415, 2005.
36. Clement M, Martin SS, Beaulieu ME, Chamberland C, Lavigne P, Leduc R, Guillemette G, Escher E. Determining the environment of the ligand binding pocket of the human angiotensin II type I (hAT1) receptor using the methionine proximity assay. J Biol Chem 280: 27121-27129, 2005.
37. Coleman DE, Lee E, Mixon MB, Linder ME, Berghuis AM, Gilman AG, Sprang SR. Crystallization and preliminary crystallographic studies of Gi alpha 1 and mutants of Gi alpha 1 in the GTP and GDP-bound states. J Mol Biol 238: 630-634, 1994.
38. Conchon S, Monnot C, Teutsch B, Corvol P, Clauser E. Internalization of the rat AT1a and AT1b receptors: pharmacological and functional requirements. FEBS Lett 349: 365-370, 1994.
39. Correa SA, Graciela C, Pignatari GC, Ferro ES, Pacheco NAS, Costa-Netto CM, Pesquero JB, Oliveira L, Paiva ACM, Shimuta SI. Role of the Cys18-Cys274 disulfide bond and of the third extracellular loop in the constitutive activation and internalization of angiotensin II type 1 receptor. Regul Pept 134: 132-140, 2006.
40. Correa SA, Pacheco NA, Costa-Neto CM, Oliveira L, Pesquero JB, Han SW, Paiva AC, Shimuta SI. Angiotensin II AT(1) receptor mutants expressed in CHO cells caused morphological change and inhibition of cell growth. Regul Pept 131:18-22, 2005.
41. Correa SA, Zalcberg H, Han SW, Oliveira L, Costa-Neto CM, Paiva AC, Shimuta SI. Aliphatic amino acids in helix VI of the AT(1) receptor play a relevant role in agonist binding and activity. Regul Pept 106: 33-38, 2002.
42. Costa-Neto CM, Miyakawa AA, Oliveira L, Hjorth SA, Schwartz TW, Paiva ACM. Mutational analysis of the interaction of N- and C-terminal ends of angiotensin II with the AT1 receptor. Br J Pharmacol 130: 1263-1268, 2000.
43. De Gasparo M, Catt KJ, Inagami T, Wright JW, Unger T. International Union of Pharmacology. XXIII. The angiotensin II receptors. Pharmacol Rev 52: 415-472, 2000.
44. DeGraff JL, Gurevich VV, Benovic JL. The third intracellular loop of alpha 2-adrenergic receptors determines subtype specificity of arrestin interaction. J Biol Chem 277: 43247-43252, 2002.
45. Doan TN, Ali MS, Bernstein KE. Tyrosine kinase activation by the angiotensin II receptor in the absence of calcium signaling. J Biol Chem 276: 20954-20958, 2001.
46. Donoghue M, Hsieh F, Baronas E, Godbout K, Gosselin M, Stagliano N, Donovan M, Woolf B, Robinson K, Jeyaseelan R, Breitbart RE, Acton S. A novel angiotensin-converting enzyme-related carboxypeptidase (ACE 2) converts angiotensin I to angiotensin (1-9). Circ Res 87: 1-9, 2000.
47. Dunker AK, Brown CJ, Lawson JD, Iakoucheva LM, Obradovic Z. Intrinsic disorder and protein function. Biochemistry 41: 6573-6582, 2002.
48. Dupre DJ, Le Gouill C, Gingras D, Rola-Pleszczynski M, Stankova J. Inverse agonist activity of selected ligands of the cysteinyl-leukotriene receptor 1. J Pharmacol Exp Ther 309: 102-108, 2004.
49. Eguchi S, Inagami T. Signal transduction of angiotensin II type 1 receptor through receptor tyrosine kinase. Regul Pept 91: 13-20, 2000.
50. Ernst OP, Hofmann KP, Sakmar TP. Characterization of rhodopsin mutants that bind transducin but fail to induce GTP nucleotide uptake. Classification of mutant pigments by fluorescence, nucleotide release, flash-induced light-scattering assays. J Biol Chem 270: 10580-10586, 1995.
51. Ernst OP, Meyer CK, Marin EP, Henklein P, Fu WY, Sakmar TP, Hofmann KP. Mutation of the fourth cytoplasmic loop of rhodopsin affects binding of transducin and peptides derived from the carboxyl-terminal sequences of transducin alpha and gamma subunits. J Biol Chem 275: 1937-1943, 2000.
52. Fan QR, Hendrickson WA. Structure of human follicle-stimulating hormone in complex with its receptor. Nature 433: 269-277, 2005.
53. Feng YH, Noda K, Saad Y, Liu XP, Husain A, Karnik SS. The docking of Arg2 of angiotensin II with Asp281 of AT1 receptor is essential for full agonism. J Biol Chem 270: 12846-12850, 1995.
54. Feng YH, Ding Y, Ren S, Zhou L, Xu C, Karnik SS. Unconventional homologous internalization of the angiotensin II type-1 receptor induced by G-protein-independent signals. Hypertension 46: 419-425, 2005.
55. Feng YH, Miura S, Husain A, Karnik SS. Mechanism of constitutive activation of the AT1 receptor: influence of the size of the agonist switch binding residue Asn(111). Biochemistry 37: 15791-15798, 1998.
56. Feng YH, Zhou L, Qiu R, Zeng R. Single mutations at Asn295 and Leu305 in the cytoplasmic half of transmembrane α-helix domain 7 of the AT1 receptor induce promiscuous agonist specificity for angiotensin II fragments: a pseudo-constitutive activity. Mol Pharmacol 68: 347-355, 2005.
57. Fermandjian S, Fromageot P, Tistchenko AM, Leicknam JP, Lutz M. Angiotensin II conformations. Infrared and raman studies. Eur J Biochem 28: 174-182, 1972.
58. Ferrario CM, Averill DB, Brosnihan KB, Chappell MC, Iskandar SS, Dean RH, Diz DI. Vasopeptidase inhibition and Ang-(1 - 7) in the spontaneously hypertensive rat. Kidney Int 62: 1349-1357, 2002.
59. Ferrario CM, Chappell MC, Tallant EA, Brosnihan KB, Diz DI. Counterregulatory actions of angiotensin-(1 - 7). Hypertension 30: 535-541, 1997.
60. Fessart D, Simaan M, Laporte SA. c-Src regulates clathrin adapter protein 2 interaction with beta-arrestin and the angiotensin II type 1 receptor during clathrin-mediated internalization. Mol Endocrinol 19: 491-503, 2005.
61. Fierens FL, Vanderheyden PM, Gaborik Z, Minh TL, Backer JP, Hunyady L, Ijzerman A, Vauquelin G. Lys(199) mutation of the human angiotensin type 1 receptor differentially affects the binding of surmountable and insurmountable non-peptide antagonists. J Renin Angiotensin Aldosterone Syst 1: 283-288, 2000.
62. Filipek S, Krzysko KA, Fotiadis D, Liang Y, Saperstein DA, Engel A, Palczewski K. A concept for G protein activation by G protein-coupled receptor dimers: the transducin/rhodopsin interface. Photochem Photobiol Sci 3: 628-638, 2004.
63. Fitzsimons JT. Angiotensin, thirst, sodium appetite. Physiol Rev 78: 583-686, 1998.
64. Fritze O, Filipek S, Kuksa V, Palczewski K, Hofmann KP, Ernst OP. Role of the conserved NPxxY(x)5,6F motif in the rhodopsin ground state and during activation. Proc Natl Acad Sci USA 100: 2290-2295, 2003.
