Targeting the mineralocorticoid receptor in cardiovascular disease

Expert Opinion on Therapeutic Targets

Volumn 17, Issue 3, 2013, Pages 321-331

  Young, Morag J ^a  

^a MONASH UNIVERSITY   (Australia)

Author keywords

Aldosterone; Cardiac fibrosis; Glucocorticoid; Hypertension; Mineralocorticoid receptor

Indexed keywords

ALDOSTERONE; ALDOSTERONE RECEPTOR; BAY 948862; CALCIUM CHANNEL BLOCKING AGENT; DROSPIRENONE; EPLERENONE; MINERALOCORTICOID ANTAGONIST; MINERALOCORTICOID RECEPTOR; SPIRONOLACTONE; TAMOXIFEN; UNCLASSIFIED DRUG;

CARDIOVASCULAR DISEASE; CONGESTIVE HEART FAILURE; DRUG MECHANISM; DRUG TARGETING; ENANTIOSELECTIVITY; HEART DISEASE; HEART FAILURE; HORMONE ACTION; HUMAN; HYPERTENSION; METABOLIC DISORDER; MOLECULAR RECOGNITION; NONHUMAN; REVIEW; TRANSCRIPTION REGULATION;

ANIMALS; CARDIOVASCULAR DISEASES; HUMANS; MINERALOCORTICOID RECEPTOR ANTAGONISTS; RECEPTORS, MINERALOCORTICOID; SIGNAL TRANSDUCTION;

EID: 84873929042     PISSN: 14728222     EISSN: 17447631     Source Type: Journal    
DOI: 10.1517/14728222.2013.748750     Document Type: Review

References (97)

