-
2
-
-
84858002935
-
Aldosterone and the Heart: From Basic Research to Clinical Evidence
-
Catena, C.; Colussi, G.; Marzano, L.; Sechi, L. A. Aldosterone and the Heart: From Basic Research to Clinical Evidence Horm. Metab. Res. 2012, 44, 181-187
-
(2012)
Horm. Metab. Res.
, vol.44
, pp. 181-187
-
-
Catena, C.1
Colussi, G.2
Marzano, L.3
Sechi, L.A.4
-
3
-
-
84858008314
-
Aldosterone and the Kidney
-
Fourkiotis, V. G.; Hanslik, G.; Hanusch, F.; Lepenies, J.; Quinkle, M. Aldosterone and the Kidney Horm. Metab. Res. 2012, 44, 194-201
-
(2012)
Horm. Metab. Res.
, vol.44
, pp. 194-201
-
-
Fourkiotis, V.G.1
Hanslik, G.2
Hanusch, F.3
Lepenies, J.4
Quinkle, M.5
-
4
-
-
80052529403
-
Aldosterone Blockers (Mineralocorticoid Receptor Antagonism) and Potassium-Sparing Diuretics
-
Epstein, M.; Calhoun, D. A. Aldosterone Blockers (Mineralocorticoid Receptor Antagonism) and Potassium-Sparing Diuretics J. Clin. Hypertens. 2011, 13, 644-648
-
(2011)
J. Clin. Hypertens.
, vol.13
, pp. 644-648
-
-
Epstein, M.1
Calhoun, D.A.2
-
5
-
-
8844262660
-
Principles for Modulation of the Nuclear Receptor Superfamily
-
Gronemeyer, H.; Gustafsson, J.-A.; Laudet, V. Principles for Modulation of the Nuclear Receptor Superfamily Nat. Rev. Drug Discovery 2004, 3, 950-964
-
(2004)
Nat. Rev. Drug Discovery
, vol.3
, pp. 950-964
-
-
Gronemeyer, H.1
Gustafsson, J.-A.2
Laudet, V.3
-
6
-
-
33646772536
-
The Nuclear Receptor Superfamily and Drug Discovery
-
Moore, J. T.; Collins, J. L.; Pearce, K. H. The Nuclear Receptor Superfamily and Drug Discovery ChemMedChem 2006, 1, 504-523
-
(2006)
ChemMedChem
, vol.1
, pp. 504-523
-
-
Moore, J.T.1
Collins, J.L.2
Pearce, K.H.3
-
7
-
-
80054120294
-
Recent Advances in Mineralocorticoid Receptor Antagonists
-
Macor, J. E. Academic Press: Boston, MA, Chapter 6
-
Leftheris, K.; Zheng, Y.; Lala, D. S. Recent Advances in Mineralocorticoid Receptor Antagonists. In Annual Reports in Medicinal Chemistry; Macor, J. E., Ed.; Academic Press: Boston, MA, 2011; Vol. 46, Chapter 6.
-
(2011)
Annual Reports in Medicinal Chemistry
, vol.46
-
-
Leftheris, K.1
Zheng, Y.2
Lala, D.S.3
-
8
-
-
84555190258
-
Emerging Drugs Which Target the Renin-Angiotensin-Aldosterone System
-
Steckelings, U. M.; Paulis, L.; Unger, T.; Bader, M. Emerging Drugs Which Target the Renin-Angiotensin-Aldosterone System Expert Opin. Emerging Drugs 2011, 16, 619-630
-
(2011)
Expert Opin. Emerging Drugs
, vol.16
, pp. 619-630
-
-
Steckelings, U.M.1
Paulis, L.2
Unger, T.3
Bader, M.4
-
9
-
-
84856347698
-
Aldosterone and Mineralocorticoid Receptors: A Personal Reflection
-
Funder, J. W. Aldosterone and Mineralocorticoid Receptors: A Personal Reflection Mol. Cell. Endocrinol. 2012, 350, 146-150
-
(2012)
Mol. Cell. Endocrinol.
, vol.350
, pp. 146-150
-
-
Funder, J.W.1
-
10
-
-
84856335862
-
Tissue-Specific Modulation of Mineralocorticoid Receptor Function by 11β-Hydroxysteroid Dehydrogenases: An Overview
-
Odermatt, A.; Kratschmar, D. V. Tissue-Specific Modulation of Mineralocorticoid Receptor Function by 11β-Hydroxysteroid Dehydrogenases: An Overview Mol. Cell. Endocrinol. 2012, 350, 168-186
-
(2012)
Mol. Cell. Endocrinol.
, vol.350
, pp. 168-186
-
-
Odermatt, A.1
Kratschmar, D.V.2
-
11
-
-
84856326788
-
Structural Determinants of Ligand Binding to the Mineralocorticoid Receptor
-
Huyet, J.; Pinon, G. M.; Fay, M. R.; Rafestin-Oblin, M.-E.; Fagart, J. Structural Determinants of Ligand Binding to the Mineralocorticoid Receptor Mol. Cell. Endocrinol. 2012, 350, 187-195
-
(2012)
Mol. Cell. Endocrinol.
, vol.350
, pp. 187-195
-
-
Huyet, J.1
Pinon, G.M.2
Fay, M.R.3
Rafestin-Oblin, M.-E.4
Fagart, J.5
-
12
-
-
84856315210
-
Interactions of the Mineralocorticoid Receptor-Within and Without
-
Yang, J.; Fuller, P. J. Interactions of the Mineralocorticoid Receptor-Within and Without Mol. Cell. Endocrinol. 2012, 350, 196-205
-
(2012)
Mol. Cell. Endocrinol.