65. Fu Y, Zhong H, Nanamori M, Mortensen RM, Huang X, Lan K, Neubig RR. RGS-insensitive G-protein mutations to study the role of endogenous RGS proteins. Methods Enzymol 389: 229-243, 2004.
66. Gaborik Z, Jagadeesh G, Zhang M, Spat A, Catt KJ, Hunyady L. The role of a conserved region of the second intracellular loop in AT1 angiotensin receptor activation and signaling. Endocrinology 144: 2220-2228, 2003.
67. Garcia KC, Ronco PM, Verroust PJ, Brunger AT, Amzel LM. Three-dimensional structure of an angiotensin II-Fab complex at 3 A: hormone recognition by an anti-idiotypic antibody. Science 257: 502-507, 1992.
68. Gendron L, Payet MD, Gallo-Payet N. The angiotensin type 2 receptor of angiotensin II and neuronal differentiation: from observations to mechanisms. J Mol Endocrinol 31: 359-372, 2003.
69. Gether U. Uncovering molecular mechanisms involved in activation of G protein-coupled receptors. Endocr Rev 21: 90-113, 2000.
70. Goghari MH, Franklin KJ, Moore GJ. Structure-activity relationships for the competitive angiotensin antagonist [sarcosine,O- methyltyrosine4]angiotensin II (sarmesin). J Med Chem 29: 1121-1124, 1986.
71. 13 in agonist-induced vascular smooth muscle cell contraction. Circ Res 87: 221-227, 2000.
72. Granzin J, Wilden U, Choe HW, Labahn J, Krafft B, Buldt G. X-ray crystal structure of arrestin from bovine rod outer segments. Nature 391: 918-921, 1998.
73. 2A receptor desensitization. Biochemistry 42: 10853-10862, 2003.
74. Griendling KK, Lassegue B, Murphy TJ, Alexander RW. Angiotensin II receptor pharmacology. Adv Pharmacol 28: 269-306, 1994.
75. Griendling KK, Berk BC, Socorro L, Tsuda T, Delafontaine P, Alexander RW. Secondary signalling mechanisms in angiotensin II-stimulated vascular smooth muscle cells. Clin Exp Pharmacol Physiol 15: 102-112, 1988.
76. Griendling KK, Ushio-Fukai M, Lasseg B, Alexander RW. Angiotensin II signaling vascular smoth muscle. New concepts. Hypertension 29: 366-373, 1997.
77. 1A angiotensin II receptor induces its constitutive activation. J Biol Chem 272: 1822-1826, 1997.
78. Groblewski T, Maigret B, Nouet S, Larguier R, Lombard C, Bonnafous JC, 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: 153-160, 1995.
79. Guo DF, Sun YL, Hamet P, Inagami T. The angiotensin II type 1 receptor and receptor-associated proteins. Cell Res 11: 165-180, 2001.
80. Gurevich VV, Gurevich EV. The molecular acrobatics of arrestin activation. Trends Pharmacol Sci 25: 105-111, 2004.
81. Hall MM, Khosla MC, Khairallah PA, Bumpus FM. Angiotensin analogs: the influence of sarcosine substituted in position 1. J Pharmacol Exp Ther 188: 222-228, 1974.
82. Han HM, Shimuta SI, Kanashiro CA, Oliveira L, Han SW, Paiva AC. Residues Val254, His256, Phe259 of the angiotensin II AT1 receptor are not involved in ligand binding but participate in signal transduction. Mol Endocrinol 12: 810-814, 1998.
83. Han M, Gurevich VV, Vishnivetskiy SA, Sigler PB, Schubert C. Crystal structure of beta-arrestin at 1.9 A: possible mechanism of receptor binding and membrane translocation. Structure 9: 869-880, 2001.
84. Han M, Smith SO, Sakmar TP. Constitutive activation of opsin by mutation of methionine 257 on transmembrane helix 6. Biochemistry 37: 8253-8261, 1998.
85. Hansen JL, Theilade J, Haunso S, Sheikh SP. Oligomerization of wild type and nonfunctional mutant angiotensin II type I receptors inhibits galphaq protein signaling but not ERK activation. J Biol Chem 279: 24108-24115, 2004.
86. Hazari A, Lowes V, Chan JH, Wong CS, Ho MK, Wong YH. Replacement of the alpha5 helix of Galpha16 with Galphas-specific sequences enhances promiscuity of Galpha16 toward Gs-coupled receptors. Cell Signal 16: 51-62, 2004.
87. Hein L, Meinel L, Pratt RE, Dzau VJ, Kobilka BK. Intracellular trafficking of angiotensin II and its AT1 and AT2 receptors: evidence for selective sorting of receptor and ligand. Mol Endocrinol 11: 1266-1277, 1997.
88. Hermans E. Biochemical and pharmacological control of the multiplicity of coupling at G-protein-coupled receptors. Pharmacol Ther 99: 25-44, 2003.
89. Herrmann R, Heck M, Henklein P, Henklein P, Kleuss C, Hofmann KP, Ernst OP. Sequence of interactions in receptor-G protein coupling. J Biol Chem 279: 24283-24290, 2004.
90. Higashi M, Shimokawa H, Hattori T, Hiroki J, Mukai Y, Morikawa K, Ichiki T, Takahashi S, Takeshita A. Long-term inhibition of Rho-kinase suppresses angiotensin II-induced cardiovascular hypertrophy in rats in vivo: effect on endothelial NAD(P)H oxidase system. Circ Res 93: 767-775, 2003.
91. 2 binding activity. Thromb Haemostasis 82: 1528-1531, 1999.
92. Hiroi Y, Hiroi J, Kudoh S, Yazaki Y, Nagai R, Komuro I. Two distinct mechanisms of angiotensin II-induced negative regulation of the mitogen-activated protein kinases in cultured cardiac myocytes. Hypertens Res 24: 385-394, 2001.
93. Hirsch JA, Schubert C, Gurevich VV, Sigler PB. The 2.8 A crystal structure of visual arrestin: a model for arrestin's regulation. Cell 97: 257-269, 1999.
94. Hjorth SA, Schambye HT, Greenlee WJ, Schwartz TW. Identification of peptide binding residues in the extracellular domains of the AT1 receptor. J Biol Chem 269: 30953-30959, 1994.
95. Ho MK, Chan JH, Wong CS, Wong YH. Identification of a stretch of six divergent amino acids on the alpha5 helix of Galpha16 as a major determinant of the promiscuity and efficiency of receptor coupling. Biochem J 380: 361-369, 2004.
96. Hollenberg NK, Barbero LR, Hinrichs KP. Angiotensin tachyphylaxis and vascular angiotensinase activity. Experientia 27: 1032-1034, 1971.
97. Holloway AC, Qian H, Pipolo L, Ziogas J, Miura S, Karnik S, Southwell BR, Lew MJ, Thomas WG. Side-chain substitutions within angiotensin II reveal different requirements for signaling, internalization, phosphorylation of type 1A angiotensin receptors. Mol Pharmacol 61: 768-777, 2002.
98. Horiuchi M. Functional aspects of angiotensin type 2 receptor. Adv Exp Med Biol 396: 217-224, 1996.
99. Horn F, Bettler E, Oliveira L, Campagne F, Cohen FE, Vriend G. GPCRDB information system for G protein-coupled receptors. Nucleic Acids Res 31: 294-297, 2003.