1. King M, Kingery J, Casey B. Diagnosis and evaluation of heart failure. Am Fam Physician 2012;85(12):1161-8
2. Albaghdadi M, Gheorghiade M, Pitt B. Mineralocorticoid receptor antagonism: therapeutic potential in acute heart failure syndromes. Eur Heart J 2011;32(21):2626-33
3. Funder J. Mineralocorticoid receptor antagonists for heart failure. Expert Opin Pharmacother 2011;12(18):2767-9
4. Young MJ, Rickard AJ. Mechanisms of mineralocorticoid salt-induced hypertension and cardiac fibrosis. Mol Cell Endocrinol 2012;350(2):248-55
5. Pitt B, Zannad F, Remme WJ, et al. The effect of spironolactone on morbidity and mortality in patients with severe heart failure. Randomized aldactone evaluation study investigators. N Engl J Med 1999;341(10):709-17
6. Pitt B, Remme W, Zannad F, et al. Eplerenone, a selective aldosterone blocker, in patients with left ventricular dysfunction after myocardial infarction. N Engl J Med 2003;348(14):1309-21
7. Zannad F, McMurray JJ, Krum H, et al. Eplerenone in patients with systolic heart failure and mild symptoms. N Engl J Med 2011;364(1):11-21
8. Zannad F, Alla F, Dousset B, et al. Limitation of excessive extracellular matrix turnover may contribute to survival benefit of spironolactone therapy in patients with congestive heart failure: insights from the randomized aldactone evaluation study (rales). Rales investigators. Circulation 2000;102(22):2700-6
9. Juurlink DN, Mamdani MM, Lee DS, et al. Rates of hyperkalemia after publication of the randomized aldactone evaluation study. N Engl J Med 2004;351(6):543-51
10. Funder JW. Mineralocorticoid-receptor blockade, hypertension and heart failure. Nat Clin Pract Endocrinol Metab 2005;1(1):4-5
11. Kolkhof P, Borden SA. Molecular pharmacology of the mineralocorticoid receptor: prospects for novel therapeutics. Mol Cell Endocrinol 2012;350(2):310-17
12. Simpson SA, Tait JF, Wettstein A, et al. Isolation from the adrenals of a new crystalline hormone with especially high effectiveness on mineral metabolism. Experientia 1953;9(9):333-5
13. Albeaux-Fernet M, Bellot L, Chabot J, et al. The clinical importance of spironolactones, peripheral antagonists of aldosterone. Annee Endocrinol 1961;13:37-71
14. Myles K, Funder JW. Progesterone binding to mineralocorticoid receptors: in vitro and in vivo studies. Am J Physiol 1996;270(4 Pt 1):E601-7
15. Bellati G, Ideo G. Gynaecomastia after spironolactone and potassium canrenoate. Lancet 1986;1(8481):626
16. Brilla CG, Weber KT. Mineralocorticoid excess, dietary sodium, and myocardial fibrosis. J Lab Clin Med 1992;120(6):893-901
17. Meyers MJ, Arhancet GB, Hockerman SL, et al. Discovery of (3s, 3ar)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3, 3a, 4, 5-tetrahydro-2h-benzo [g] indazole-7-carboxylic acid (pf-3882845), an orally efficacious mineralocorticoid receptor (mr) antagonist for hypertension and nephropathy. J Med Chem 2010;53(16):5979-6002
18. Krattenmacher R. Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception 2000;62(1):29-38
19. Oelkers W. Drospirenone-a new progestogen with antimineralocorticoid activity, resembling natural progesterone. Eur J Contracept Reprod Health Care 2000;5(Suppl 3):17-24
20. Caprio M, Antelmi A, Chetrite G, et al. Antiadipogenic effects of the mineralocorticoid receptor antagonist drospirenone: potential implications for the treatment of metabolic syndrome. Endocrinology 2011;152(1):113-25
21. Simoncini T, Fu XD, Caruso A, et al. Drospirenone increases endothelial nitric oxide synthesis via a combined action on progesterone and mineralocorticoid receptors. Hum Reprod 2007;22(8):2325-34
22. Caprio M, Zennaro MC, Feve B, et al. Potential role of progestogens in the control of adipose tissue and salt sensitivity via interaction with the mineralocorticoid receptor. Climacteric 2008;11(3):258-64
23. Fagart J, Hillisch A, Huyet J, et al. A new mode of mineralocorticoid receptor antagonism by a potent and selective nonsteroidal molecule. J Biol Chem 2010;285(39):29932-40
24. Barfacker L, Kuhl A, Hillisch A, et al. Discovery of bay 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases. ChemMedChem 2012;7(8):1385-403
