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Antagonism in the humanmineralocorticoid receptor [PDF]
EMBO Journal, 1998 Key residues of the human mineralocorticoid receptor (hMR) involved in the recognition of agonist and antagonist ligands were identified by alanine-scanning mutagenesis based on a homology model of the hMR ligand-binding domain. They were tested for their transactivation capacity and ability to bind agonists (aldosterone, cortisol) and antagonists ...
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Rapid mineralocorticoid receptor trafficking
Steroids, 2014The mineralocorticoid receptor (MR) is a ligand-dependent transcription factor that physiologically regulates water-electrolyte homeostasis and controls blood pressure. The MR can also elicit inflammatory and remodeling processes in the cardiovascular system and the kidneys, which require the presence of additional pathological factors like for example
M, Gekle +4 more
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Mineralocorticoid receptors in the metabolic syndrome
Trends in Endocrinology & Metabolism, 2009The mineralocorticoid receptor (MR) mediates aldosterone effects on salt homeostasis and blood pressure regulation. MR activation also promotes inflammation, cardiovascular remodelling and endothelial dysfunction, and affects adipose tissue differentiation and function. Some of these effects derive from MR activation by glucocorticoids.
Maria-Christina, Zennaro +2 more
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The Mineralocorticoid Receptor and Oxidative Stress
Heart Failure Reviews, 2005Reactive oxygen species are profoundly important for many physiologic functions and are also pivotal to numerous disease processes, particularly those involving inflammation. Much evidence has accrued demonstrating that aldosterone acts locally in many cells aside from those in the cortical collecting duct.
Anette, Fiebeler, Friedrich C, Luft
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Interdomain interactions in the mineralocorticoid receptor
Molecular and Cellular Endocrinology, 2003The potential for interaction between the N-terminal domain and the C-terminal region (hinge and ligand-binding domain) of the mineralocorticoid receptor (MR) was examined using the mammalian-2-hybrid assay. The MR C-terminal region was fused to the GAL4 DNA-binding domain (GAL4-MRC).
Fraser M, Rogerson, Peter J, Fuller
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Pseudohypoaldosteronism and mineralocorticoid receptor abnormalities
The Journal of Steroid Biochemistry and Molecular Biology, 1991Pseudohypoaldosteronism is a rare inherited disease characterized by renal salt loss, hyperkalemia and metabolic acidosis despite highly elevated aldosterone values. We previously reported absent or reduced numbers of mineralocorticoid receptors in mononuclear leukocytes and defective effector mechanism as shown by no response in vitro to the ...
ARMANINI, DECIO +8 more
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The mineralocorticoid receptor in skin disease
British Journal of Pharmacology, 2021The mineralocorticoid receptor (MR or NR3C2) is expressed in all types of cells from the different skin compartments. The binding and activation by glucocorticoids has a higher affinity than that on the closely related glucocorticoid receptor (GR or NR3C1).
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Mineralocorticoid Receptors in Human Kidney
The Journal of Clinical Endocrinology & Metabolism, 1976Cytosol binding of [3H]aldosterone was measured after incubation of the hormone at 37 C with slices of human kidney obtained after surgical removal. High affinity [3H]aldosterone binding with an apparent equilibrium dissociation constant (Kd) of approximately 0.5 nM was observed to probably "mineralo-corticoid receptors." [3H]aldosterone binding of ...
D T, Matulich +3 more
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Nihon rinsho. Japanese journal of clinical medicine, 2009
Recent clinical trials have indicated the utility of mineralocorticoid receptor (MR) antagonists in patients with cardiovascular and renal diseases. Experiments studies have shown that chronic treatment with aldosterone resulted in severe cardiac and renal injuries, which were ameliorated by MR antagonists.
Akira, Nishiyama +2 more
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Recent clinical trials have indicated the utility of mineralocorticoid receptor (MR) antagonists in patients with cardiovascular and renal diseases. Experiments studies have shown that chronic treatment with aldosterone resulted in severe cardiac and renal injuries, which were ameliorated by MR antagonists.
Akira, Nishiyama +2 more
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Novel interactions of the mineralocorticoid receptor
Molecular and Cellular Endocrinology, 2015The mineralocorticoid receptor (MR) differs from the other steroid receptors in that it responds to two physiological ligands, aldosterone and cortisol. In epithelial tissues, aldosterone selectivity is determined by 11β-hydroxysteroid dehydrogenase type II.
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