100. Hsieh KH, Marshall GR. Role of the C-terminal carboxylate in angiotensin II activity: alcohol, ketone, ester analogues of angiotensin II. J Med Chem 29: 1968-1971, 1986.
101. Huang P, Visiers I, Weinstein H, Liu-Chen LY. The local environment at the cytoplasmic end of TM6 of the mu opioid receptor differs from those of rhodopsin and monoamine receptors: introduction of an ionic lock between the cytoplasmic ends of helices 3 and 6 by a L6 30(275)E mutation inactivates the mu opioid receptor and reduces the constitutive activity of its T6 34(279)K mutant. Biochemistry 41: 11972-11980, 2002.
102. Hunyady L, Baukal AJ, Balla T, Catt KJ. Independence of type I angiotensin II receptor endocytosis from G protein coupling and signal transduction. J Biol Chem 269: 24798-247804, 1994.
103. Hunyady L, Bor M, Balla T, Catt KJ. Critical role of a conserved intramembrane tyrosine residue in angiotensin II receptor activation. J Biol Chem 270: 9702-9705, 1995.
104. Hunyady L, Bor M, Balla T, Catt KJ. Identification of a cytoplasmic Ser-Thr-Leu motif that determines agonist-induced internalization of the AT1 angiotensin receptor. J Biol Chem 269: 31378-31382, 1994.
105. Hunyady L, Catt KJ, Clark AJ, Gaborik Z. Mechanisms and functions of AT(1) angiotensin receptor internalization. Regul Pept 91: 29-44, 2000.
106. Hunyady L, Vauquelin G, Vanderheyden P. Agonist induction and conformational selection during activation of a G-protein-coupled receptor. Trends Pharmacol Sci 24: 81-86, 2003.
107. Hunyady L, Ji H, Jagadeesh G, Zhang M, Gaborik Z, Mihalik B, Catt KJ. Dependence of AT1 angiotensin receptor function on adjacent asparagine residues in the seventh transmembrane helix. Mol Pharmacol 54: 427-434, 1998.
108. Hunyady L. Molecular mechanism of angiotensin II receptor internalization. J Am Soc Nephrol 11: S47-S56, 1999.
109. Hunyady L, Zhang M, Jagadeesh G, Bor M, Balla T, Catt KJ. Dependence of agonist activation on a conserved apolar residue in the third intracellular loop of the AT1 angiotensin receptor. Proc Natl Acad Sci USA 93: 10040-10045, 1996.
110. Inglese J, Freedman NJ, Koch WJ, Lefkowitz RJ. Structure and mechanism of the G protein-coupled receptor kinases. J Biol Chem 268: 23735-23738, 1993.
111. Inoue Y, Nakamura N, Inagami T. A review of mutagenesis studies of angiotensin II type 1 receptor, the three-dimensional receptor model in search of the agonist and antagonist binding site and the hypothesis of a receptor activation mechanism. J Hypertens 15: 703-714, 1997.
112. Ishiguro M, Oyama Y, Hirano T. Structural models of the photointermediates in the rhodopsin photocascade, lumirhodopsin, metarhodopsin I, metarhodopsin II. Chembiochem 5: 298-310, 2004.
113. Ishii K, Takekoshi K, Shibuya S, Kawakami Y, Isobe K, Nakai T. Angiotensin subtype-2 receptor (AT2) negatively regulates subtype-1 receptor (AT1) in signal transduction pathways in cultured porcine adrenal medullary chromaffin cells. J Hypertens 19: 1991-1999, 2001.
114. Iwai N, Inagami T. Identification of two subtypes in the rat type I angiotensin II receptor. FEBS Lett 298: 257-260, 1992.
115. Iwai N, Yamano Y, Chaki S, Konishi F, Bardhan S, Tibbetts C, Sasaki K, Hasegawa M, Matsuda Y, Inagami T. Rat angiotensin II receptor: cDNA sequence and regulation of the gene expression. Biochem Biophys Res Commun 177: 299-304, 1991.
116. Jagadeesh G. Angiotensin II receptors - antagonists, molecular biology, signal transduction. Indian J Exp Biol 36: 1171-1194, 1998.
117. Jastrzebska B, Maeda T, Zhu L, Fotiadis D, Filipek S, Engel A, Stenkamp RE, Palczewski K. Functional characterization of rhodopsin monomers and dimers in detergents. J Biol Chem 279: 54663-54675, 2004.
118. Javitch JA, Ballesteros JA, Weinstein H, Chen J. A cluster of aromatic residues in the sixth membrane-spanning segment of the dopamine D2 receptor is accessible in the binding-site crevice. Biochemistry 37: 998-1006, 1998.
119. Javitch JA, Fu D, Liapakis G, Chen J. Constitutive activation of the beta2 adrenergic receptor alters the orientation of its sixth membrane-spanning segment. J Biol Chem 272: 18546-18549, 1997.
120. Javitch JA, Li X, Kaback J, Karlin A. A cysteine residue in the third membrane-spanning segment of the human D2 dopamine receptor is exposed in the binding-site crevice. Proc Natl Acad Sci USA 91: 10355-10359, 1994.
121. Ji H, Leung M, Zhang Y, Catt KJ, Sandberg K. Differential structural requirements for specific binding of nonpeptide and peptide antagonists to the AT1 angiotensin receptor. Identification of amino acid residues that determine binding of the antihypertensive drug losartan. J Biol Chem 269: 16533-16536, 1994.
122. Johannesson P, Lindeberg G, Johansson A, Nikiforovich GV, Gogoll A, Synnergren B, Le Greves M, Nyberg F, Karlen A, Hallberg A. Vinyl sulfide cyclized analogues of angiotensin II with high affinity and full agonist activity at the AT(1) receptor. J Med Chem 45: 1767-1777, 2002.
123. Jonker HR, Wechselberger RW, Boelens R, Folkers GE, Kaptein R. Structural properties of the promiscuous VP16 activation domain. Biochemistry 44: 827-839, 2005.
124. Kalatskaya I, Schussler S, Blaukat A, Muller-Esterl W, Jochum M, Proud D, Faussner A. Mutation of tyrosine in the conserved NPXXY sequence leads to constitutive phosphorylation and internalization, but not signaling, of the human B2 bradykinin receptor. J Biol Chem 279: 31268-31276, 2004.
125. Kambayashi Y, Bardhan S, Takahashi K, Tsuzuki S, Inui H, Hamakubo T, Inagami T. Molecular cloning of a novel angiotensin II receptor isoform involved in phosphotyrosine phosphatase inhibition. J Biol Chem 268: 24543-24546, 1993.
126. Kanashiro CA, Paiva TB, Paiva ACM, Prioste RN, Aboulafia J, Shimuta SI. Angiotensin II tachyphylaxis in the guinea-pig ileum and its prevention: a pharmacological and biochemical study. J Pharmacol Exp Ther 275: 1543-1550, 1995.
127. Kariya K, Takai Y. Distinct functions of down-regulation-sensitive and -resistant types of protein kinase C in rabbit aortic smooth muscle cells. FEBS Lett 219: 119-124, 1987.
128. Karnik SS, Gogonea C, Patil S, Saad Y, Takezako T. Activation of G-protein-coupled receptors: a common molecular mechanism. Trends Endocrinol Metab 14: 431-437, 2003.
