-
1
-
-
84921599010
-
Mineralocorticoid receptor activation and mineralocorticoid receptor antagonist treatment in cardiac and renal diseases
-
This article focuses on the current knowledge and understanding of the direct roles of aldosterone and mineralocorticoid receptor activation in heart and kidneys, including common pathophysiological mechanisms in both organs and implications for the clinical use of MRAs in the trea tment of cardiac and renal diseases
-
Bauersachs J, Jaisser F, Toto R. Mineralocorticoid receptor activation and mineralocorticoid receptor antagonist treatment in cardiac and renal diseases. Hypertension 2015; 65:257-263. This article focuses on the current knowledge and understanding of the direct roles of aldosterone and mineralocorticoid receptor activation in heart and kidneys, including common pathophysiological mechanisms in both organs and implications for the clinical use of MRAs in the trea tment of cardiac and renal diseases.
-
(2015)
Hypertension
, vol.65
, pp. 257-263
-
-
Bauersachs, J.1
Jaisser, F.2
Toto, R.3
-
2
-
-
84920842451
-
Mineralocorticoids in the heart and vasculature: New insights for old hormones
-
Lother A, Moser M, Bode C, et al. Mineralocorticoids in the heart and vasculature: new insights for old hormones. Annu Rev Pharmacol Toxicol 2015; 55:8.1-8.24.
-
(2015)
Annu Rev Pharmacol Toxicol
, vol.55
, pp. 81-824
-
-
Lother, A.1
Moser, M.2
Bode, C.3
-
3
-
-
84897093353
-
Aldosterone and vascular mineralocorticoid receptors: Regulators of ion channels beyond the kidney
-
DuPont JJ, Hill MA, Bender SB, et al. Aldosterone and vascular mineralocorticoid receptors: regulators of ion channels beyond the kidney. Hypertension 2014; 63:632-637.
-
(2014)
Hypertension
, vol.63
, pp. 632-637
-
-
DuPont, J.J.1
Hill, M.A.2
Bender, S.B.3
-
4
-
-
84923849534
-
Aldosterone blockade in ckd: Emphasis on pharmacology
-
These authors have provided a comprehensive overview of mineralocorticoid receptor-blocking therapy in prote inuric CKD. Available MRAs directly target the inflammatory and fibrotic effects of aldosterone in CKD patients, but their use is limited because of unresolved safety issues
-
Schwenk MH, Hirsch JS, Bomback AS. Aldosterone blockade in CKD: emphasis on pharmacology. Adv Chronic Kidney Dis 2015; 22:123-132. These authors have provided a comprehensive overview of mineralocorticoid receptor-blocking therapy in prote inuric CKD. Available MRAs directly target the inflammatory and fibrotic effects of aldosterone in CKD patients, but their use is limited because of unresolved safety issues. 5.
-
(2015)
Adv Chronic Kidney Dis
, vol.22
, pp. 123-132
-
-
Schwenk, M.H.1
Hirsch, J.S.2
Bomback, A.S.3
-
5
-
-
84901689853
-
Therapeutic approaches to diabetic nephropathy: Beyond the ras nat
-
This is an excellent review on current clinical approaches in diabetic nephropathy. The authors emphasize that ins u fficient understanding of drug mechanisms and the pathogenesis of diabetic kidney disease, heterogeneity of trial populations and a paucity of hard outcomes are major causes of recent failures in clinical trials
-
Fernandez-Fernandez B, Ortiz A, Gomez-Guerrero C, Egido J. Therapeutic approaches to diabetic nephropathy: beyond the RAS Nat. Rev Nephrol 2014; 10:325-346. This is an excellent review on current clinical approaches in diabetic nephropathy. The authors emphasize that ins u fficient understanding of drug mechanisms and the pathogenesis of diabetic kidney disease, heterogeneity of trial populations and a paucity of hard outcomes are major causes of recent failures in clinical trials.
-
(2014)
Rev Nephrol
, vol.10
, pp. 325-346
-
-
Fernandez-Fernandez, B.1
Ortiz, A.2
Gomez-Guerrero, C.3
Egido, J.4
-
6
-
-
84869417804
-
Mineralocorticoid receptor antagonists for heart failure with reduced ejection fraction: Integrating evidence into clinical practice
-
Zannad F, Gat tis Stough W, Rossignol P, et al. Mineralocorticoid receptor antagonists for heart failure with reduced ejection fraction: integrating evidence into clinical practice. Eur Heart J 2012; 33:2782-2795.