25. Pitt B, Filippatos G, Gheorghiade M, et al. Rationale and design of arts: a randomized, double-blind study of bay 94-8862 in patients with chronic heart failure and mild or moderate chronic kidney disease. Eur J Heart Fail 2012;14(6):668-75
26. Fuller PJ, Yao Y, Yang J, Young MJ. Mechanisms of ligand specificity of the mineralocorticoid receptor. J Endocrinol 2012;213(1):15-24
27. Fuller PJ, Young MJ. Mechanisms of mineralocorticoid action. Hypertension 2005;46(6):1227-35
28. Funder JW, Pearce PT, Smith R, Smith AI. Mineralocorticoid action: target tissue specificity is enzyme, not receptor, mediated. Science 1988;242(4878):583-5
29. Edwards CR, Stewart PM, Burt D, et al. Localisation of 11 beta-hydroxysteroid dehydrogenase-tissue specific protector of the mineralocorticoid receptor. Lancet 1988;2(8618):986-9
30. Funder JW, Pearce PT, Smith R, Campbell J. Vascular type i aldosterone binding sites are physiological mineralocorticoid receptors. Endocrinology 1989;125(4):2224-6
31. Armanini D, Wehling M, Weber PC. Mineralocorticoid effector mechanism in human mononuclear leukocytes. J Steroid Biochem 1987;27(4-6):967-70
32. Van Eekelen JA, Jiang W, De Kloet ER, Bohn MC. Distribution of the mineralocorticoid and the glucocorticoid receptor mrnas in the rat hippocampus. J Neurosci Res 1988;21(1):88-94
33. Pearce P, Funder JW. High affinity aldosterone binding sites (type i receptors) in rat heart. Clin Exp Pharmacol Physiol 1987;14(11-12):859-66
34. Caprio M, Feve B, Claes A, et al. Pivotal role of the mineralocorticoid receptor in corticosteroid-induced adipogenesis. Faseb J 2007;21(9):2185-94
35. Funder JW. Reconsidering the roles of the mineralocorticoid receptor. Hypertension 2009;53(2):286-90
36. Joels M, Karst H, DeRijk R, de Kloet ER. The coming out of the brain mineralocorticoid receptor. Trends Neurosci 2008;31(1):1-7
37. Young MJ, Morgan J, Brolin K, et al. Activation of mineralocorticoid receptors by exogenous glucocorticoids and the development of cardiovascular inflammatory responses in adrenalectomized rats. Endocrinology 2010;151(6):2622-8
38. Christy C, Hadoke PW, Paterson JM, et al. 11beta-hydroxysteroid dehydrogenase type 2 in mouse aorta. Localization and influence on response to glucocorticoids. Hypertension 2003;42(4):580-7
39. Christ M, Wehling M. Rapid actions of aldosterone: lymphocytes, vascular smooth muscle and endothelial cells. Steroids 1999;64(1-2):35-41
40. Mihailidou AS, Funder JW. Nongenomic effects of mineralocorticoid receptor activation in the cardiovascular system. Steroids 2005;70(5-7):347-51
41. Haseroth K, Gerdes D, Berger S, et al. Rapid nongenomic effects of aldosterone in mineralocorticoid-receptor-knockout mice. Biochem Biophys Res Commun 1999;266(1):257-61
42. Grossmann C, Krug AW, Freudinger R, et al. Aldosterone-induced egfr expression: interaction between the human mineralocorticoid receptor and the human egfr promoter. Am J Physiol Endocrinol Metab 2007;292(6):E1790-800
43. Langer G, Bader B, Meoli L, et al. A critical review of fundamental controversies in the field of gpr30 research. Steroids 2010;75(8-9):603-10
44. Gros R, Ding Q, Sklar LA, et al. Gpr30 expression is required for the mineralocorticoid receptor-independent rapid vascular effects of aldosterone. Hypertension 2011;57(3):442-51
45. Barton M. Position paper: the membrane estrogen receptor gper-clues and questions. Steroids 2012;77(10):935-42
46. Batenburg WW, Jansen PM, van den Bogaerdt AJ, J Danser AH. Angiotensin ii-aldosterone interaction in human coronary microarteries involves gpr30, egfr, and endothelial no synthase. Cardiovasc Res 2012;94(1):136-43
47. Montezano AC, Callera GE, Yogi A, et al. Aldosterone and angiotensin ii synergistically stimulate migration in vascular smooth muscle cells through c-src-regulated redox-sensitive rhoa pathways. Arterioscler Thromb Vasc Biol 2008;28(8):1511-18
48. De Giusti VC, Nolly MB, Yeves AM, et al. Aldosterone stimulates the cardiac na(+)/h(+) exchanger via transactivation of the epidermal growth factor receptor. Hypertension 2011;58(5):912-19
49. Messaoudi S, Zhang AD, Griol-Charhbili V, et al. The epidermal growth factor receptor is involved in angiotensin ii but not aldosterone/salt-induced cardiac remodelling. PLoS ONE 2012;7(1):e30156
50. Griol-Charhbili V, Fassot C, Messaoudi S, et al. Epidermal growth factor receptor mediates the vascular dysfunction but not the remodeling induced by aldosterone/salt. Hypertension 2011;57(2):238-44
51. Chai W, Garrelds IM, de Vries R, et al. Nongenomic effects of aldosterone in the human heart: interaction with angiotensin ii. Hypertension 2005;46(4):701-6
52. Young M, Fullerton M, Dilley R, Funder J. Mineralocorticoids, hypertension, and cardiac fibrosis. J Clin Invest 1994;93(6):2578-83
53. Brandish PE, Forest TW, Chen H, et al. Eplerenone decreases inflammatory foci in spontaneously hypertensive rat hearts with minimal effects on blood pressure. J Cardiovasc Pharmacol 2009;53(1):44-51
54. Rocha R, Chander PN, Zuckerman A, Stier CT Jr. Role of aldosterone in renal vascular injury in stroke-prone hypertensive rats. Hypertension 1999;33(1 Pt 2):232-7
55. Rocha R, Martin-Berger CL, Yang P, et al. Selective aldosterone blockade prevents angiotensin ii/salt-induced vascular inflammation in the rat heart. Endocrinology 2002;143(12):4828-36
56. Tsukamoto O, Minamino T, Sanada S, et al. The antagonism of aldosterone receptor prevents the development of hypertensive heart failure induced by chronic inhibition of nitric oxide synthesis in rats. Cardiovasc Drugs Ther 2006;20(2):93-102
57. Berger S, Bleich M, Schmid W, et al. Mineralocorticoid receptor knockout mice: pathophysiology of na+ metabolism. Proc Natl Acad Sci USA 1998;95(16):9424-9
58. Rickard AJ, Morgan J, Tesch G, et al. Deletion of mineralocorticoid receptors from macrophages protects against deoxycorticosterone/salt-induced cardiac fibrosis and increased blood pressure. Hypertension 2009;54(3):537-43
59. Bienvenu LA, Morgan J, Rickard AJ, et al. Macrophage mineralocorticoid receptor signaling plays a key role in aldosterone-independent cardiac fibrosis. Endocrinology 2012;153(7):3416-25
60. Usher MG, Duan SZ, Ivaschenko CY, et al. Myeloid mineralocorticoid receptor controls macrophage polarization and cardiovascular hypertrophy and remodeling in mice. J Clin Invest 2010;120(9):3350-64
61. Frieler RA, Meng H, Duan SZ, et al. Myeloid-specific deletion of the mineralocorticoid receptor reduces infarct volume and alters inflammation during cerebral ischemia. Stroke 2011;42(1):179-85
62. Vinh A, Chen W, Blinder Y, et al. Inhibition and genetic ablation of the b7/cd28 t-cell costimulation axis prevents experimental hypertension. Circulation 2010;122(24):2529-37
63. Harrison DG, Vinh A, Lob H, Madhur MS. Role of the adaptive immune system in hypertension. Curr Opin Pharmacol 2010;10(2):203-7
64. Shen J, young M. Corticosteroids, heart failure and hypertension; a role for immune cells? Endocrinology 2012;In press
65. Lother A, Berger S, Gilsbach R, et al. Ablation of mineralocorticoid receptors in myocytes but not in fibroblasts preserves cardiac function. Hypertension 2011;57(4):746-54
66. Fraccarollo D, Berger S, Galuppo P, et al. Deletion of cardiomyocyte mineralocorticoid receptor ameliorates adverse remodeling after myocardial infarction. Circulation 2011;123(4):400-8
67. Rickard A, Morgan J, Bienvenu L, et al. Cardiomyocyte mineralocorticoid receptors are essential for doc/salt-mediated inflammation and cardiac fibrosis. Hypertension 2012;In press
68. McCurley A, Pires PW, Bender SB, et al. Direct regulation of blood pressure by smooth muscle cell mineralocorticoid receptors. Nat Med 2012;18(9):1429-33
69. Jaffe IZ, Newfell BG, Aronovitz M, et al. Placental growth factor mediates aldosterone-dependent vascular injury in mice. J Clin Invest 2010;120(11):3891-900
70. Ouvrard-Pascaud A, Sainte-Marie Y, Benitah JP, et al. Conditional mineralocorticoid receptor expression in the heart leads to life-threatening arrhythmias. Circulation 2005;111(23):3025-33
71. Favre J, Gao J, Zhang AD, et al. Coronary endothelial dysfunction after cardiomyocyte-specific mineralocorticoid receptor overexpression. Am J Physiol Heart Circ Physiol 2011;300(6):H2035-43
72. Nguyen Dinh Cat A, Griol-Charhbili V, Loufrani L, et al. The endothelial mineralocorticoid receptor regulates vasoconstrictor tone and blood pressure. Faseb J 2010;24(7):2454-63
73. de Resende MM, Kauser K, Mill JG. Regulation of cardiac and renal mineralocorticoid receptor expression by captopril following myocardial infarction in rats. Life Sci 2006;78(26):3066-73