, vol.350
, pp. 196-205
-
-
Yang, J.1
Fuller, P.J.2
-
13
-
-
84856346254
-
Mechanisms of Mineralocorticoid Salt-Induced Hypertension and Cardiac Fibrosis
-
Young, M. J.; Rickard, A. J. Mechanisms of Mineralocorticoid Salt-Induced Hypertension and Cardiac Fibrosis Mol. Cell. Endocrinol. 2012, 350, 248-255
-
(2012)
Mol. Cell. Endocrinol.
, vol.350
, pp. 248-255
-
-
Young, M.J.1
Rickard, A.J.2
-
14
-
-
84856325649
-
Mineralocorticoid Receptors in Vascular Function and Disease
-
McCurley, A.; Jaffe, I. Z. Mineralocorticoid Receptors in Vascular Function and Disease Mol. Cell. Endocrinol. 2012, 350, 256-265
-
(2012)
Mol. Cell. Endocrinol.
, vol.350
, pp. 256-265
-
-
McCurley, A.1
Jaffe, I.Z.2
-
15
-
-
84856339877
-
Aldosterone, Mineralocorticoid Receptor, and Heart Failure
-
Messaoudi, S.; Azibani, F.; Delcayre, C.; Jaisser, F. Aldosterone, Mineralocorticoid Receptor, and Heart Failure Mol. Cell. Endocrinol. 2012, 350, 266-272
-
(2012)
Mol. Cell. Endocrinol.
, vol.350
, pp. 266-272
-
-
Messaoudi, S.1
Azibani, F.2
Delcayre, C.3
Jaisser, F.4
-
16
-
-
84856318868
-
Mineralocorticoid Receptors in the Pathophysiology of Chronic Kidney Diseases and the Metabolic Syndrome
-
Shibata, S.; Fujita, T. Mineralocorticoid Receptors in the Pathophysiology of Chronic Kidney Diseases and the Metabolic Syndrome Mol. Cell. Endocrinol. 2012, 350, 273-280
-
(2012)
Mol. Cell. Endocrinol.
, vol.350
, pp. 273-280
-
-
Shibata, S.1
Fujita, T.2
-
17
-
-
84856351941
-
Central Regulation of Blood Pressure by the Mineralocorticoid Receptor
-
Gomez-Sanchez, E. P.; Gomez-Sanchez, C. E. 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
-
18
-
-
84856277878
-
Mineralocorticoid and Glucocorticoid Receptors at the Neuronal Membrane, Regulators of Nongenomic Corticosteroid Signaling
-
Groeneweg, F. L.; Karst, H.; de Kloet, E. R.; Joëls, M. Mineralocorticoid and Glucocorticoid Receptors at the Neuronal Membrane, Regulators of Nongenomic Corticosteroid Signaling Mol. Cell. Endocrinol. 2012, 350, 299-309
-
(2012)
Mol. Cell. Endocrinol.
, vol.350
, pp. 299-309
-
-
Groeneweg, F.L.1
Karst, H.2
De Kloet, E.R.3
Joëls, M.4
-
19
-
-
84856337738
-
Molecular Pharmacology of the Mineralocorticoid Receptor: Prospects for Novel Therapeutics
-
Kolkhof, P.; Borden, S. A. 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
-
20
-
-
68149160053
-
Physicochemical Drug Properties Associated with in Vivo Toxicological Outcomes: A Review
-
Price, D. A.; Blagg, J.; Jones, L.; Greene, N.; Wager, T. Physicochemical Drug Properties Associated with in Vivo Toxicological Outcomes: A Review Expert Opin. Drug Metab. Toxicol. 2009, 5, 921-931
-
(2009)
Expert Opin. Drug Metab. Toxicol.
, vol.5
, pp. 921-931
-
-
Price, D.A.1
Blagg, J.2
Jones, L.3
Greene, N.4
Wager, T.5
-
21
-
-
80052974259
-
Improving Drug Candidates by Design: A Focus on Physicochemical Properties as a Means of Improving Compound Disposition and Safety
-
Meanwell, N. A. Improving Drug Candidates by Design: A Focus on Physicochemical Properties as a Means of Improving Compound Disposition and Safety Chem. Res. Toxicol. 2011, 24, 1420-1456
-
(2011)
Chem. Res. Toxicol.
, vol.24
, pp. 1420-1456
-
-
Meanwell, N.A.1
-
22
-
-
33745636105
-
The Evolution of Mineralocorticoid Receptors
-
Hu, X.; Funder, J. W. The Evolution of Mineralocorticoid Receptors Mol. Endocrinol. 2006, 20, 1471-1478
-
(2006)
Mol. Endocrinol.
, vol.20
, pp. 1471-1478
-
-
Hu, X.1
Funder, J.W.2
-
23
-
-
2342511545
-
The 45-Year Story of the Development of an Anti-Aldosterone More Specific than Spironolactone
-
Ménard, J. The 45-Year Story of the Development of an Anti-Aldosterone More Specific than Spironolactone Mol. Cell. Endocrinol. 2004, 217, 45-52
-
(2004)
Mol. Cell. Endocrinol.