129. Karnik SS, Husain A, Graham RM. Molecular determinants of peptide and non-peptide binding to the AT1 receptor. Clin Exp Pharmacol Physiol Suppl 3: S58-S56, 1996.
130. Khairallah PA, Page IH, Bumpus FM, Turker RK. Angiotensin tachyphylaxis and its reversal. Circ Res 19: 247-254, 1966.
131. Khosla MC, Smeby RR, Bumpus FM. Structure activity relationship in angiotensin II analogs. In: Handbook of Experimental Pharmacology, edited by IH Page and RM. Bumpus. New York: Springer-Verlag, 1974, p. 126-156.
132. Kisselev OG, Downs MA, McDowell JH, Hargrave PA. Conformational changes in the phosphorylated C-terminal domain of rhodopsin during rhodopsin arrestin interactions. J Biol Chem 279:5 1203-5 1207, 2004.
133. Kisselev OG, Kao J, Ponder JW, Fann YC, Gautam N, Marshall GR. Light-activated rhodopsin induces structural binding motif in G protein alpha subunit. Proc Natl Acad Sci USA 95: 4270-4275, 1998.
134. Kisselev OG, Meyer CK, Heck M, Ernst OP, Hofmann KP. Signal transfer from rhodopsin to the G-protein: evidence for a two-site sequential fit mechanism. Proc Natl Acad Sci USA 96: 4898-4903, 1999.
135. Kisselev OG, Downs MA. Rhodopsin controls a conformational switch on the transducin gamma subunit. Structure 11: 367-373, 2003.
136. Klco JM, Wiegand CB, Narzinski K, Baranski TJ. Essential role for the second extracellular loop in C5a receptor activation. Nat Struct Mol Biol 12: 320-326, 2005.
137. Kochendoerfer GG, Kaminaka S, Mathies RA. Ultraviolet resonance Raman examination of the light-induced protein structural changes in rhodopsin activation. Biochemistry 36: 13153-13159, 1997.
138. Kohen R, Fashingbauer LA, Heidmann DE, Guthrie CR, Hamblin MW. Cloning of the mouse 5-HT6 serotonin receptor and mutagenesis studies of the third cytoplasmic loop. Brain Res 90: 110-117, 2001.
139. Kostenis E, Zeng FY, Wess J. Functional characterization of a series of mutant G protein alphaq subunits displaying promiscuous receptor coupling properties. J Biol Chem 273: 17886-17892, 1998.
140. Lagane B, Ballet S, Planchenault T, Balabanian K, Le Poul E, Blanpain C, Percherancier Y, Staropoli I, Vassart G, Oppermann M, Parmentier M, Bachelerie F. Mutation of the DRY motif reveals different structural requirements for CCR5-mediated signaling and receptor endocytosis. Mol Pharmacol 67: 1966-1976, 2005.
141. Lagerholm BC, Weinreb GE, Jacobson K, Thompson NL. Detecting microdomains in intact cell membranes. Annu Rev Phys Chem 56: 309-336, 2005.
142. Lambright DG, Sondek J, Bohm A, Skiba NP, Hamm HE, Sigler PB. The 2.0 A crystal structure of a heterotrimeric G protein. Nature 379: 311-319, 1996.
143. Langford K, Frenzel K, Martin BM, Bernstein KE. The genomic organization of the rat AT1 angiotensin receptor. Biochem Biophys Res Commun 183: 1025-1032, 1992.
144. Laporte SA, Roy SF, Escher E, Guillemette G, Leduc R. Essential role of leucine222 in mediating signal transduction of the human angiotensin II type 1 receptor. Receptors Channels 5: 103-112, 1998.
145. Le MT, Vanderheyden PM, Szaszak M, Hunyady L, Vauquelin G. Angiotensin IV is a potent agonist for constitutive active human AT1 receptors. Distinct roles of the N- and C-terminal residues of angiotensin II during AT1 receptor activation. J Biol Chem 277: 23107-23110, 2002.
146. Leff P. The two-state model of receptor activation. Trends Pharmacol Sci 16: 89-97, 1995.
147. Lefkowitz RJ, Shenoy SK. Transduction of receptor signals by beta-arrestins. Science 308: 512-517, 2005.
148. Lefkowitz RJ, Whalen EJ. Beta-arrestins: traffic cops of cell signaling. Curr Opin Cell Biol 16: 162-168, 2004.
149. Lew MJ, Ziogas J. The two-state model of antagonist-AT1 receptor interaction: an hypothesis defended but not tested. Biochem Pharmacol 67: 397-399, 2004.
150. Lewis JW, Kliger DS. Photointermediates of visual pigments. J Bioenerg Biomembr 4: 201-210, 1992.
151. Li J, Edwards PC, Burghammer M, Villa C, Schertler GF. Structure of bovine rhodopsin in a trigonal crystal form. J Mol Biol 343: 1409-1438, 2004.
152. Li JM, Iwai M, Cui TX, Min LJ, Tsuda M, Iwanami J, Suzuki J, Mogi M, Horiuchi M. Effect of azelnidipine on angiotensin II-mediated growth-promoting signaling in vascular smooth muscle cells. Mol Pharmacol 67: 1666-1673, 2005.
153. Li S, Liu X, Min L, Ascoli M. Mutations of the second extracellular loop of the human lutropin receptor emphasize the importance of receptor activation and de-emphasize the importance of receptor phosphorylation in agonist-induced internalization. J Biol Chem 276: 7968-7973, 2001.
154. Li YM, Marnerakis M, Stimson ER, Maggio JE. Mapping peptide-binding domains of the substance P (NK-1) receptor from P388D cells with photolabile agonists. J Biol Chem 270: 1213-1220, 1995.
155. Liang M, Eason MG, Theiss CT, Liggett SB. Phosphorylation of Ser360 in the third intracellular loop of the alpha2A-adrenoceptor during protein kinase C-mediated desensitization. Eur J Pharmacol 437: 41-46, 2002.
156. Limbird LE, Speck JL, Smith SK. Sodium ion modulates agonist and antagonist interactions with the human platelet 2-adrenergic receptor in membrane and solubilized preparations. Mol Pharmacol 21: 609-617, 1982.
157. Lin SW, Sakmar TP. Specific tryptophan UV-absorbance changes are probes of the transition of rhodopsin to its active state. Biochemistry 35: 11149-11159, 1996.
158. 1 receptors in rabbit aorta. Eur J Pharmacol 235: 9-15, 1993.
159. Lu D, Vage DI, Cone RD. A ligand-mimetic model for constitutive activation of the melanocortin-1 receptor. Mol Endocrinol 12: 592-604, 1998.
160. Marie J, Koch C, Pruneau D, Paquet JL, Groblewski T, Larguier R, Lombard C, Deslauriers B, Maigret B, Bonnafous JC. Constitutive activation
161. Marie J, Maigret B, Joseph MP, Larguier R, Nouet S, Lombard C, Bonnafous JC. Tyr292 in the seventh transmembrane domain of the AT1A angiotensin II receptor is essential for its coupling to phospholipase C. J Biol Chem 269: 20815-20818, 1994.
162. Marin EP, Krishna AG, Zvyaga TA, Isele J, Siebert F, Sakmar TP. The amino terminus of the fourth cytoplasmic loop of rhodopsin modulates rhodopsin-transducin interaction. J Biol Chem 275: 1930-1936, 2000.
163. Marshall GR, Bosshard HE. Angiotensin II. Studies on the biologically active conformation. Circ Res 31: 143-150, 1972.
164. Marshall GR, Vine W, Needlemann P. A specific competitive inhibitor of angiotensin II. Proc Natl Acad Sci USA 67: 1624-1630, 1970.
165. Martin S, Boucard AA, Clement M, Escher E, Leduc R, Guillemette G. Analysis of the third transmembrane domain of the human type 1 angiotensin II receptor by cysteine scanning mutagenesis. J Biol Chem 279: 51415-51423, 2004.
166. Martin S, Botto JM, Vincent JP, Mazella J. Pivotal role of an aspartate residue in sodium sensitivity and coupling to G proteins of neurotensin receptors. Mol Pharmacol 55: 210-215, 1999.
167. Maudsley S, Martin B, Luttrell LM. The origins of diversity and specificity in G protein-coupled receptor signaling. J Pharmacol Exp Ther 314: 485-494, 2005.
168. Menon ST, Han M, Sakmar TP. Rhodopsin: structural basis of molecular physiology. Physiol Rev 81: 1659-1688, 2001.
169. Miasiro N, Oshiro MEM, Paiva TB, Paiva ACM. Role of the two N-terminal residues of angiotensin II in the production of tachyphylaxis. Eur J Pharmacol 87: 397-406, 1983.
170. Mielke T, Alexiev U, Glasel M, Otto H, Heyn MP. Light-induced changes in the structure and accessibility of the cytoplasmic loops of rhodopsin in the activated MII state. Biochemistry 41: 7875-7884, 2002.
171. Min L, Ascoli M. Effect of activating and inactivating mutations on the phosphorylation and trafficking of the human lutropin/choriogonadotropin receptor. Mol Endocrinol 14: 1797-1810, 2000.
172. Min L, Galet C, Ascoli M. The association of arrestin-3 with the human lutropin/choriogonadotropin receptor depends mostly on receptor activation rather than on receptor phosphorylation. J Biol Chem 277: 702-710, 2002.
173. Miserey-Lenkei S, Lenkei Z, Parnot C, Corvol P, Clauser E. A functional enhanced green fluorescent protein (EGFP)-tagged angiotensin II at(1a) receptor recruits the endogenous Galphaq/11 protein to the membrane and induces its specific internalization independently of receptor-G protein coupling in HEK-293 cells. Mol Endocrinol 15: 294-307, 2001.
174. Miserey-Lenkei S, Parnot C, Bardin S, Corvol P, Clauser E. Constitutive internalization of constitutively active agiotensin II AT(1A) receptor mutants is blocked by inverse agonists. J Biol Chem 277: 5891-5901, 2002.
175. Miura S, Karnik SS. Angiotensin II type 1 and type 2 receptors bind angiotensin II through different types of epitope recognition. J Hypertens 17: 397-404, 1999.
176. Miura S, Karnik SS. Constitutive activation of angiotensin II type 1 receptor alters the orientation of transmembrane Helix-2. J Biol Chem 277: 24299-24305, 2002.
177. Miura S, Karnik SS. Ligand-independent signals from angiotensin II type 2 receptor induce apoptosis. EMBO J 19: 4026-4035, 2000.
178. Miura S, Feng YH, Husain A, Karnik SS. Role of aromaticity of agonist switches of angiotensin II in the activation of the AT1 receptor. J Biol Chem 274: 7103-7110, 1999.
179. Miura S, Karnik SS, Saku K. Constitutively active homo-oligomeric angiotensin II type 2 receptor induces cell signaling independent of receptor conformation and ligand stimulation. J Biol Chem 280: 18237-18244, 2005.
180. Miura S, Saku K, Karnik SS. Molecular analysis of the structure and function of the angiotensin II type 1 receptor. Hypertens Res 26: 937-943, 2003.
181. Miura S, Zhang J, Boros J, Karnik SS. TM2-TM7 interaction in coupling movement of transmembrane helices to activation of the angiotensin II type-1 receptor. J Biol Chem 278: 3720-3725, 2003.
182. Mizuno K, Niimura S, Tani M, Saito I, Sanada H, Takahashi M, Okazaki K, Yamaguchi M, Fukuchi S. Hypotensive activity of TCV-116, a newly developed angiotensin II receptor antagonist, in spontaneously hypertensive rats. Life Sci 51: PL183-PL187, 1992.
183. Monnot C, Bihoreau C, Conchon S, Curnow KM, 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: 1507-1513, 1996.
184. Moore A, Khairallah PA. Further studies on angiotensin tachyphylaxis. J Pharmacol Exp Ther 197: 575-581, 1976.
185. Moore GJ, Franklin KJ, Nystrom DM, Goghari MH. Structure-desensitization relationships of angiotensin analogues in the rat isolated uterus. Can J Physiol Pharmacol 63: 966-971, 1985.
186. Mukoyama M, Nakajima M, Horiuchi M, Sasamura H, Pratt RE, Dzau VJ. Expression cloning of type 2 angiotensin II receptor reveals a unique class of seven-transmembrane receptors. J Biol Chem 268: 24539-24542, 1993.
187. Murphy TJ, Alexander RW, Griendling KK, Runge MS, Bernstein KE. Isolation of a cDNA encoding the vascular type-1 angiotensin II receptor. Nature 351: 233-236, 1991.
188. Naka T, Kubo K. A new class of diacidic nonpeptide angiotensin II receptor antagonists: candesartan cilexetil. Curr Pharm Des 5: 453-472, 1999.
189. Natochin M, Gasimov KG, Moussaif M, Artemyev NO. Rhodopsin determinants for transducin activation: a gain-of-function approach. J Biol Chem 278: 37574-37581, 2003.
190. Neubig RR, Siderovski DP. Regulators of G-protein signalling as new central nervous system drug targets. Nat Rev Drug Discov 1: 187-197, 2002.
191. Neve KA, Cumbay MG, Thompson KR, Yang R, Buck DC, Watts VJ, DuRand CJ, Teeter MM. Modeling and mutational analysis of a putative sodium-binding pocket on the dopamine D2 receptor. Mol Pharmacol 60: 373-381, 2001.
192. Nikiforovich GV, Kao JL, Plucinska K, Zhang WJ, Marshall GR. Conformational analysis of two cyclic analogs of angiotensin: implications for the biologically active conformation. Biochemistry 33: 3591-3598, 1994.
193. Nikiforovich GV, Mihali B, Catt KJ, Marshall GR. Molecular mechanisms of constitutive activity: mutations at position 111 of the angiotensin AT1 receptor. J Pept Res 66: 236-248, 2005.
194. Nikiforovich GV, Vesterman BG, Betins J. Combined use of spectroscopic and energy calculation methods for the determination of peptide conformation in solution. Biophys Chem 31: 101-106, 1988.
195. Noda K, Feng YH, Liu XP, Saad Y, Husain A, Karnik SS. The active state of the AT1 angiotensin receptor is generated by angiotensin II induction. Biochemistry 35: 16435-16442, 1996.
196. 1 receptor in agonist activation. J Biol Chem 270: 28511-28514, 1995.
197. Noda K, Saad Y, Kinoshita A, Boyle TP, Graham RM, Husain A, Karnik SS. Tetrazole and carboxylate groups of angiotensin receptor antagonists bind to the same subsite by different mechanisms. J Biol Chem 270: 2284-2289, 1995.
198. Oakley RH, Laporte SA, Holt JA, Barak LS, Caron MG. Molecular determinants underlying the formation of stable intracellular G protein-coupled receptor-beta-arrestin complexes after receptor endocytosis. J Biol Chem 276: 19452-19460, 2001.
199. 2-terminal kinase mediates migration of vascular smooth muscle cells stimulated by angiotensin II. Arterioscler Thromb Vasc Biol 25: 1831-1836, 2005.
200. Ohyama K, Yamano Y, Sano T, Nakagomi Y, Hamakubo T, Morishima I, Inagami T. Disulfide bridges in extracellular domains of angiotensin II receptor type IA. Regul Pept 57: 141-147, 1995.
201. Ohyama K, Yamano Y, Sano T, Nakagomi Y, Wada M, Inagami T. Role of the conserved DRY motif on G protein activation of rat angiotensin II receptor type 1A. Biochem Biophys Res Commun 292: 362-367, 2002.
202. 1A angiotensin receptor. J Biol Chem 276: 37761-37768, 2001.
203. Oliveira L, Hulsen T, Lutje Hulsik D, Paiva AC, Vriend G. Heavier-than-air flying machines are impossible. FEBS Lett 564: 269-273, 2004.
204. Oliveira L, Paiva AC, Vriend G. A low resolution model for the interaction of G proteins with G protein-coupled receptors. Protein Eng 12: 1087-1095, 1999.
205. Oliveira L, Paiva AC, Vriend G. Correlated mutation analyses on very large sequence families. Chembiochemistry 3: 1010-1017, 2002.
206. Oliveira L, Paiva AC, Sander C, Vriend G. A common step for signal transduction in G protein-coupled receptors. Trends Pharmacol Sci 15: 170-172, 1994.
207. Oliveira L, Paiva ACM, Vriend G. A common motif in G-protein-coupled seven transmembrane helix receptors. J Comp-Aid Mol Des 7: 649-658, 1993.
208. Oliveira L, Paiva PB, Paiva AC, Vriend G. Identification of functionally conserved residues with the use of entropy-variability plots. Proteins 52: 544-552, 2003.
209. Oliveira L, Paiva PB, Paiva AC, Vriend G. Sequence analysis reveals how G protein-coupled receptors transduce the signal to the G protein. Proteins 52: 553-560, 2003.
210. Oosterom J, Garner KM, den Dekker WK, Nijenhuis WA, Gispen WH, Burbach JP, Barsh GS, Adan RA. Common requirements for melanocortin-4 receptor selectivity of structurally unrelated melanocortin agonist and endogenous antagonist, Agouti protein. J Biol Chem 276: 931-936, 2001.
211. Oshiro MEM, Miasiro N, Paiva TB, Paiva ACM. Angiotensin tachyphylaxis in the isolated rabbit aorta. Blood Vessels 21: 72-79, 1984.
212. Paiva ACM, Paiva TB. The importance of the N-terminal end of angiotensin II for its pressor and oxytocic activities. Biochem Pharmacol 5: 187-191, 1960.
213. Paiva ACM, Paiva TB. The photo-oxidative inactivation of angiotensinamide. Biochim Biophys Acta 48: 412-414, 1961.
214. Paiva TB, Juliano L, Nouailhetas VLA, Paiva ACM. The effect of pH on tachyphylaxis to angiotensin peptides in the isolated guinea pig ileum and rat uterus. Eur J Pharmacol 25: 191-196, 1974.
215. Paiva TB, Paiva ACM. Some pharmacological actions of synthetic analogues of angiotensinamide. Br J Pharmacol Chemother 15: 557-560, 1960.
216. Paiva TB, Miyamoto ME, Juliano L, Paiva ACM. Requirements for angiotensin tachyphylaxis in smooth muscle. J Pharmacol Exp Ther 202: 294-300, 1977.
217. Paiva TB, Paiva AC, Scheraga HA. The conformation of angiotensin II in aqueous solution. Biochemistry 12:1327-1334, 1963.
218. Palaic D, Lemorvan P. Angiotensin tachyphylaxis in guinea-pig aortic strips. J Pharmacol Exp Ther 179: 522-531, 1971.
219. Palczewski K. Structure and functions of arrestins. Protein Sci 3: 1355-1361, 1994.
220. Palczewski K, Buczylko J, Ohguro H, Annan RS, Carr SA, Crabb JW, Kaplan MW, Johnson RS, Walsh KA. Characterization of a truncated form of arrestin isolated from bovine rod outer segments. Protein Sci 3: 314-324, 1994.
221. Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, Yamamoto M, Miyano M. Crystal structure of rhodopsin: a G protein-coupled receptor. Science 289: 739-745, 2000.
222. Pals DT, Denning GS Jr, Keenan RE. Historical development of saralasin. Kidney Int Suppl 9: S7-S10, 1979.
223. Parnot C, Bardin S, Miserey-Lenkei S, Guedin D, Corvol P, 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 USA 97: 7615-7620, 2000.
224. Patel AB, Crocker E, Reeves PJ, Getmanova EV, Eilers M, Khorana HG, Smith SO. Changes in interhelical hydrogen bonding upon rhodopsin activation. J Mol Biol 347: 803-812, 2005.
225. Pauwels PJ, Wurch T. Review: amino acid domains involved in constitutive activation of G-protein-coupled receptors. Mol Neurobiol 17: 109-135, 1998.
226. Peach MJ, Bumpus FM, Khairallah PA. Release of adrenal catecholamines by angiotensin I. J Pharmacol Exp Ther 176: 366-376, 1971.
227. Peach MJ. Renin-angiotensin system: biochemistry and mechanisms of action. Physiol Rev 57: 313-370, 1977.
228. Pederson SE, Ross EM. Functional activation of beta-adrenergic receptors by thiols in the presence or absence of agonists. J Biol Chem 260: 14150-14157, 1985.
229. Perez DM, Karnik SS. Multiple signaling states of G-protein-coupled receptors. Pharmacol Rev 57: 147-161, 2005.
230. 1 ligands: susceptibility to receptor mutations. Mol Pharmacol 51: 301-311, 1990.
231. Perlman S, Schambye HT, Rivero RA, Greenlee WJ, Hjorth SA, Schwartz TW. Non-peptide angiotensin agonist. Functional and molecular interaction with the AT1 receptor. J Biol Chem 270: 1493-1496, 1995.
232. Pert CB, Snyder SH. Opiate receptor binding of agonists and antagonists affected differentially by sodium. Mol Pharmacol 10: 868-879, 1974.
233. 1 receptor. Biol Chem 387: 269-276, 2006.
234. 2+! The physiology and pathology of Ca(2+)-binding proteins in the retina. Trends Neurosci 19: 547-554, 1996.
235. Presland J. G-protein-coupled receptor accessory proteins: their potential role in future drug discovery. Biochem Soc Trans 32: 888-891, 2004.
236. Printz MP, Nemethy G, Bleich H. Proposed models for angiotensin II in aqueous solution and conclusions about receptor topography. Nat New Biol 237: 135-140, 1972.
237. Pulvermuller A, Maretzki D, Rudnicka-Nawrot M, Smith WC, Palczewski K, Hofmann KP. Functional differences in the interaction of arrestin and its splice variant, p44, with rhodopsin. Biochemistry 36: 9253-9260, 1997.
238. Regoli D, Park WK. The pressor and myotropic effects and the antagonistic properties of several analogues of angiotensin II. Can J Physiol Pharmacol 50: 99-112, 1972.