-
(2012)
Eur Heart J
, vol.33
, pp. 2782-2795
-
-
Zannad, F.1
Gattis Stough, W.2
Rossignol, P.3
-
7
-
-
4143062592
-
How prevalent is hyperkalemia and renal dysfunction during treatment with spironolactone in patients with congestive heart failure
-
Svensson M, Gustafsson F, Galatius S, et al. How prevalent is hyperkalemia and renal dysfunction during treatment with spironolactone in patients with congestive heart failure J Card Fail 2004; 10:297-303.
-
(2004)
J Card Fail
, vol.10
, pp. 297-303
-
-
Svensson, M.1
Gustafsson, F.2
Galatius, S.3
-
8
-
-
26944459667
-
Tolerability of spironolactone as adjunctive treatment for heart failure in patients over 75 years of age
-
Dinsdale C, Wani M, Steward J, O'Mahony MS. Tolerability of spironolactone as adjunctive treatment for heart failure in patients over 75 years of age. Age Ageing 2005; 34:395-398.
-
(2005)
Age Ageing
, vol.34
, pp. 395-398
-
-
Dinsdale, C.1
Wani, M.2
Steward, J.3
O'Mahony, M.S.4
-
9
-
-
84866859500
-
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy
-
Piotrowski DW. Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy. J Med Chem 2012; 55:7957-7966.
-
(2012)
J Med Chem
, vol.55
, pp. 7957-7966
-
-
Piotrowski, D.W.1
-
10
-
-
84856337738
-
Molecular pharmacology of the mineralocorticoid receptor: Prospects for novel therapeutics
-
Kolkhof P, Borden SA. Molecular pharmacology of the mineralocorticoid receptor: prospects for novel therapeutics. Mol Cell Endocrinol 2012; 350:310-317.
-
(2012)
Mol Cell Endocrinol
, vol.350
, pp. 310-317
-
-
Kolkhof, P.1
Borden, S.A.2
-
11
-
-
84903999244
-
Comparison of agents that affect aldosterone action
-
Tamargo J, Solini A, Ruilope LM. Comparison of agents that affect aldosterone action. Semin Nephrol 2014; 34:285-306.
-
(2014)
Semin Nephrol
, vol.34
, pp. 285-306
-
-
Tamargo, J.1
Solini, A.2
Ruilope, L.M.3
-
12
-
-
84906101087
-
Is there a new dawn for selective mineralocorticoid receptor antagonism?
-
Luther JM. Is there a new dawn for selective mineralocorticoid receptor antagonism? Curr Opin Nephrol Hypertens 2014; 23:456-461.
-
(2014)
Curr Opin Nephrol Hypertens
, vol.23
, pp. 456-461
-
-
Luther, J.M.1
-
13
-
-
84892723636
-
Mineralocorticoid receptor modulators: A patent review 2007-2012
-
In this review article, the authors give a comprehensive overview of patents on MRA modulators which were published between the years 2007 and 2012. The authors conclude that novel nonsteroidal MRAs with particular pharmacokinetic profiles may avoid the undesirable renal side-e ffects of steroidal MRAs. These so-called kidney friendly MRAs' are expected to become a clear breakthrough in the field
-
Collin M, Niemann F, Jaisser F. Mineralocorticoid receptor modulators: a patent review (2007-2012). Expert Opin Ther Pat 2014; 24:177-183. In this review article, the authors give a comprehensive overview of patents on MRA modulators which were published between the years 2007 and 2012. The authors conclude that novel nonsteroidal MRAs with particular pharmacokinetic profiles may avoid the undesirable renal side-e ffects of steroidal MRAs. These so-called ' kidney friendly MRAs' are expected to become a clear breakthrough in the field.
-
(2014)
Expert Opin Ther Pat
, vol.24
, pp. 177-183
-
-
Collin, M.1
Niemann, F.2
Jaisser, F.3
-
14
-
-
84861563400
-
Rationale and design of arts: A rand omized, double-blind study of bay 94-8862 in patients with chronic heart failure and mild or moderate chronic kidney disease
-
Pitt B,Filippatos G,Gheorghiade M,et al. Rationale and design of ARTS: a rand omized, 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 14 668-6675.