, vol.217
, pp. 45-52
-
-
Ménard, J.1
-
24
-
-
2342563102
-
Drospirenone, a Progestogen with Antimineralocorticoid Properties: A Short Review
-
Oelkers, W. Drospirenone, a Progestogen with Antimineralocorticoid Properties: A Short Review Mol. Cell. Endocrinol. 2004, 217, 255-261
-
(2004)
Mol. Cell. Endocrinol.
, vol.217
, pp. 255-261
-
-
Oelkers, W.1
-
25
-
-
0016687047
-
Antiandrogenic Effect of Spirolactones: Mechanism of Action
-
Corvol, P.; Michaud, A.; Menard, J.; Freifeld, M.; Mahoudeau, J. Antiandrogenic Effect of Spirolactones: Mechanism of Action Endocrinology 1975, 97, 52-58
-
(1975)
Endocrinology
, vol.97
, pp. 52-58
-
-
Corvol, P.1
Michaud, A.2
Menard, J.3
Freifeld, M.4
Mahoudeau, J.5
-
26
-
-
0036786124
-
Eplerenone-A Novel Selective Aldosterone Blocker
-
Zillich, A. J.; Carter, B. L. Eplerenone-A Novel Selective Aldosterone Blocker Ann. Pharmacother. 2002, 36, 1567-1576
-
(2002)
Ann. Pharmacother.
, vol.36
, pp. 1567-1576
-
-
Zillich, A.J.1
Carter, B.L.2
-
27
-
-
0037417252
-
Eplerenone, a Selective Aldosterone Blocker, in Patients with Left Ventricular Dysfunction after Myocardial Infarction
-
Pitt, B.; Remme, W.; Zannad, F.; Neaton, J.; Martinez, F.; Roniker, B.; Bittman, R.; Hurley, S.; Kleiman, J.; Gatlin, M. Eplerenone, a Selective Aldosterone Blocker, in Patients with Left Ventricular Dysfunction after Myocardial Infarction N. Engl. J. Med. 2003, 348, 1309-1321
-
(2003)
N. Engl. J. Med.
, vol.348
, pp. 1309-1321
-
-
Pitt, B.1
Remme, W.2
Zannad, F.3
Neaton, J.4
Martinez, F.5
Roniker, B.6
Bittman, R.7
Hurley, S.8
Kleiman, J.9
Gatlin, M.10
-
28
-
-
81855183776
-
Mineralocorticoid Receptor Antagonists for Heart Failure
-
For a recent review of multiple clinical studies with MR antagonists, see the following: Richards, A. M. Mineralocorticoid Receptor Antagonists for Heart Failure Expert Opin. Pharmacother. 2011, 12, 2801-2815
-
(2011)
Expert Opin. Pharmacother.
, vol.12
, pp. 2801-2815
-
-
Richards, A.M.1
-
29
-
-
69749100645
-
Predictors of Hyperkalemia Risk following Hypertension Control with Aldosterone Blockade
-
Khosla, N.; Kalaitzidis, R.; Bakris, G. L. Predictors of Hyperkalemia Risk following Hypertension Control with Aldosterone Blockade Am. J. Nephrol. 2009, 30, 418-424
-
(2009)
Am. J. Nephrol.
, vol.30
, pp. 418-424
-
-
Khosla, N.1
Kalaitzidis, R.2
Bakris, G.L.3
-
30
-
-
84860367978
-
Aldosterone Blockade and the Mineralocorticoid Receptor in the Management of Chronic Kidney Disease: Current Concepts and Emerging Treatment Paradigms
-
Shavit, L.; Lifschitz, M. D.; Epstein, M. Aldosterone Blockade and the Mineralocorticoid Receptor in the Management of Chronic Kidney Disease: Current Concepts and Emerging Treatment Paradigms Kidney Int. 2012, 81, 955-968
-
(2012)
Kidney Int.
, vol.81
, pp. 955-968
-
-
Shavit, L.1
Lifschitz, M.D.2
Epstein, M.3
-
31
-
-
0019732922
-
Chemical Suppression of Steroidogenesis
-
Colby, H. D. Chemical Suppression of Steroidogenesis Environ. Health Perspect. 1981, 38, 119-127
-
(1981)
Environ. Health Perspect.
, vol.38
, pp. 119-127
-
-
Colby, H.D.1
-
32
-
-
67649371482
-
Interactions between Human Cytochrome P450 Enzymes and Steroids: Physiological and Pharmacological Implications
-
Zhang, Y.-Y.; Yang, L. Interactions between Human Cytochrome P450 Enzymes and Steroids: Physiological and Pharmacological Implications Expert Opin. Drug Metab. Toxicol. 2009, 5, 621-629
-
(2009)
Expert Opin. Drug Metab. Toxicol.
, vol.5
, pp. 621-629
-
-
Zhang, Y.-Y.1
Yang, L.2
-
33
-
-
60249091230
-
Contrasting Effects of Eplerenone and Spironolactone on Adrenal Cell Steroidogenesis
-
Ye, P.; Yamashita, T.; Pollock, D. M.; Sasano, H.; Rainey, W. E. Contrasting Effects of Eplerenone and Spironolactone on Adrenal Cell Steroidogenesis Horm. Metab. Res. 2009, 41, 35-39
-
(2009)
Horm. Metab. Res.
, vol.41
, pp. 35-39
-
-
Ye, P.1
Yamashita, T.2
Pollock, D.M.3
Sasano, H.4
Rainey, W.E.5
-
34
-
-
0022578468
-
Correspondence Analysis Applied to Steroid Receptor Binding
-
Dore, J.-C.; Gilbert, J.; Ojasoo, T.; Raynaudt, J.-P. Correspondence Analysis Applied to Steroid Receptor Binding J. Med. Chem. 1986, 29, 54-60
-
(1986)
J. Med. Chem.
, vol.29
, pp. 54-60
-
-
Dore, J.-C.1
Gilbert, J.2
Ojasoo, T.3
Raynaudt, J.-P.4
-
35
-
-
0032526977
-
Antagonism in the Human Mineralocorticoid Receptor
-
Fagart, J.; Wurtz, J. M.; Souque, A.; Hellal-Levy, C.; Moras, D.; Rafestin-Oblin, M. E. Antagonism in the Human Mineralocorticoid Receptor EMBO J. 1998, 17, 3317-3325
-
(1998)
EMBO J.
, vol.17
, pp. 3317-3325
-
-
Fagart, J.1
Wurtz, J.M.2
Souque, A.3
Hellal-Levy, C.4
Moras, D.5
Rafestin-Oblin, M.E.6
-
36
-
-
77953325281
-
Improved Docking, Screening and Selectivity Prediction for Small Molecule Nuclear Receptor Modulators Using Conformational Ensembles
-
Park, S.-J.; Kufareva, I.; Abagyan, R. Improved Docking, Screening and Selectivity Prediction for Small Molecule Nuclear Receptor Modulators Using Conformational Ensembles J. Comput.-Aided Mol. Des. 2010, 24, 459-471
-
(2010)
J. Comput.-Aided Mol. Des.
, vol.24
, pp. 459-471
-
-
Park, S.-J.1
Kufareva, I.2
Abagyan, R.3
-
37
-
-
84866880867
-
Molecular Recognition of Nuclear Receptor-Ligand Complexes
-
Babine, R. E. Abdel-Meguid, S. S. Wiley-VCH: Weinheim, Germany, Chapter 1.
-
Babine, R. E. Molecular Recognition of Nuclear Receptor-Ligand Complexes. In Protein Crystallography in Drug Discovery; Babine, R. E.; Abdel-Meguid, S. S., Eds.; Wiley-VCH: Weinheim, Germany, 2004; Chapter 1.
-
(2004)
Protein Crystallography in Drug Discovery
-
-
Babine, R.E.1
-
38
-
-
77951901129
-
Structural Overview of the Nuclear Receptor Superfamily: Insights into Physiology and Therapeutics
-
Huang, P.; Chandra, V.; Rastinejad, F. Structural Overview of the Nuclear Receptor Superfamily: Insights into Physiology and Therapeutics Annu. Rev. Physiol. 2010, 72, 247-272
-
(2010)
Annu. Rev. Physiol.
, vol.72
, pp. 247-272
-
-
Huang, P.1
Chandra, V.2
Rastinejad, F.3
-
39
-
-
4544376911
-
New Naturally Occurring Missense Mutations of the Human Mineralocorticoid Receptor Disclose Important Residues Involved in Dynamic Interactions with Deoxyribonucleic Acid, Intracellular Trafficking, and Ligand Binding
-
Sartorato, P.; Cluzeaud, F.; Fagart, J.; Viengchareun, S.; Lombès, M.; Zennaro, M.-C. New Naturally Occurring Missense Mutations of the Human Mineralocorticoid Receptor Disclose Important Residues Involved in Dynamic Interactions with Deoxyribonucleic Acid, Intracellular Trafficking, and Ligand Binding Mol. Endocrinol. 2004, 18, 2151-2165
-
(2004)
Mol. Endocrinol.
, vol.18
, pp. 2151-2165
-
-
Sartorato, P.1
Cluzeaud, F.2
Fagart, J.3
Viengchareun, S.4
Lombès, M.5
Zennaro, M.-C.6
-
40
-
-
2342456441
-
Identification of Steroid Ligands Able to Inactivate the Mineralocorticoid Receptor Harboring the S810L Mutation Responsible for a Severe Form of Hypertension
-
Pinon, G. M.; Fagart, J.; Souque, A.; Auzoub, G.; Vandewalle, A.; Rafestin-Oblin, M.-E. Identification of Steroid Ligands Able To Inactivate the Mineralocorticoid Receptor Harboring the S810L Mutation Responsible for a Severe Form of Hypertension Mol. Cell. Endocrinol. 2004, 217, 181-188
-
(2004)
Mol. Cell. Endocrinol.
, vol.217
, pp. 181-188
-
-
Pinon, G.M.1
Fagart, J.2
Souque, A.3
Auzoub, G.4
Vandewalle, A.5
Rafestin-Oblin, M.-E.6
-
41
-
-
33846180691
-
Non-Steroidal Mineralocorticoid Receptor Antagonists
-
Meyers, M. J.; Hu, X. Non-Steroidal Mineralocorticoid Receptor Antagonists Expert Opin. Ther. Pat. 2007, 17, 17-23
-
(2007)
Expert Opin. Ther. Pat.
, vol.17
, pp. 17-23
-
-
Meyers, M.J.1
Hu, X.2
-
42
-
-
68949119585
-
The Topology of Drug-Target Interaction Networks: Implicit Dependence on Drug Properties and Target Families
-
Mestres, J.; Gregori-Puigjané, E.; Valverde, S.; Sole, R. S. The Topology of Drug-Target Interaction Networks: Implicit Dependence on Drug Properties and Target Families Mol. BioSyst. 2009, 5, 1051-1057
-
(2009)
Mol. BioSyst.
, vol.5
, pp. 1051-1057
-
-
Mestres, J.1
Gregori-Puigjané, E.2
Valverde, S.3
Sole, R.S.4
-
43
-
-
33644855557
-
Recent Developments in Focused Library Design: Targeting Gene-Families
-
Miller, J. L. Recent Developments in Focused Library Design: Targeting Gene-Families Curr. Top. Med. Chem. 2006, 6, 19-29
-
(2006)
Curr. Top. Med. Chem.
, vol.6
, pp. 19-29
-
-
Miller, J.L.1
-
44
-
-
79960021792
-
Target Validation: Linking Target and Chemical Properties to Desired Product Profile
-
Wyatt, P. G.; Gilbert, I. H.; Read, K. D.; Fairlamb, A. H. Target Validation: Linking Target and Chemical Properties to Desired Product Profile Curr. Top. Med. Chem. 2011, 11, 1275-1283
-
(2011)
Curr. Top. Med. Chem.
, vol.11
, pp. 1275-1283
-
-
Wyatt, P.G.1
Gilbert, I.H.2
Read, K.D.3
Fairlamb, A.H.4
-
45
-
-
33746156959
-
Global Mapping of Pharmacological Space
-
Paolini, G. V.; Shapland, R. H. B.; van Hoorn, W. P.; Mason, J. S.; Hopkins, A. L. Global Mapping of Pharmacological Space Nat. Biotechnol. 2006, 24, 805-815
-
(2006)
Nat. Biotechnol.
, vol.24
, pp. 805-815
-
-
Paolini, G.V.1
Shapland, R.H.B.2
Van Hoorn, W.P.3
Mason, J.S.4
Hopkins, A.L.5
-
46
-
-
33745126636
-
Dependence of Molecular Properties on Proteomic Family for Marketed Oral Drugs
-
Vieth, M.; Sutherland, J. J. Dependence of Molecular Properties on Proteomic Family for Marketed Oral Drugs J. Med. Chem. 2006, 49, 3451-3453
-
(2006)
J. Med. Chem.
, vol.49
, pp. 3451-3453
-
-
Vieth, M.1
Sutherland, J.J.2
-
47
-
-
33646715920
-
The Influence of Target Family and Functional Activity on the Physicochemical Properties of Pre-Clinical Compounds
-
Morphy, R. The Influence of Target Family and Functional Activity on the Physicochemical Properties of Pre-Clinical Compounds J. Med. Chem. 2006, 49, 2969-2978
-
(2006)
J. Med. Chem.
, vol.49
, pp. 2969-2978
-
-
Morphy, R.1
-
48
-
-
84872430490
-
-
Pipeline on Eli Lilly Web site at
-
Pipeline on Eli Lilly Web site at http://www.lilly.com.
-
-
-
-
49
-
-
84872429900
-
-
Information obtained from
-
Information obtained from http://clinicaltrials.gov.
-
-
-
-
50
-
-
77956909015
-
A New Mode of Mineralocorticoid Receptor Antagonism by a Potent and Selective Nonsteroidal Molecule
-
Fagart, J.; Hillisch, A.; Huyet, J.; Barfacker, L.; Fay, M.; Pleiss, U.; Pook, E.; Schafer, S.; Rafestin-Oblin, M.-E.; Kolkhof, P. 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
Barfacker, L.4
Fay, M.5
Pleiss, U.6
Pook, E.7
Schafer, S.8
Rafestin-Oblin, M.-E.9
Kolkhof, P.10
-
51
-
-
77956918665
-
-
PCT Int. Appl. WO2007025604
-
Kuhl, A.; Kolkhof, P.; Heckroth, H.; Schlemmer, K.-H.; Flamme, I.; Figueroa Perez, S.; Gielen-Haertwig, H.; Grosser, R.; Erguden, J.-K.; Lang, D. 4-Chromenonyl-1,4-dihydropyridines and Their Use. PCT Int. Appl. WO2007025604, 2007.
-
(2007)
4-Chromenonyl-1,4-dihydropyridines and Their Use
-
-
Kuhl, A.1
Kolkhof, P.2
Heckroth, H.3
Schlemmer, K.-H.4
Flamme, I.5
Figueroa Perez, S.6
Gielen-Haertwig, H.7
Grosser, R.8
Erguden, J.-K.9
Lang, D.10
-
52
-
-
77955878489
-
-
PCT Int. Appl. WO2008104306
-
Barfacker, L.; Kolkhof, P.; Schlemmer, K.-H.; Grosser, R.; Nitsche, A.; Klein, M.; Munter, K.; Albrecht-Kupper, B.; Hartmann, E. Substituted 4-Aryl-1,4-dihydro-1,6-naphthyridinamides and Use Thereof. PCT Int. Appl. WO2008104306, 2008.
-
(2008)
Substituted 4-Aryl-1,4-dihydro-1,6-naphthyridinamides and Use Thereof
-
-
Barfacker, L.1
Kolkhof, P.2
Schlemmer, K.-H.3
Grosser, R.4
Nitsche, A.5
Klein, M.6
Munter, K.7
Albrecht-Kupper, B.8
Hartmann, E.9
-
53
-
-
84872428699
-
-
Information disclosed on Bayer Trial Finder Web site at
-
Information disclosed on Bayer Trial Finder Web site at http://www.bayerhealthcare.com.
-
-
-
-
54
-
-
39749199510
-
A Number of Marketed Dihydropyridine Calcium Channel Blockers Have Mineralocorticoid Receptor Antagonist Activity
-
Dietz, J. D.; Du, S.; Bolten, C. W.; Payne, M. A.; Xia, C.; Blinn, J. R.; Funder, J. W.; Hu, X. A Number of Marketed Dihydropyridine Calcium Channel Blockers Have Mineralocorticoid Receptor Antagonist Activity Hypertension 2008, 51, 742-748
-
(2008)
Hypertension
, vol.51
, pp. 742-748
-
-
Dietz, J.D.1
Du, S.2
Bolten, C.W.3
Payne, M.A.4
Xia, C.5
Blinn, J.R.6
Funder, J.W.7
Hu, X.8
-
55
-
-
77952727090
-
Stereochemical Requirements for the Mineralocorticoid Receptor Antagonist Activity of Dihydropyridines
-
Arhancet, G. B.; Woodard, S. S.; Dietz, J. D.; Garland, D. J.; Wagner, G. M.; Iyanar, K.; Collins, J. T.; Blinn, J. R.; Numann, R. E.; Hu, X.; Huang, H.-C. Stereochemical Requirements for the Mineralocorticoid Receptor Antagonist Activity of Dihydropyridines J. Med. Chem. 2010, 53, 4300-4304
-
(2010)
J. Med. Chem.
, vol.53
, pp. 4300-4304
-
-
Arhancet, G.B.1
Woodard, S.S.2
Dietz, J.D.3
Garland, D.J.4
Wagner, G.M.5
Iyanar, K.6
Collins, J.T.7
Blinn, J.R.8
Numann, R.E.9
Hu, X.10
Huang, H.-C.11
-
56
-
-
77955907538
-
Discovery of Novel Cyanodihydropyridines as Potent Mineralocorticoid Receptor Antagonists
-
Arhancet, G. B.; Woodard, S. S.; Iyanar, K.; Case, B. L.; Woerndle, R.; Dietz, J. D.; Garland, D. J.; Collins, J. T.; Payne, M. A.; Blinn, J. R.; Pomposiello, S. I.; Hu, X.; Heron, M. I.; Huang, H. C.; Lee, L. F. Discovery of Novel Cyanodihydropyridines as Potent Mineralocorticoid Receptor Antagonists J. Med. Chem. 2010, 53, 5970-5978
-
(2010)
J. Med. Chem.
, vol.53
, pp. 5970-5978
-
-
Arhancet, G.B.1
Woodard, S.S.2
Iyanar, K.3
Case, B.L.4
Woerndle, R.5
Dietz, J.D.6
Garland, D.J.7
Collins, J.T.8
Payne, M.A.9
Blinn, J.R.10
Pomposiello, S.I.11
Hu, X.12
Heron, M.I.13
Huang, H.C.14
Lee, L.F.15
-
57
-
-
77955888805
-
Discovery of (3 S,3a R)-2-(3-Chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4, 5-tetrahydro-2 H -benzo[ g ]indazole-7-carboxylic Acid (PF-3882845), an Orally Efficacious Mineralocorticoid Receptor (MR) Antagonist for Hypertension and Nephropathy
-
Meyers, M. J.; Arhancet, G. B.; Hockerman, S. L.; Chen, X.; Long, S. A.; Mahoney, M. W.; Rico, J. R.; Garland, D. J.; Blinn, J. R.; Collins, J. T.; Yang, S.; Huang, H.-C.; McGee, K. F.; Wendling, J. M.; Dietz, J. D.; Payne, M. A.; Homer, B. L.; Heron, M. I.; Reitz, D. B.; Hu, X. Discovery of (3 S,3a R)-2-(3-Chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2 H -benzo[ g ]indazole-7-carboxylic Acid (PF-3882845), an Orally Efficacious Mineralocorticoid Receptor (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
Chen, X.4
Long, S.A.5
Mahoney, M.W.6
Rico, J.R.7
Garland, D.J.8
Blinn, J.R.9
Collins, J.T.10
Yang, S.11
Huang, H.-C.12
McGee, K.F.13
Wendling, J.M.14
Dietz, J.D.15
Payne, M.A.16
Homer, B.L.17
Heron, M.I.18
Reitz, D.B.19
Hu, X.20
more..
-
58
-
-
80054716865
-
The Use of Plasma Aldosterone and Urinary Sodium to Potassium Ratio as Translatable Quantitative Biomarkers of Mineralocorticoid Receptor Antagonism
-
Eudy, R. J.; Sahasrabudhe, V.; Sweeney, K.; Tugnait, M.; King-Ahmad, A.; Near, K.; Loria, P.; Banker, M. E.; Piotrowski, D. W.; Boustany-Kari, C. M. The Use of Plasma Aldosterone and Urinary Sodium to Potassium Ratio as Translatable Quantitative Biomarkers of Mineralocorticoid Receptor Antagonism J. Transl. Med. 2011, 9, 180
-
(2011)
J. Transl. Med.
, vol.9
, pp. 180
-
-
Eudy, R.J.1
Sahasrabudhe, V.2
Sweeney, K.3
Tugnait, M.4
King-Ahmad, A.5
Near, K.6
Loria, P.7
Banker, M.E.8
Piotrowski, D.W.9
Boustany-Kari, C.M.10
-
59
-
-
82255191301
-
Synthesis and Cross Coupling of a Highly Substituted 2-Pyridylboronate: Application to the Large Scale Synthesis of a Mineralocorticoid Antagonist
-
Boos, C.; Bowles, D. M.; Cai, C.; Casimiro-Garcia, A.; Chen, X.; Hulford, C. A.; Jennings, S. M.; Kiser, E. J.; Piotrowski, D. W.; Sammons, M.; Wade, R. A. Synthesis and Cross Coupling of a Highly Substituted 2-Pyridylboronate: Application to the Large Scale Synthesis of a Mineralocorticoid Antagonist Tetrahedron Lett. 2011, 52, 7025-7029
-
(2011)
Tetrahedron Lett.
