Agonist-dependent modulation of arterial endothelin A receptor function

British Journal of Pharmacology

Volumn 166, Issue 6, 2012, Pages 1833-1845

  Compeer, M G ^a   Meens, M J P M T ^a   Hackeng, T M ^a   Neugebauer, W A ^b   Holtke C ^c   De Mey, Jo G R ^a  

^a MAASTRICHT UNIVERSITY   (Netherlands)

^b UNIVERSITÉ DE SHERBROOKE   (Canada)

^c UNIVERSITY HOSPITAL MÜNSTER   (Germany)

Author keywords

Agonist dependence; Allosteric modulation; Endothelin 1; ET A receptors

Indexed keywords

4 (4 METHOXYPHENYL) 2 (3,4 METHYLENEDIOXYPHENYL) 4 OXO 3 (3,4,5 TRIMETHOXYBENZYL) 2 BUTENOIC ACID; CYCLO(DEXTRO TRYPTOPHYL DEXTRO ASPARTYLPROLYL DEXTRO VALYLLEUCYL); ENDOTHELIN 1; ENDOTHELIN 2; ENDOTHELIN 3; ENDOTHELIN A RECEPTOR; FELODIPINE; N (2,6 DIMETHYLPIPERIDINOCARBONYL) 4 METHYLLEUCYL DEXTRO (1 METHOXYCARBONYLTRYPTOPHANYL) DEXTRO NORLEUCINE;

ANIMAL TISSUE; ARTERY CONSTRICTION; ARTERY DILATATION; ARTICLE; BINDING COMPETITION; BLOOD VESSEL TONE; CONTROLLED STUDY; LIGAND BINDING; MALE; MESENTERIC ARTERY; NONHUMAN; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN FUNCTION; PROTEIN SYNTHESIS INHIBITION; RAT; RECEPTOR BINDING; VASOMOTOR REFLEX;

ANIMALS; BINDING, COMPETITIVE; CARBOCYANINES; DIOXOLES; ENDOTHELINS; FLUORESCEIN-5-ISOTHIOCYANATE; MESENTERIC ARTERIES; MUSCLE CONTRACTION; MUSCLE, SMOOTH, VASCULAR; PEPTIDES, CYCLIC; RATS; RECEPTOR, ENDOTHELIN A;

EID: 84863214200     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2012.01896.x     Document Type: Article

References (58)

1. Adner M, Shankley N, Edvinsson L (2001). Evidence that ET-1, but not ET-3 and S6b, ET(A)-receptor mediated contractions in isolated rat mesenteric arteries are modulated by co-activation of ET(B) receptors. Br J Pharmacol 133: 927-935. (Pubitemid 32751803)
2. Bagnato A, Rosano L (2008). The endothelin axis in cancer. Int J Biochem Cell Biol 40: 1443-1451.
3. Bax WA, Saxena PR (1994). The current endothelin receptor classification: time for reconsideration? Trends Pharmacol Sci 15: 379-386. (Pubitemid 24325710)
4. Blandin V, Vigne P, Breittmayer JP, Frelin C (2000). Allosteric inhibition of endothelin ETA receptors by 3, 5-dibromosalicylic acid. Mol Pharmacol 58: 1461-1469.
5. Bohm F, Ahlborg G, Johansson BL, Hansson LO, Pernow J (2002). Combined endothelin receptor blockade evokes enhanced vasodilatation in patients with atherosclerosis. Arterioscler Thromb Vasc Biol 22: 674-679. (Pubitemid 34408752)
6. Breu V, Hashido K, Broger C, Miyamoto C, Furuichi Y, Hayes A et al. (1995). Separable binding sites for the natural agonist endothelin-1 and the non-peptide antagonist bosentan on human endothelin-A receptors. Eur J Biochem 231: 266-270.
7. Brosseau JP, Neugebauer WA, Gobeil F, Jr, D'Orleans-Juste P (2009). Design, synthesis and pharmacological characterization of fluorescein-derived endothelin antagonists Bq-123 and Bq-788. Adv Exp Med Biol 611: 443-444.
8. Cardillo C, Campia U, Kilcoyne CM, Bryant MB, Panza JA (2002). Improved endothelium-dependent vasodilation after blockade of endothelin receptors in patients with essential hypertension. Circulation 105: 452-456. (Pubitemid 34141701)
9. Cardillo C, Campia U, Iantorno M, Panza JA (2004). Enhanced vascular activity of endogenous endothelin-1 in obese hypertensive patients. Hypertension 43: 36-40. (Pubitemid 38031908)
10. Christopoulos A, Kenakin T (2002). G protein-coupled receptor allosterism and complexing. Pharmacol Rev 54: 323-374. (Pubitemid 34575719)
11. Conner AC, Simms J, Barwell J, Wheatley M, Poyner DR (2007). Ligand binding and activation of the CGRP receptor. Biochem Soc Trans 35: 729-732. (Pubitemid 47310355)
12. D'Orleans-Juste P, Claing A, Warner TD, Yano M, Telemaque S (1993). Characterization of receptors for endothelins in the perfused arterial and venous mesenteric vasculatures of the rat. Br J Pharmacol 110: 687-692. (Pubitemid 23279279)
13. Davenport AP (2002). International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature. Pharmacol Rev 54: 219-226.
14. De Mey J, Compeer M, Meens M (2009). Endothelin-1, an endogenous irreversible agonist in search of an allosteric inhibitor. Mol Cell Pharmacol 1: 246.
15. De Mey JG, Megens R, Fazzi GE (2008). Functional antagonism between endogenous neuropeptide Y and calcitonin gene-related peptide in mesenteric resistance arteries. J Pharmacol Exp Ther 324: 930-937. (Pubitemid 351397826)
16. De Mey JG, Compeer MG, Lemkens P, Meens MJ (2011). ETA-receptor antagonists or allosteric modulators? Trends Pharmacol Sci 32: 345-351.
17. Doherty AM, Cody WL, DePue PL, He JX, Waite LA, Leonard DM et al. (1993). Structure-activity relationships of C-terminal endothelin hexapeptide antagonists. J Med Chem 36: 2585-2594. (Pubitemid 23294124)
18. Donoso MV, Faundez H, Rosa G, Fournier A, Edvinsson L, Huidobro-Toro JP (1996). Pharmacological characterization of the ETA receptor in the vascular smooth muscle comparing its analogous distribution in the rat mesenteric artery and in the arterial mesenteric bed. Peptides 17: 1145-1153. (Pubitemid 26419740)
19. Ehlert FJ (2005). Analysis of allosterism in functional assays. J Pharmacol Exp Ther 315: 740-754.
20. Hans G, Deseure K, Adriaensen H (2008). Endothelin-1-induced pain and hyperalgesia: a review of pathophysiology, clinical manifestations and future therapeutic options. Neuropeptides 42: 119-132.
21. Hilal-Dandan R, Villegas S, Gonzalez A, Brunton LL (1997). The quasi-irreversible nature of endothelin binding and G protein-linked signaling in cardiac myocytes. J Pharmacol Exp Ther 281: 267-273. (Pubitemid 27203077)
22. Hoare SR (2007). Allosteric modulators of class B G-protein-coupled receptors. Curr Neuropharmacol 5: 168-179.
23. Höltke C, von Wallbrunn A, Kopka K, Schober O, Heindel W, Schäfers M et al. (2007). A fluorescent photoprobe for the imaging of endothelin receptors. Bioconjug Chem 18: 685-694. (Pubitemid 47010787)
24. Hynynen MM, Khalil RA (2006). The vascular endothelin system in hypertension - recent patents and discoveries. Recent Pat Cardiovasc Drug Discov 1: 95-108.
25. Ihara M, Noguchi K, Saeki T, Fukuroda T, Tsuchida S, Kimura S et al. (1992). Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor. Life Sci 50: 247-255.
26. Inoue A, Yanagisawa M, Kimura S, Kasuya Y, Miyauchi T, Goto K et al. (1989). The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc Natl Acad Sci USA 86: 2863-2867. (Pubitemid 19112640)
27. Ishikawa K, Ihara M, Noguchi K, Mase T, Mino N, Saeki T et al. (1994). Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc Natl Acad Sci USA 91: 4892-4896. (Pubitemid 24177756)
28. Kenakin T, Miller LJ (2010). Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev 62: 265-304.
29. Keov P, Sexton PM, Christopoulos A (2011). Allosteric modulation of G protein-coupled receptors: a pharmacological perspective. Neuropharmacology 60: 24-35.