-
(2012)
Eur J Heart Fail
, vol.14
, pp. 668-6675
-
-
Pitt, B.1
Filippatos, G.2
Gheorghiade, M.3
-
15
-
-
84882415231
-
Safety and tolerability of the novel nonsteroidal mineralocorticoid receptor antagonist bay 94-8862 in patients with chronic heart failure and mild or moderate chronic kidney disease: A randomized, double-blind trial
-
Pitt B, Kober L, Ponikowski P, et al. Safety and tolerability of the novel nonsteroidal mineralocorticoid receptor antagonist BAY 94-8862 in patients with chronic heart failure and mild or moderate chronic kidney disease: a randomized, double-blind trial. Eur Heart J 2013; 34:2453-2463.
-
(2013)
Eur Heart J
, vol.34
, pp. 2453-2463
-
-
Pitt, B.1
Kober, L.2
Ponikowski, P.3
-
16
-
-
84923587123
-
Rationale design, and baseline characteristics of arts-dn: A randomized study to assess the safety and efficacy of finerenone in patients with type 2 diabetes mellitus and a clinical diagnosis of diabetic nephropathy
-
Ruilope LM, Agarwal R, Chan JC, et al. Rationale design, and baseline characteristics of ARTS-DN: a randomized study to assess the safety and efficacy of finerenone in patients with type 2 diabetes mellitus and a clinical diagnosis of diabetic nephropathy. Am J Nephrol 2014; 40:572-581.
-
(2014)
Am J Nephrol
, vol.40
, pp. 572-581
-
-
Ruilope, L.M.1
Agarwal, R.2
Chan, J.C.3
-
17
-
-
84941425176
-
Results of arts-dn: A randomized study to assess the safety and efficacy of finerenone in patients with type 2 diabetes and diabetic nephropathy
-
13-17 March 2015, Cape Town, South Africa Accessed 2 0 May 2015] ARTS-DN was a double-blind, placebo-controlled, parallel-group, multicenter study in patients with diabetic nephropathy (T2DM and albuminuria30 mg/g) receiving an ACE inhibitor or angiotensin receptor blocker and a serum potassium of at least 4.8 mmol/l at screening. Once-daily oral finerenone reduced albuminuria dose-dependently. Statistically significant differences in albuminuria reduction compared with placebo were observed with the four highest doses (7.5-20 mg once daily). The inci d ence of an eGFR decrease of at least 30% was not different between the placebo group and the finerenone groups. Hyperkalemia leading to discontinuation was not observed in the placebo and finerenone 10mg groups; incidences in the finerenone 7.515 and 20mg groups were as low as 2.1, 3.2 and 1.7%, respectively
-
Bakris GL, Nowack C, Ruilope LM. Results of ARTS-DN: a randomized study to assess the safety and efficacy of finerenone in patients with type 2 diabetes and diabetic nephropathy. In: World Congress of Nephrology 2015, 13-17 March 2015, Cape Town, South Africa http://www.abstracts2view.com/wcn/view.php?nu=WCN15L-SUN-488&terms=. [Accessed 2 0 May 2015] ARTS-DN was a double-blind, placebo-controlled, parallel-group, multicenter study in patients with diabetic nephropathy (T2DM and albuminuria30 mg/g) receiving an ACE inhibitor or angiotensin receptor blocker and a serum potassium of at least 4.8 mmol/l at screening. Once-daily oral finerenone reduced albuminuria dose-dependently. Statistically significant differences in albuminuria reduction compared with placebo were observed with the four highest doses (7.5-20 mg once daily). The inci d ence of an eGFR decrease of at least 30% was not different between the placebo group and the finerenone groups. Hyperkalemia leading to discontinuation was not observed in the placebo and finerenone 10mg groups; incidences in the finerenone 7.5, 15 and 20mg groups were as low as 2.1, 3.2 and 1.7%, respectively.
-
(2015)
World Congress of Nephrology
-
-
Bakris, G.L.1
Nowack, C.2
Ruilope, L.M.3
-
18
-
-
84922931063
-
Filippatos g rationale and design of mineralocorticoid receptor antagonist tolerability study-heart failure ( arts-hf): A randomized study of finerenone versus eplerenone in patients who have worsening chronic heart failure with diabetes and/or chronic kidney disease
-
Pitt B, Anker SD, Böhm M, et al. Filippatos G rationale and design of MinerAlocorticoid Receptor antagonist Tolerability Study-Heart Failure ( ARTS-HF): a randomized study of finerenone versus eplerenone in patients who have worsening chronic heart failure with diabetes and/or chronic kidney disease. Eur J Heart Failure 2015; 17:224-232.