239. Regoli D, Rioux F, Park WK, Choi C. Role of the N-terminal amino acid for the biological activities of angiotensin and inhibitory analogues. Can J Physiol Pharmacol 52: 39-49, 1974.
240. Regoli D, Park WK, Rioux F. Pharmacology of angiotensin. Pharmacol Rev 26: 69-123, 1974.
241. Robertson MJ, Wragg A, Clark KL. Modulation of tachyphylaxis to angiotensin II in rabbit isolated aorta by the angiotensin AT1 receptor antagonist, losartan. Regul Pept 50: 137-145, 1994.
242. Rosendorff A, Ebersole BJ, Sealfon SC. Conserved helix 7 tyrosine functions as an activation relay in the serotonin 5HT(2C) receptor. Brain Res Mol Brain Res 84: 90-96, 2000.
243. Ruprecht JJ, Mielke T, Vogel R, Villa C, Schertler GF. Electron crystallography reveals the structure of metarhodopsin I. EMBO J 23: 3609-3620, 2004.
244. Sakmar TP, Menon ST, Marin EP, Awad ES. Rhodopsin: insights from recent structural studies. Annu Rev Biophys Biomol Struct 31: 443-484, 2002.
245. Sakuta H, Sekiguchi M, Okamoto K, Sakai Y. Oscillatory muscarinic acetylcholine responses of Xenopus oocytes are desensitized by protein kinase C and sensitized by protein phosphatase 2B. Eur J Pharmacol 208: 297-305, 1991.
246. Samanen J, Regoli D. Angiotensin Receptors, edited by R. R. Ruffolo. Boca Raton, FL: CRC, 1994, p. 11-97.
247. Samanen J, Cash T, Narindray D, Brandeis E, Yellin E, Addams W Jr, Yellin T, Eggleston D, DeBrosse C, Regoli D. The role of position 4 in angiotensin II antagonism: a structure-activity study. J Med Chem 32: 1366-1370, 1989.
248. Sano T, Ohyama K, Yamano Y, Nakagomi Y, Nakazawa S, Kikyo M, Shirai H, Blank JS, Exton JH, Inagami T. A domain for G protein coupling in carboxyl-terminal tail of rat angiotensin II receptor type 1A. J Biol Chem 272: 23631-23636, 1997.
249. Santos EL, Pesquero JB, Oliveira L, Paiva AC, Costa-Neto CM. Mutagenesis of the AT1 receptor reveals different binding modes of angiotensin II and [Sar1]-angiotensin II. Regul Pept 119: 183-188, 2004.
250. Santos RAS, Simoes e Silva AC, Maric C, Silva DMR, Machado RP, de Buhr I, Heringer-Walther S, Pinheiro SVB, Lopes MT, Bader M, Mendes EP, Lemos VS, Campagnole-Santos MJ, Schultheiss H-P, Speth R, Walther T. Angiotensin-(1 - 7) is an endogenous ligand for the G protein-coupled receptor Mas. Proc Natl Acad Sci USA 100: 8258-8263, 2003.
251. Sasaki K, Yamano Y, Bardhan S, Iwai N, Murray JJ, Hasegawa M, Matsuda Y, Inagami T. Cloning and expression of a complementary DNA encoding a bovine adrenal angiotensin II type-1 receptor. Nature 351: 230-233, 1991.
252. Scanlon MN, Matsoukas JM, Franklin KJ, Moore GJ. A new approach to angiotensin antagonists: methylation of the tyrosine hydroxyl in angiotensin II. Life Sci 34: 317-321, 1984.
253. Schambye HT, Hjorth SA, Weinstock J, Schwartz TW. Interaction between the nonpeptide angiotensin antagonist SKF-108,566 and histidine 256 (HisVI:16) of the angiotensin type 1 receptor. Mol Pharmacol 47: 425-431, 1995.
254. Schertler GF. Structure of rhodopsin and the metarhodopsin I photointermediate. Curr Opin Struct Biol 15: 408-415, 2005.
255. Sealfon SC, Chi L, Ebersole BJ, Rodic V, Zhang D, Ballesteros JA, Weinstein H. Related contribution of specific helix 2 and 7 residues to conformational activation of the serotonin 5-HT2A receptor. J Biol Chem 270: 16683-16688, 1995.
256. Senbonmatsu T, Saito T, Landon EJ, Watanabe O, Price E Jr, Roberts RL, Imboden H, Fitzgerald TG, Gaffney FA, Inagami T. A novel angiotensin II type 2 receptor signaling pathway: possible role in cardiac hypertrophy. EMBO J 22: 6471-6482, 2003.
257. Shenoy SK, Lefkowitz RJ.Angiotensin II-stimulated signaling through G proteins and β-arrestin. Sci STKE 311: Cm14, 2005.
258. Shenoy SK, Lefkowitz RJ. Receptor regulation: beta-arrestin moves up a notch. Nat Cell Biol 7: 1059-1061, 2005.
259. Shi W, Sports CD, Raman D, Shirakawa S, Osawa S, Weiss ER. Rhodopsin arginine-135 mutants are phosphorylated by rhodopsin kinase and bind arrestin in the absence of 11-cis-retinal. Biochemistry 37: 4869-4874, 1998.
260. q coupling by mutagenesis study. Biochem Biophys Res Commun 218: 383-389, 1996.
261. Shieh T, Han M, Sakmar TP, Smith SO. The steric trigger in rhodopsin activation. J Mol Biol 269: 373-384, 1997.
262. Shimuta SI, Nakaie CR, Paiva AC, Cordopatis P, Theodoropoulos D. Changes in residues 1 and 4 of angiotensin II affect differently its agonist and tachyphylactic properties. Naunyn-Schmiedebergs Arch Pharmacol 340: 309-313, 1989.
263. + and protein kinase C in angiotensin desensibilization and tachyphylaxis in the guinea-pig ileum. Naunyn-Schmiedebergs Arch Pharmacol 347: 425-431, 1993.
264. + fluxes in cultured intestinal smooth muscle cells. J Pharmacol Exp Ther 253: 1215-1221, 1990.
265. Simons K, Vaz WL. Model systems, lipid rafts, cell membranes. Annu Rev Biophys Biomol Struct 33: 269-295, 2004.
266. Smith RD, Hunyady L, Olivares-Reyes JA, Mihalik B, Jayadev S, Catt KJ. Agonist-induced phosphorylation of the angiotensin AT1a receptor is localized to a serine/threonine-rich region of its cytoplasmic tail. Mol Pharmacol 54: 935-941, 1998.
267. Spat A, Hunyady L. Control of aldosterone secretion: a model for convergence in cellular signaling pathways. Physiol Rev 84: 489-539, 2004.
268. Spooner PJ, Sharples JM, Goodall SC, Bovee-Geurts PH, Verhoeven MA, Lugtenburg J, Pistorius AM, Degrip WJ, Watts A. The ring of the rhodopsin chromophore in a hydrophobic activation switch within the binding pocket. J Mol Biol 343: 719-730, 2004.
269. Stefanini E, Marchisio AM, Devoto P, Vernaleone F, Collu R, Spano PF. Sodium-dependent interaction of benzamides with dopamine receptors. Brain Res 198: 229-233, 1980.
270. Stewart JM. Tachyphylaxis to angiotensin. In: Angiotensin, edited by I. H. Page and F. M. Bumpus. Berlin: Springer, 1974, p. 170-184.
271. 2 receptor: new insights into an old system. Regul Pept 99: 175-182, 2001.