30. Kirkby NS, Hadoke PW, Bagnall AJ, Webb DJ (2008). The endothelin system as a therapeutic target in cardiovascular disease: great expectations or bleak house? Br J Pharmacol 153: 1105-1119. (Pubitemid 351415492)
31. Lattig J, Oksche A, Beyermann M, Rosenthal W, Krause G (2009). Structural determinants for selective recognition of peptide ligands for endothelin receptor subtypes ETA and ETB. J Pept Sci 15: 479-491.
32. Lee JA, Elliott JD, Sutiphong JA, Friesen WJ, Ohlstein EH, Stadel JM et al. (1994). Tyr-129 is important to the peptide ligand affinity and selectivity of human endothelin type A receptor. Proc Natl Acad Sci USA 91: 7164-7168. (Pubitemid 24226823)
33. Maguire JJ, Kuc RE, Davenport AP (1997). Affinity and selectivity of PD156707, a novel nonpeptide endothelin antagonist, for human ET(A) and ET(B) receptors. J Pharmacol Exp Ther 280: 1102-1108. (Pubitemid 27171378)
34. Masaki T (2004). Historical review: endothelin. Trends Pharmacol Sci 25: 219-224.
35. Masaki T, Kimura S, Yanagisawa M, Goto K (1991). Molecular and cellular mechanism of endothelin regulation. Implications for vascular function. Circulation 84: 1457-1468.
36. Meens MJ, Fazzi GE, van Zandvoort MA, De Mey JG (2009). Calcitonin gene-related peptide selectively relaxes contractile responses to endothelin-1 in rat mesenteric resistance arteries. J Pharmacol Exp Ther 331: 87-95.
37. Meens MJ, Compeer MG, Hackeng TM, van Zandvoort MA, Janssen BJ, De Mey JG (2010). Stimuli of sensory-motor nerves terminate arterial contractile effects of endothelin-1 by CGRP and dissociation of ET-1/ET(A)-receptor complexes. PLoS ONE 5: e10917.
38. Meens MJ, Mattheij NJ, Nelissen J, Lemkens P, Compeer MG, Janssen BJ et al. (2011). Calcitonin gene-related peptide terminates long-lasting vasopressor responses to endothelin 1 in vivo. Hypertension 58: 99-106.
39. Millecamps M, Laferriere A, Ragavendran JV, Stone LS, Coderre TJ (2010). Role of peripheral endothelin receptors in an animal model of complex regional pain syndrome type 1 (CRPS-I). Pain 151: 174-183.
40. Mulvany MJ, Aalkjaer C (1990). Structure and function of small arteries. Physiol Rev 70: 921-961. (Pubitemid 20364819)
41. Nohria A, Garrett L, Johnson W, Kinlay S, Ganz P, Creager MA (2003). Endothelin-1 and vascular tone in subjects with atherogenic risk factors. Hypertension 42: 43-48. (Pubitemid 36842235)
42. Palmer MJ (2009). Endothelin receptor antagonists: status and learning 20 years on. Prog Med Chem 47: 203-237.
43. Pierre LN, Davenport AP (1999). Blockade and reversal of endothelin-induced constriction in pial arteries from human brain. Stroke 30: 638-643. (Pubitemid 29115404)
44. Portoghese PS (1989). Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists. Trends Pharmacol Sci 10: 230-235.
45. Randall MD, Douglas SA, Hiley CR (1989). Vascular activities of endothelin-1 and some alanyl substituted analogues in resistance beds of the rat. Br J Pharmacol 98: 685-699. (Pubitemid 19245779)
46. Saeki T, Ihara M, Fukuroda T, Yamagiwa M, Yano M (1991). [Ala1,3,11,15]endothelin-1 analogs with ETB agonistic activity. Biochem Biophys Res Commun 179: 286-292.
47. Sakamoto A, Yanagisawa M, Sawamura T, Enoki T, Ohtani T, Sakurai T et al. (1993). Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J Biol Chem 268: 8547-8553. (Pubitemid 23118635)
48. Sakurai T, Yanagisawa M, Masaki T (1992). Molecular characterization of endothelin receptors. Trends Pharmacol Sci 13: 103-108.
49. Sokolovsky M (1993). BQ-123 identifies heterogeneity and allosteric interactions at the rat heart endothelin receptor. Biochem Biophys Res Commun 196: 32-38.
50. Stauffer BL, Westby CM, Greiner JJ, Van Guilder GP, Desouza CA (2010). Sex differences in endothelin-1-mediated vasoconstrictor tone in middle-aged and older adults. Am J Physiol Regul Integr Comp Physiol 298: R261-R265.
51. Tam JP, Liu W, Zhang JW, Galantino M, Bertolero F, Cristiani C et al. (1994). Alanine scan of endothelin: importance of aromatic residues. Peptides 15: 703-708. (Pubitemid 24221846)
52. Wagner OF, Vierhapper H, Gasic S, Nowotny P, Waldhausl W (1992). Regional effects and clearance of endothelin-1 across pulmonary and splanchnic circulation. Eur J Clin Invest 22: 277-282.
53. Wang Y, Wang DH (2004). Prevention of endothelin-1-induced increases in blood pressure: role of endogenous CGRP. Am J Physiol Heart Circ Physiol 287: H1868-H1874. (Pubitemid 39313297)
54. Warner TD (1990). Simultaneous perfusion of rat isolated superior mesenteric arterial and venous beds: comparison of their vasoconstrictor and vasodilator responses to agonists. Br J Pharmacol 99: 427-433.
55. Warner TD, Mitchell JA, de Nucci G, Vane JR (1989). Endothelin-1 and endothelin-3 release EDRF from isolated perfused arterial vessels of the rat and rabbit. J Cardiovasc Pharmacol 13 (Suppl 5): S85-S88. discussion S102.
56. Webb ML, Patel PS, Rose PM, Liu EC, Stein PD, Barrish J et al. (1996). Mutational analysis of the endothelin type A receptor (ETA): interactions and model of selective ETA antagonist BMS-182874 with putative ETA receptor binding cavity. Biochemistry 35: 2548-2556.
57. Yanagisawa H, Hammer RE, Richardson JA, Williams SC, Clouthier DE, Yanagisawa M (1998). Role of Endothelin-1/Endothelin-A receptor-mediated signaling pathway in the aortic arch patterning in mice. J Clin Invest 102: 22-33. (Pubitemid 28323826)
58. Yanagisawa M, Kurihara H, Kimura S, Tomobe Y, Kobayashi M, Mitsui Y et al. (1988). A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 332: 411-415. (Pubitemid 18090241)