-
(2015)
Eur J Heart Failure
, vol.17
, pp. 224-232
-
-
Pitt, B.1
Anker, S.D.2
Böhm, M.3
-
19
-
-
84923358879
-
Best of both worlds: Combining pharma data and state of the art modeling technology to improve in silico pka prediction
-
Fraczkiewi cz R, Lobell M, Göller AH, et al. Best of both worlds: combining pharma data and state of the art modeling technology to improve in silico pKa prediction. J Chem Inf Model 2015; 55:389-397.
-
(2015)
J Chem Inf Model
, vol.55
, pp. 389-397
-
-
Fraczkiewicz, R.1
Lobell, M.2
Göller, A.H.3
-
20
-
-
0034609833
-
Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties
-
Ertl P , Rohde B, Selzer P. Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties. J Med Chem 2000; 43:3714-3717.
-
(2000)
J Med Chem
, vol.43
, pp. 3714-3717
-
-
Ertl, P.1
Rohde, B.2
Selzer, P.3
-
21
-
-
84861554853
-
Discovery of bay 94-8862: A nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases
-
Bärfacker 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; 7:1385-13403.
-
(2012)
ChemMedChem
, vol.7
, pp. 1385-13403
-
-
Bärfacker, L.1
Kuhl, A.2
Hillisch, A.3
-
22
-
-
77955888805
-
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 recepto r (mr) antagonist for hypertension and nephropathy
-
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 recepto r (MR) antagonist for hypertension and nephropathy. J Med Chem 2010; 53:5979-6002.
-
(2010)
J Med Chem
, vol.53
, pp. 5979-6002
-
-
Meyers, M.J.1
Arhancet, G.B.2
Hockerman, S.L.3
-
23
-
-
84879693447
-
Discovery of novel oxazolidinedione derivatives as potent and selective mineraloco rticoid receptor antagonists
-
Yang C, Shen HC, WuZ, et al. Discovery of novel oxazolidinedione derivatives as potent and selective mineraloco rticoid receptor antagonists. Bioorg Med Chem Lett 2013; 23:4388-4392.
-
(2013)
Bioorg Med Chem Lett
, vol.23
, pp. 4388-4392
-
-
Yang, C.1
Shen, H.C.2
Wu, Z.3
-
24
-
-
84897381384
-
Mineralocorticoid receptor antagonists: Identification of heterocyclic amide replacements in the oxazolidinedione series
-
Cox JM, Chu HD, Yang C, et al. Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series. Bioorg Med Chem Lett 2014; 24:1681-1684.
-
(2014)
Bioorg Med Chem Lett
, vol.24
, pp. 1681-1684
-
-
Cox, J.M.1
Chu, H.D.2
Yang, C.3
-
25
-
-
79952786293
-
Sm-368229, a novel selective and potent nonsteroidal mineralocorticoid receptor antagonist with strong urinary na+ excretion activity
-
Nariai T, Fujita K, Mori M, et al. SM-368229, a novel selective and potent nonsteroidal mineralocorticoid receptor antagonist with strong urinary Na+ excretion activity. J Pharmacol Sci 2011; 115:346-353.
-
(2011)
J Pharmacol Sci
, vol.115
, pp. 346-353
-
-
Nariai, T.1
Fujita, K.2
Mori, M.3
-
26
-
-
84856505776
-
Antihypertensive and cardiorenal protective effects of sm-368229, a novel mineralocorticoid receptor antagonist, in aldosterone/salt-treated rats
-
Nariai T, Fujita K, Mori M, et al. Antihypertensive and cardiorenal protective effects of SM-368229, a novel mineralocorticoid receptor antagonist, in aldosterone/salt-treated rats. Pharmacology 2012; 89:44-52.
-
(2012)
Pharmacology
, vol.89
, pp. 44-52
-
-
Nariai, T.1
Fujita, K.2
Mori, M.3
-
27
-
-
84861098413
-
Sm-368229, a novel promising mineralocorticoid receptor antagonist, shows antihypertensive efficacy with minimal effect on serum potassium level in rats
-
Nariai T, Fujita K, Mori M, et al. SM-368229, a novel promising mineralocorticoid receptor antagonist, shows antihypertensive efficacy with minimal effect on serum potassium level in rats. J Cardiovasc Pharmacol 2012; 59:458-464.
-
(2012)
J Cardiovasc Pharmacol
, vol.59
, pp. 458-464
-
-
Nariai, T.1
Fujita, K.2
Mori, M.3
-
28
-
-
84939429572
-
Dsr-71167, a novel mineralocorticoid receptor antagonist with carbonic anhydrase inhibitory activity, s eparates urinary sodium excretion and serum potassium elevation in rats
-
[Epub ahead of print]
-
Nariai T, Fujita K, Kawane K, et al. DSR-71167, a novel mineralocorticoid receptor antagonist with carbonic anhydrase inhibitory activity, s eparates urinary sodium excretion and serum potassium elevation in rats. J Pharmacol Exp Ther 2015; 354:2-9; doi: 10.1124/jpet.114.221341. [Epub ahead of print].
-
(2015)
J Pharmacol Exp Ther
, vol.354
, pp. 2-9
-
-
Nariai, T.1
Fujita, K.2
Kawane, K.3
-
29
-
-
84055217558
-
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists
-
Hasui T, Matsunaga N, Ora T, et al. Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists. J Med Chem 2011; 54:8616-8631.
-
(2011)
J Med Chem
, vol.54
, pp. 8616-8631
-
-
Hasui, T.1
Matsunaga, N.2
Ora, T.3
-
30
-
-
84883456249
-
Design, synthesis and structure-Activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists
-
Hasui T, Ohra T, Ohyabu N, et al. Design, synthesis, and structure-Activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists. Bioorg Med Chem 2013; 21:5983-5994.
-
(2013)
Bioorg Med Chem
, vol.21
, pp. 5983-5994
-
-
Hasui, T.1
Ohra, T.2
Ohyabu, N.3
-
31
-
-
84907506017
-
Discovery of 6-[5-(4-fluorophenyl)-3-methylpyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists
-
Hasui T, Ohyabu N, Ohra T, et al. Discovery of 6-[5-(4-fluorophenyl)-3-methylpyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists. Bi oorg Med Chem 2014; 22: 5428-5445.
-
(2014)
Bioorg Med Chem
, vol.22
, pp. 5428-5445
-
-
Hasui, T.1
Ohyabu, N.2
Ohra, T.3
-
32
-
-
84861726854
-
-
ClinicalTrials.gov [online]). [Accessed 20 May 2015]
-
US National Library of Medicine. ClinicalTrials.gov [online] http://www.clinicaltrials. gov/ct2/show/NCT01889277 (2014). [Accessed 20 May 2015]
-
(2014)
US National Library of Medicine
-
-
-
33
-
-
84861726854
-
-
ClinicalTrials.gov [online]). [Accessed 20 May 2015]
-
US N ational Library of Medicine. ClinicalTrials.gov [online] http://www.clinicaltrials. gov/ct2/show/NCT02345057 (2015). [Accessed 20 May 2015]
-
(2015)
US National Library of Medicine
-
-
-
34
-
-
84861726854
-
-
ClinicalTrials.gov [online] [Accessed 20 May 2015]
-
US National Library of Medicine. ClinicalTrials.gov [online] http://www.clinicaltrials. gov/ct2/show/NCT02345044 (2015). [Accessed 20 May 2015]
-
(2015)
US National Library of Medicine
-
-
-
35
-
-
84901272015
-
Pf-03882845, a nonsteroidal mineralocorticoid receptor antagonist, prevents renal injury with reduced risk of hyperkalemia in an animal model of nephropathy
-
Orena S, Maurer TS, She L, et al. PF-03882845, a nonsteroidal mineralocorticoid receptor antagonist, prevents renal injury with reduced risk of hyperkalemia in an animal model of nephropathy. Front Pharmacol 2 013; 4:115. doi: 10.3389/fphar.2013.00115.
-
(2013)
Front Pharmacol
, vol.4
, pp. 115
-
-
Orena, S.1
Maurer, T.S.2
She, L.3
-
36
-
-
84901265587
-
Identification of (r)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1h-pyrazol-3-yl)-2-meth oxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist
-
Casimiro-Garcia A, Piotrowski DW, Ambler C, et al. Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-meth oxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist. J Med Chem 2014; 57:4273-4288.
-
(2014)
J Med Chem
, vol.57
, pp. 4273-4288
-
-
Casimiro-Garcia, A.1
Piotrowski, D.W.2
Ambler, C.3
-
37
-
-
84886949205
-
Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists
-
Futatsugi K,Piotrowski DW,Casimiro-Garcia A,et al. Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists. Bioorg Med Chem Lett 2013 23 6239-6242.
-
(2013)
Bioorg Med Chem Lett
, vol.23
, pp. 6239-6242
-
-
Futatsugi, K.1
Piotrowski, D.W.2
Casimiro-Garcia, A.3
-
38
-
-
84904267679
-
Finerenone, a novel selective nonsteroidal mineralocorticoid receptor antagonist protects from rat cardiorenal injury
-
In this study, the autho rs carefully determined minimal effective doses of finerenone and eplerenone with respect to acute renal electrolyte effects (natriuresis) and to chronic end-organ protective effects. They found that finerenone reduced cardiac hypertrophy and proteinuria more efficiently than eplerenone when comparing equinatriuretic doses
-
Kolkhof P, Delbeck M, Kretschmer A, et al. Finerenone, a novel selective nonsteroidal mineralocorticoid receptor antagonist protects from rat cardiorenal injury. J Cardiovasc Pharmacol 2014; 64:69-78. In this study, the autho rs carefully determined minimal effective doses of finerenone and eplerenone with respect to acute renal electrolyte effects (natriuresis) and to chronic end-organ protective effects. They found that finerenone reduced cardiac hypertrophy and proteinuria more efficiently than eplerenone when comparing equinatriuretic doses.
-
(2014)
J Cardiovasc Pharmacol
, vol.64
, pp. 69-78
-
-
Kolkhof, P.1
Delbeck, M.2
Kretschmer, A.3
-
39
-
-
84882321401
-
The arts of third-generation mineralocorticoid receptor antagonists: Achieving cardiovascular benefit with minimized renal side effects
-
Bauersachs J. The ARTS of third-generation mineralocorticoid receptor antagonists: achieving cardiovascular benefit with minimized renal side effects Eur Heart J 2013; 34:2426-2428.
-
(2013)
Eur Heart J
, vol.34
, pp. 2426-2428
-
-
Bauersachs, J.1
-
40
-
-
84907709951
-
Identification and characterization of a ligand-selective mineralocorticoid receptor coactivator
-
Rogerson FM, Yao YZ, Young MJ, Fuller PJ. Identification and characterization of a ligand-selective mineralocorticoid receptor coactivator. FASEB J 2014; 28:4200-4210
-
(2014)
FASEB J
, vol.28
, pp. 4200-4210
-
-
Rogerson, F.M.1
Yao, Y.Z.2
Young, M.J.3
Fuller, P.J.4
-
41
-
-
84929515429
-
Use of phage display to identify novel mineralocorticoid receptor-interacting proteins
-
These au thors identified eukaryotic elongation factor 1A1 (EEF1A1), structurespecific recognition protein 1 (SSRP1) and X-ray repair cross-complementing protein 6 (XRCC6) as novel interacting partners of the mineralocorticoid receptor. Interestingly, these cofact o rs demonstrated ligand-, promoter-And cell-specific modulation of mineralocorticoid receptor-mediated transactivation which would also support the concept of developing compounds which may possess tissuespecific MRA activity
-
Yang J, Fuller PJ, Morgan J, et al. Use of phage display to identify novel mineralocorticoid receptor-interacting proteins. Mol Endocrinol 2014; 28:1571-1584. These au thors identified eukaryotic elongation factor 1A1 (EEF1A1), structurespecific recognition protein 1 (SSRP1) and X-ray repair cross-complementing protein 6 (XRCC6) as novel interacting partners of the mineralocorticoid receptor. Interestingly, these cofact o rs demonstrated ligand-, promoter-And cell-specific modulation of mineralocorticoid receptor-mediated transactivation which would also support the concept of developing compounds which may possess tissuespecific MRA activity.
-
(2014)
Mol Endocrinol
, vol.28
, pp. 1571-1584
-
-
Yang, J.1
Fuller, P.J.2
Morgan, J.3
-
42
-
-
84929091720
-
Gemin4 functions as a coregulator of the mineralocorticoid receptor
-
Yan g J, Fuller PJ, Morgan J, et al. GEMIN4 functions as a coregulator of the mineralocorticoid receptor. J Mol Endocrinol 2015; 54:149-160.
-
(2015)
J Mol Endocrinol
, vol.54
, pp. 149-160
-
-
Yang, J.1
Fuller, P.J.2
Morgan, J.3
-
43
-
-
84887432790
-
Mineralocorticoid receptor phosphorylation regulates ligand binding and renal response to volume depletion and hyperkalemia
-
Shibata S, Rinehart J, Zhang J, et al. Mineralocorticoid receptor phosphorylation regulates ligand binding and renal response to volume depletion and hyperkalemia. Cell Metab 2013; 18:660-671.
-
(2013)
Cell Metab
, vol.18
, pp. 660-671
-
-
Shibata, S.1
Rinehart, J.2
Zhang, J.3
-
44
-
-
84856351941
-
Central regulation of blood pressure by the mineralocorticoid receptor
-
Gomez-Sanchez EP, Gomez-Sanchez CE. Central regulation of blood pressure by the mineralocorticoid receptor. Mol Cell Endocrinol 2012; 350:289-298.
-
(2012)
Mol Cell Endocrinol
, vol.350
, pp. 289-298
-
-
Gomez-Sanchez, E.P.1
Gomez-Sanchez, C.E.2
-
45
-
-
80053175990
-
Pubchem3d: A new resource for scientists
-
Bolton EE, Chen J, Kim S, et al. PubChem3D: a new resource for scientists. J Cheminform 2011; 3:32.
-
(2011)
J Cheminform
, vol.3
, pp. 32
-
-
Bolton, E.E.1
Chen, J.2
Kim, S.3
-
47
-
-
0028986469
-
The two faces of a steroid antagonist: When an antagonist isn't
-
Nordeen SK, Bona BJ, Beck CA, et al. The two faces of a steroid antagonist: when an antagonist isn't. Steroids 1995; 60:97-104.
-
(1995)
Steroids
, vol.60
, pp. 97-104
-
-
Nordeen, S.K.1
Bona, B.J.2
Beck, C.A.3
-
48
-
-
0031034423
-
Cell-specific, promoter-dependent mineralocorticoid agonist activity of spironolactone
-
Massaad C, Lombé s M, Aggerbeck M, et al. Cell-specific, promoter-dependent mineralocorticoid agonist activity of spironolactone. Mol Pharmacol 1997; 51:285-292.
-
(1997)
Mol Pharmacol
, vol.51
, pp. 285-292
-
-
Massaad, C.1
Lombé, S.M.2
Aggerbeck, M.3
-
49
-
-
77956909015
-
A new mode of mineralocorticoid receptor antagonism by a potent and selective nonsteroidal molecule
-
Fagart J, H illisch A, Huyet J, et al. A new mode of mineralocorticoid receptor antagonism by a potent and selective nonsteroidal molecule. J Biol Chem 2010; 285:29932-29940.
-
(2010)
J Biol Chem
, vol.285
, pp. 29932-29940
-
-
Fagart, J.1
Hillisch, A.2
Huyet, J.3
-
50
-
-
22344444725
-
The ligand-dependent interaction of mineralocorticoid receptor with coactivator and corepressor peptides suggests multiple activation mechanisms
-
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; 19:1460-1473.
-
(2005)
Mol Endocrinol
, vol.19
, pp. 1460-1473
-
-
Hultman, M.L.1
Krasnoperova, N.V.2
Li, S.3
-
51
-
-
84942642642
-
Effects of finerenone, a novel nonsteroidal mineralocorticoid receptor antagonist in a model of pressure overload-induced cardiac hypertrophy. in
-
San Francisco, CA, Hypertension 64 (-):ABSTR007
-
Grune J, Benz V, Brix S, et al. Effects of finerenone, a novel nonsteroidal mineralocorticoid receptor antagonist in a model of pressure overload-induced cardiac hypertrophy. In: Conference American Heart Association's High Blood Pre ssure Research 2014 Scientific Sessions, HBPR 2014, San Francisco, CA, Hypertension 64 (-):ABSTR 007 (2014).
-
(2014)
Conference American Heart Association's High Blood Pre Ssure Research 2014 Scientific Sessions, HBPR 2014
-
-
Grune, J.1
Benz, V.2
Brix, S.3
-
52
-
-
0037192501
-
Molecular determinants for the tissue specificity of serms
-
Shang Y, Brown M. Molecular determinants for the tissue specificity of SERMs. Science 2002; 295:2465-2468.
-
(2002)
Science
, vol.295
, pp. 2465-2468
-
-
Shang, Y.1
Brown, M.2
|