Approaches towards tissue‐selective pharmacology of the mineralocorticoid receptor
- Author
- Dorien Clarisse (UGent) , Lisa Deng, Karolien De Bosscher (UGent) and Achim Lother
- Organization
- Project
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- Combining lower doses of glucocorticoids with mineralocorticoid receptor antagonists as a novel drug repurposing strategy in multiple myeloma
- Study of novel bivalent ligands targeting glucocorticoid and mineralocorticoid receptor heterodimers: towards an improved glucocorticoid-based multiple myeloma therapy"
- Abstract
- Mineralocorticoid receptor antagonists (MRAs) are highly effective therapies for cardiovascular and renal disease. However, the widespread clinical use of currently available MRAs in cardiorenal medicine is hampered by an increased risk of hyperkalaemia. The mineralocorticoid receptor (MR) is a nuclear receptor responsible for fluid and electrolyte homeostasis in epithelial tissues, whereas pathophysiological MR activation in nonepithelial tissues leads to undesirable pro-inflammatory and profibrotic effects. Therefore, new strategies that selectively target the deleterious effects of the MR but spare its physiological function are needed. In this review, we discuss recent pharmacological developments starting from novel non-steroidal MRAs, such as finerenone or esaxerenone, that are now entering clinical use, to concepts arising from the current knowledge of the MR signalling pathway, aiming at receptor-coregulator interaction, epigenetics or downstream effectors of the MR.
- Keywords
- Pharmacology, drug discovery, heart failure, hyperkalemia, kidney disease, mineralocorticoid receptor, GELATINASE-ASSOCIATED LIPOCALIN, ALDOSTERONE-REGULATED GENES, GLUCOCORTICOID-RECEPTOR, HEART-FAILURE, CONCISE GUIDE, MEDIATED TRANSACTIVATION, CORTICOSTEROID RECEPTORS, CARDIAC INFLAMMATION, BINDING DOMAIN, KIDNEY-DISEASE
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Citation
Please use this url to cite or link to this publication: http://hdl.handle.net/1854/LU-8730035
- MLA
- Clarisse, Dorien, et al. “Approaches towards Tissue‐selective Pharmacology of the Mineralocorticoid Receptor.” BRITISH JOURNAL OF PHARMACOLOGY, vol. 179, no. 13, 2022, pp. 3235–49, doi:10.1111/bph.15719.
- APA
- Clarisse, D., Deng, L., De Bosscher, K., & Lother, A. (2022). Approaches towards tissue‐selective pharmacology of the mineralocorticoid receptor. BRITISH JOURNAL OF PHARMACOLOGY, 179(13), 3235–3249. https://doi.org/10.1111/bph.15719
- Chicago author-date
- Clarisse, Dorien, Lisa Deng, Karolien De Bosscher, and Achim Lother. 2022. “Approaches towards Tissue‐selective Pharmacology of the Mineralocorticoid Receptor.” BRITISH JOURNAL OF PHARMACOLOGY 179 (13): 3235–49. https://doi.org/10.1111/bph.15719.
- Chicago author-date (all authors)
- Clarisse, Dorien, Lisa Deng, Karolien De Bosscher, and Achim Lother. 2022. “Approaches towards Tissue‐selective Pharmacology of the Mineralocorticoid Receptor.” BRITISH JOURNAL OF PHARMACOLOGY 179 (13): 3235–3249. doi:10.1111/bph.15719.
- Vancouver
- 1.Clarisse D, Deng L, De Bosscher K, