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Clinical Pharmacokinetics and Pharmacodynamics of Esaxerenone, a Novel Mineralocorticoid Receptor Antagonist: A Review
Esaxerenone is a selective, nonsteroidal, high-affinity mineralocorticoid receptor antagonist recently approved in Japan for the treatment of...
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Pharmacokinetics of the Novel Nonsteroidal Mineralocorticoid Receptor Antagonist Ocedurenone (KBP-5074) in Individuals with Moderate Hepatic Impairment
Background and ObjectivesOcedurenone (KBP-5074) is a novel nonsteroidal mineralocorticoid receptor antagonist that has demonstrated safety and...
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Effects of Glucocorticoid Hormones on Pain Sensitivity: Involvement of Glucocorticoid and Mineralocorticoid Receptors
Glucocorticoid hormones are widely used in the clinic as analgesic and anti-inflammatory drugs for various types of pain. The actions of...
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Mineralocorticoid receptor-antagonism prevents COVID-19-dependent glycocalyx damage
Proinflammatory cytokines target vascular endothelial cells during COVID-19 infections. In particular, the endothelial glycocalyx (eGC), a...
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Apparent mineralocorticoid excess: comprehensive overview of molecular genetics
Apparent mineralocorticoid excess is an autosomal recessive form of monogenic disease characterized by juvenile resistant low-renin hypertension,...
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Molecular Pharmacology of the Youngest Member of the Nuclear Receptor Family: The Mineralocorticoid Receptor
The mineralocorticoid receptor (MR) was the last member of the nuclear receptor superfamily to evolve. It is responsible for the maintenance of the...
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Role of glucocorticoid receptor mutations in hypertension and adrenal gland hyperplasia
Hypertension is one of the leading causes of premature death in humans and exhibits a complex aetiology including environmental and genetic factors....
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Selective deletion of endothelial mineralocorticoid receptor protects from vascular dysfunction in sodium-restricted female mice
BackgroundRecent evidence by our laboratory demonstrates that women and female mice endogenously express higher endothelial mineralocorticoid...
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Histamine H2-receptor antagonism improves conduit artery endothelial function and reduces plasma aldosterone level without lowering arterial blood pressure in angiotensin II–hypertensive mice
Aldosterone through the mineralocorticoid receptor MR has detrimental effects on cardiovascular disease. It reduces the bioavailability of nitric...
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Cardiovascular risks of androgen receptor targeted agents in prostate cancer: a systematic review and meta-analysis
IntroductionAndrogen receptor targeted agents (ARTA) have increasingly been incorporated into treatment regimens for various stages of prostate...
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Repurposing of IL 33/ST2 Modulating Drugs as a Cardioprotective Agent: A Promising Approach
Drug repurposing has emerged as an enigmatic clinical approach in disorders affecting the cardiovascular system. The concept of drug repurposing has...
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Neurosteroid Receptor Modulators for Treating Traumatic Brain Injury
Traumatic brain injury (TBI) triggers wide-ranging pathology that impacts multiple biochemical and physiological systems, both inside and outside the...
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A tumour suppressive relationship between mineralocorticoid and retinoic acid receptors activates a transcriptional program consistent with a reverse Warburg effect in breast cancer
BackgroundThe role of nuclear receptors in both the aetiology and treatment of breast cancer is exemplified by the use of the oestrogen receptor (ER)...
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Protein Condensation in the Nuclear Receptor Family; Implications for Transcriptional Output
The nuclear receptorNuclear receptors superfamily is a group of transcriptional regulators that orchestrate multiple vital processes such as...
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Glucocorticoid Receptor Down-Regulation Affects Neural Stem Cell Proliferation and Hippocampal Neurogenesis
Dysregulation of the hypothalamic–pituitary–adrenal axis and abnormalities in the glucocorticoid receptor (GR) have been linked to major depressive...
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Stress-induced Neuroinflammation of the Spinal Cord is Restrained by Cort113176 (Dazucorilant), A Specific Glucocorticoid Receptor Modulator
Glucocorticoids exert antiinflammatory, antiproliferative and immunosupressive effects. Paradoxically they may also enhance inflammation particularly...
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A Genomic Study of the Japanese Population Focusing on the Glucocorticoid Receptor Interactome Highlights Distinct Genetic Characteristics Associated with Stress Response
All living organisms have been programmed to maintain a complex inner equilibrium called homeostasis, despite numerous adversities during their...
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A potent new-scaffold androgen receptor antagonist discovered on the basis of a MIEC-SVM model
Prostate cancer (PCa) is the second most prevalent malignancy among men worldwide. The aberrant activation of androgen receptor (AR) signaling has...
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Corticosteroid Receptors in Cardiac Health and Disease
Nuclear receptors play a central role in both energy metabolism and cardiomyocyte death and survival in the heart. Recent evidence suggests they may...
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Sacubitril/valsartan compared to equivalent/sub-equivalent dose angiotensin receptor blocker or angiotensin-converting enzyme inhibitor in heart failure with reduced ejection fraction: a meta-analysis of randomized trials
PurposeThe objective of this meta-analysis is to determine how sacubitril/valsartan (SV) compares to equivalent and sub-equivalent angiotensin...