74. Ohtani T, Ohta M, Yamamoto K, et al. Elevated cardiac tissue level of aldosterone and mineralocorticoid receptor in diastolic heart failure: beneficial effects of mineralocorticoid receptor blocker. Am J Physiol Regul Integr Comp Physiol 2007;292(2):R946-54
75. Yoshida M, Ma J, Tomita T, et al. Mineralocorticoid receptor is overexpressed in cardiomyocytes of patients with congestive heart failure. Congest Heart Fail 2005;11(1):12-16
76. Krug AW, Allenhofer L, Monticone R, et al. Elevated mineralocorticoid receptor activity in aged rat vascular smooth muscle cells promotes a proinflammatory phenotype via extracellular signal-regulated kinase 1/2 mitogen-activated protein kinase and epidermal growth factor receptor-dependent pathways. Hypertension 2010;55(6):1476-83
77. Chae CU, Albert CM, Moorthy MV, et al. Vitamin e supplementation and the risk of heart failure in women. Circ Heart Fail 2012;5(2):176-82
78. Dzhanashiya P, Vladytskaya OV, Salibegashvili NV. Efficiency and mechanisms of the antioxidant effect of standard therapy and refracterin in the treatment of chronic heart failure in elderly patients with postinfarction cardiosclerosis. Bull Exp Biol Med 2004;138(4):412-14
79. Mihailidou AS, Loan Le TY, Mardini M, Funder JW. Glucocorticoids activate cardiac mineralocorticoid receptors during experimental myocardial infarction. Hypertension 2009;54(6):1306-12
80. Wilson P, Morgan J, Funder JW, et al. Mediators of mineralocorticoid receptor-induced profibrotic inflammatory responses in the heart. Clin Sci (Lond) 2009;116(9):731-9
81. Rossier MF, Python M, Maturana AD. Contribution of mineralocorticoid and glucocorticoid receptors to the chronotropic and hypertrophic actions of aldosterone in neonatal rat ventricular myocytes. Endocrinology 2010;151(6):2777-87
82. Nagase M, Ayuzawa N, Kawarazaki W, et al. Oxidative stress causes mineralocorticoid receptor activation in rat cardiomyocytes: role of small gtpase rac1. Hypertension 2012;59(2):500-6
83. Huang P, Chandra V, Rastinejad F. Structural overview of the nuclear receptor superfamily: insights into physiology and therapeutics. Annu Rev Physiol 2010;72:247-72
84. McDonnell DP, Dana SL, Hoener PA, et al. Cellular mechanisms which distinguish between hormone-and antihormone-activated estrogen receptor. Ann NY Acad Sci 1995;761:121-37
85. McDonnell DP. Definition of the molecular mechanism of action of tissue-selective oestrogen-receptor modulators. Biochem Soc Trans 1998;26(1):54-60
86. Yang J, Chang CY, Safi R, et al. Identification of ligand-selective peptide antagonists of the mineralocorticoid receptor using phage display. Mol Endocrinol 2011;25(1):32-43
87. Li Y, Suino K, Daugherty J, Xu HE. Structural and biochemical mechanisms for the specificity of hormone binding and coactivator assembly by mineralocorticoid receptor. Mol Cell 2005;19(3):367-80
88. Hultman ML, Krasnoperova NV, Li S, et al. The ligand-dependent interaction of mineralocorticoid receptor with coactivator and corepressor peptides suggests multiple activation mechanisms. Mol Endocrinol 2005;19(6):1460-73
89. Kitagawa H, Yanagisawa J, Fuse H, et al. Ligand-selective potentiation of rat mineralocorticoid receptor activation function 1 by a cbp-containing histone acetyltransferase complex. Mol Cell Biol 2002;22(11):3698-706
90. McKenna NJ, O'Malley BW. Minireview: nuclear receptor coactivators-an update. Endocrinology 2002;143(7):2461-5
91. Shao D, Berrodin TJ, Manas E, et al. Identification of novel estrogen receptor alpha antagonists. J Steroid Biochem Mol Biol 2004;88(4-5):351-60
92. McDonnell DP. The molecular pharmacology of serms. Trends Endocrinol Metab 1999;10(8):301-11
93. McDonnell DP. The molecular determinants of estrogen receptor pharmacology. Maturitas 2004;48(Suppl 1):S7-12
94. Norris JD, Chang C, McDonnell DP. Estrogen receptor-cofactor interactions as targets for novel drug discovery. Ernst Schering Res Found Workshop 2001;34:181-201
95. Norris JD, Paige LA, Christensen DJ, et al. Peptide antagonists of the human estrogen receptor. Science 1999;285(5428):744-6
96. Lazar MA. Nuclear receptor corepressors. Nucl Recept Signal 2003;1:e001
97. Gomez-Sanchez CE, Foecking MF, Ferris MW, et al. The production of monoclonal antibodies against aldosterone. Steroids 1987;49(6):581-7