, vol.52
, pp. 7025-7029
-
-
Boos, C.1
Bowles, D.M.2
Cai, C.3
Casimiro-Garcia, A.4
Chen, X.5
Hulford, C.A.6
Jennings, S.M.7
Kiser, E.J.8
Piotrowski, D.W.9
Sammons, M.10
Wade, R.A.11
-
63
-
-
84872428849
-
-
Pipeline information obtained from the Mitsubishi Tanabe Web site
-
Pipeline information obtained from the Mitsubishi Tanabe Web site http://www.mt-pharma.co.jp/e/
-
-
-
-
64
-
-
79952786293
-
+ Excretion Activity
-
+ 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
Katayama, S.4
Hori, S.5
Matsui, K.6
-
65
-
-
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.; Katayama, S.; Hori, S.; Matsui, K. 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
Katayama, S.4
Hori, S.5
Matsui, K.6
-
66
-
-
84861098413
-
SM-368229, a Novel Promising Mineralocorticoid Receptor Antagonist, Shows Anti-Hypertensive Efficacy with Minimal Effect on Serum Potassium Level in Rats
-
Nariai, T.; Fujita, K.; Mori, M.; Katayama, S.; Hori, S.; Matsui, K. SM-368229, a Novel Promising Mineralocorticoid Receptor Antagonist, Shows Anti-Hypertensive 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
Katayama, S.4
Hori, S.5
Matsui, K.6
-
68
-
-
84866873353
-
-
PCT Int. Appl. WO2008126831
-
Aoki, K.; Tsuruoka, H.; Hayashi, N.; Yoshida, J.; Asoh, Y. Atropisomer of Pyrrole Derivative. PCT Int. Appl. WO2008126831, 2008.
-
(2008)
Atropisomer of Pyrrole Derivative
-
-
Aoki, K.1
Tsuruoka, H.2
Hayashi, N.3
Yoshida, J.4
Asoh, Y.5
-
69
-
-
84872430354
-
-
Pipeline information obtained from the Exelixis Web site
-
Pipeline information obtained from the Exelixis Web site http://www.exelixis.com
-
-
-
-
70
-
-
84055217558
-
Identification of Benzoxazin-3-one Derivatives as Novel, Potent, and Selective Nonsteroidal Mineralocorticoid Receptor Antagonists
-
Hasui, T.; Matsunaga, N.; Ora, T.; Ohyabu, N.; Nishigaki, N.; Imura, Y.; Igata, Y.; Matsui, H.; Motoyaji, T.; Tanaka, T.; Habuka, N.; Sogabe, S.; Ono, M.; Siedem, C. S.; Tang, T. P.; Gauthier, C.; De Meese, L. A.; Boyd, S. A.; Fukumoto, S. 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
Ohyabu, N.4
Nishigaki, N.5
Imura, Y.6
Igata, Y.7
Matsui, H.8
Motoyaji, T.9
Tanaka, T.10
Habuka, N.11
Sogabe, S.12
Ono, M.13
Siedem, C.S.14
Tang, T.P.15
Gauthier, C.16
De Meese, L.A.17
Boyd, S.A.18
Fukumoto, S.19
-
73
-
-
78649496901
-
Nitrile-Containing Pharmaceuticals: Efficacious Roles of the Nitrile Pharmacophore
-
Fleming, F. F.; Yao, L.; Ravikumar, P. C.; Funk, L.; Shook, B. C. Nitrile-Containing Pharmaceuticals: Efficacious Roles of the Nitrile Pharmacophore J. Med. Chem. 2010, 53, 7902-7917
-
(2010)
J. Med. Chem.
, vol.53
, pp. 7902-7917
-
-
Fleming, F.F.1
Yao, L.2
Ravikumar, P.C.3
Funk, L.4
Shook, B.C.5
-
74
-
-
22444438401
-
Crystal Structure of a Mutant Mineralocorticoid Receptor Responsible for Hypertension
-
Fagart, J.; Huyet, J.; Pinon, G. M.; Rochel, M.; Mayer, C.; Rafestin-Oblin, M. E. Crystal Structure of a Mutant Mineralocorticoid Receptor Responsible for Hypertension Nat. Struct. Mol. Biol. 2005, 12, 554-555. Also see references cited in ref 7c
-
(2005)
Nat. Struct. Mol. Biol.
, vol.12
, pp. 554-555
-
-
Fagart, J.1
Huyet, J.2
Pinon, G.M.3
Rochel, M.4
Mayer, C.5
Rafestin-Oblin, M.E.6
-
75
-
-
24744451821
-
A Ligand-Mediated Hydrogen Bond Network Required for the Activation of the Mineralocorticoid Receptor
-
Bledsoe, R. K.; Madauss, K. P.; Holt, J. A.; Apolito, C. J.; Lambert, M. H.; Pearce, K. H.; Stanley, T. B.; Stewart, E. L.; Trump, R. P.; Willson, T. M.; Williams, S. P. A Ligand-Mediated Hydrogen Bond Network Required for the Activation of the Mineralocorticoid Receptor J. Biol. Chem. 2005, 280, 31283-31293
-
(2005)
J. Biol. Chem.
, vol.280
, pp. 31283-31293
-
-
Bledsoe, R.K.1
Madauss, K.P.2
Holt, J.A.3
Apolito, C.J.4
Lambert, M.H.5
Pearce, K.H.6
Stanley, T.B.7
Stewart, E.L.8
Trump, R.P.9
Willson, T.M.10
Williams, S.P.11
-
76
-
-
84866873015
-
Nuclear Hormone Receptor Architecture-Form and Dynamics: The 2009 FASEB Summer Conference on Dynamic Structure of the Nuclear Hormone Receptors
-
McEwan, I. J.; Nardulli, A. M. Nuclear Hormone Receptor Architecture-Form and Dynamics: The 2009 FASEB Summer Conference on Dynamic Structure of the Nuclear Hormone Receptors Nucl. Recept. Signaling Atlas 2007, 5, e012
-
(2007)
Nucl. Recept. Signaling Atlas
, vol.5
, pp. 012
-
-
McEwan, I.J.1
Nardulli, A.M.2
-
77
-
-
56749130032
-
Structure of the Intact PPAR-γ-RXR-Nuclear Receptor Complex on DNA
-
Chandra, V.; Huang, P.; Hamuro, Y.; Raghuram, S.; Wang, Y.; Burris, T. P.; Rastinejad, F. Structure of the Intact PPAR-γ-RXR-Nuclear Receptor Complex on DNA Nature 2008, 456, 350-356
-
(2008)
Nature
, vol.456
, pp. 350-356
-
-
Chandra, V.1
Huang, P.2
Hamuro, Y.3
Raghuram, S.4
Wang, Y.5
Burris, T.P.6
Rastinejad, F.7
-
78
-
-
69449087342
-
Structural and Functional Characterization of the Interdomain Interaction in the Mineralocorticoid Receptor
-
Pippal, J. B.; Yao, Y.; Rogerson, F. M.; Fuller, P. Structural and Functional Characterization of the Interdomain Interaction in the Mineralocorticoid Receptor J. Mol. Endocrinol. 2009, 23, 1360-1370
-
(2009)
J. Mol. Endocrinol.
, vol.23
, pp. 1360-1370
-
-
Pippal, J.B.1
Yao, Y.2
Rogerson, F.M.3
Fuller, P.4
-
79
-
-
77049123191
-
Expression, Purification and Primary Crystallographic Study of Human Androgen Receptor in Complex with DNA and Coactivator Motifs
-
Zhou, X. E.; Suino-Powell, K.; Ludidi, P. L.; McDonnell, D. P.; Xu, H. E. Expression, Purification and Primary Crystallographic Study of Human Androgen Receptor in Complex with DNA and Coactivator Motifs Protein Expression Purif. 2010, 71, 21-27
-
(2010)
Protein Expression Purif.
, vol.71
, pp. 21-27
-
-
Zhou, X.E.1
Suino-Powell, K.2
Ludidi, P.L.3
McDonnell, D.P.4
Xu, H.E.5
-
80
-
-
23344449647
-
Molecular and Pharmacological Properties of a Potent and Selective Novel Nonsteroidal Progesterone Receptor Agonist Tanaproget
-
Zhang, Z.; Olland, A. M.; Zhu, Y.; Cohen, J.; Berrodin, T.; Chippari, S.; Appavu, C.; Li, S.; Wilhem, J.; Chopra, R.; Fensome, A.; Zhang, P.; Wrobel, J.; Unwalla, R. J.; Lyttle, C. R.; Winneker, R. C. Molecular and Pharmacological Properties of a Potent and Selective Novel Nonsteroidal Progesterone Receptor Agonist Tanaproget J. Biol. Chem. 2005, 280, 28468-28475
-
(2005)
J. Biol. Chem.
, vol.280
, pp. 28468-28475
-
-
Zhang, Z.1
Olland, A.M.2
Zhu, Y.3
Cohen, J.4
Berrodin, T.5
Chippari, S.6
Appavu, C.7
Li, S.8
Wilhem, J.9
Chopra, R.10
Fensome, A.11
Zhang, P.12
Wrobel, J.13
Unwalla, R.J.14
Lyttle, C.R.15
Winneker, R.C.16
-
81
-
-
69849091806
-
The Mineralocorticoid Receptor and Its Coregulators
-
Yang, J.; Young, M. J. The Mineralocorticoid Receptor and Its Coregulators J. Mol. Endocrinol. 2009, 43, 53-64
-
(2009)
J. Mol. Endocrinol.
, vol.43
, pp. 53-64
-
-
Yang, J.1
Young, M.J.2
-
82
-
-
77950442251
-
Minireview: Not Picking Pockets: Nuclear Receptor Alternate-Site Modulators (NRAMs)
-
Moore, T. W.; Mayne, C. G.; Katzenellenbogen, J. A. Minireview: Not Picking Pockets: Nuclear Receptor Alternate-Site Modulators (NRAMs) Mol. Endocrinol. 2010, 24, 683-695
-
(2010)
Mol. Endocrinol.
, vol.24
, pp. 683-695
-
-
Moore, T.W.1
Mayne, C.G.2
Katzenellenbogen, J.A.3
|