272. salpha. Science 278: 1943-1947, 1997.
273. Takeda K, Ichiki T, Tokunou T, Iino N, Fujii S, Kitabatake A, Shimokawa H, Takeshita A. Critical role of Rho-kinase and MEK/ERK pathways for angiotensin II-induced plasminogen activator inhibitor type-1 gene expression. Arterioscler Thromb Vasc Biol 21: 868-873, 2001.
274. Takezako T, Gogonea C, Saad Y, Noda K, Karnik SS. "Network leaning" as a mechanism of insurmountable antagonism of the angiotensin II type 1 receptor by non-peptide antagonists. J Biol Chem 279: 15248-15257, 2004.
275. Tang H, Shirai H, Inagami T. Inhibition of protein kinase C prevents rapid desensitization of type 1B angiotensin II receptor. Circ Res 77: 239-248, 1995.
276. Tao YX, Mizrachi D, Segaloff DL. Chimeras of the rat and human FSH receptors (FSHRs) identify residues that permit or suppress transmembrane 6 mutation-induced constitutive activation of the FSHR via rearrangements of hydrophobic interactions between helices 6 and 7. Mol Endocrinol 2002: 600-608, 2002.
277. Terrillon S, Bouvier M. Roles of G-protein-coupled receptor dimerization. EMBO Rep 5: 30-34, 2004.
278. Thomas WG, Baker KM, Motel TJ, Thekkumkara TJ. Angiotensin II receptor endocytosis involves two distinct regions of the cytoplasmic tail. A role for residues on the hydrophobic face of a putative amphipathic helix. J Biol Chem 270: 22153-22159, 1995.
279. Thomas WG, Motel TJ, Kule CE, Karoor V, Baker KM. Phosphorylation of the angiotensin II (AT1A) receptor carboxyl terminus: a role in receptor endocytosis. Mol Endocrinol 12: 1513-1524, 1998.
280. Thomas WG, Qian H, Chang CS, Karnik S. Agonist-induced phosphorylation of the angiotensin II (AT(1A)) receptor requires generation of a conformation that is distinct from the inositol phosphate-signaling state. J Biol Chem 275: 2893-2900, 2000.
281. 1) receptor function. Regul Pept 79: 9-23, 1999.
282. Timmermans PB, Smith RD. Angiotensin II receptor subtypes: selective antagonists and functional correlates. Eur Heart J 15: 79-87, 1994.
283. Timmermans PB, Chiu AT, Herblin WF, Wong PC, Smith RD. Angiotensin II receptor subtypes. Am J Hypertens 5: 406-410, 1992.
284. Timmermans PB, Wong PC, Chiu AT, Herblin WF. Nonpeptide angiotensin II receptor antagonists. Trends Pharmacol Sci 12: 55-62, 1991.
285. Tipnis SR, Hooper NM, Hyde R, Karran E, Christie G, Turner AJ. A human homolog of angiotensin-converting enzyme. Cloning and functional expression as a captopril-insensitive carboxypeptidase. J Biol Chem 275: 33238-33243, 2000.
286. 4]-angiotensin II in the rat mesentery in vivo. J Pharmacol Exp Ther 276: 13-20, 1996.
287. Tucek S, Michal P, Vlachova V. Modelling the consequences of receptor-G-protein promiscuity. Trends Pharmacol Sci 23: 171-176, 2002.
288. 2 angiotensin receptors. FEBS Lett 580: 41-45, 2006.
289. Ullian ME, Linas SL. Role of receptor cycling in the regulation of angiotensin II surface receptor number and angiotensin II uptake in rat vascular smooth muscle cells. J Clin Invest 84: 840-846, 1989.
290. Urizar E, Claeysen S, Deupi X, Govaerts C, Costagliola S, Vassart G, Pardo L. An activation switch in the rhodopsin family of G protein coupled receptors: the thyrotropin receptor. J Biol Chem 280: 17135-17141, 2005.
291. Vanderheyden PM, Fierens FL, Vauquelin G. Angiotensin II type 1 receptor antagonists. Why do some of them produce insurmountable inhibition? Biochem Pharmacol 60: 1557-1563, 2000.
292. 1 receptors. Br J Pharmacol 126: 1057-1065, 1999.
293. Vassart G, Pardo L, Costagliola S. A molecular dissection of the glycoprotein hormone receptors. Trends Biochem Sci 29: 119-126, 2004.
294. Vauquelin G, Fierens F, Verheijen I, Vanderheyden P. Insurmountable AT1 receptor antagonism: the need for different antagonist binding states of the receptor. Trends Pharmacol Sci 22: 333-334, 2001.
295. 1 receptor antagonists. Curr Med Chem Cardiovasc Hematol Agents 2: 69-77, 2004.
296. Wald G. Molecular basis of visual excitation. Science 162: 230-239, 1968.
297. Watson S, Arkinstall S. The G-Protein Linked Receptor Fact Book, edited by S. Watson and S. Arkinstall. London: Academic, 1994.
298. Wei H, Ahn S, Shenoy SK, Karnik SS, Hunyady L, Luttrell LM, Lefkowitz RJ. Independent beta-arrestin 2 and G protein-mediated pathways for angiotensin II activation of extracellular signal-regulated kinases 1 and 2. Proc Natl Acad Sci USA 100: 10782-10787, 2003.
299. Wilbanks AM, Laporte SA, Bohn LM, Barak LS, Caron MG. Apparent loss-of-function mutant GPCRs revealed as constitutively desensitized receptors. Biochemistry 41: 11981-11989, 2002.
300. Wright JW, Harding JW. Important roles for angiotensin III and IV in the brain renin-angiotensin system. Brain Res Rev 25: 96-124, 1997.
301. Yamakawa T, Tanaka S, Numaguchi K, Yamakawa Y, Motley ED, Ichihara S, Inagami T. Involvement of Rho-kinase in angiotensin II-induced hypertrophy of rat vascular smooth muscle cells. Hypertension 35: 313-318, 2000.
302. Yamano Y, Ohyama K, Chaki S, Guo DF, Inagami T. Identification of amino acid residues of rat angiotensin II receptor for ligand binding by site directed mutagenesis. Biochem Biophys Res Commun 187: 1426-1431, 1992.
303. Yamano Y, Ohyama K, Kikyo M, Sano T, Nakagomi Y, Inoue Y, Nakamura N, Morishima I, Guo DF, Hamakubo T, Inagami T. Mutagenesis and the molecular modeling of the rat angiotensin II receptor (AT1). J Biol Chem 270: 14024-14030, 1995.
304. Yu J, Prado GN, Taylor L, Piserchio A, Gupta A, Mierke DF, Polgar P. Global chimeric exchanges within the intracellular face of the bradykinin B2 receptor with corresponding angiotensin II type Ia receptor regions: generation of fully functional hybrids showing characteristic signaling of the AT1a receptor. J Cell Biochem 85: 809-819, 2002.
305. Zhang M, Zhao X, Chen HC, Catt KJ, Hunyady L. Activation of the AT1 angiotensin receptor is dependent on adjacent apolar residues in the carboxyl terminus of the third cytoplasmic loop. J Biol Chem 275: 15782-15788, 2000.
306. Zhang WJ, Nikiforovich GV, Perodin J, Richard DE, Escher E, Marshall GR. Novel cyclic analogs of angiotensin II with cyclization between positions 5 and 7: conformational and biological implications. J Med Chem 39: 2738-2744, 1996.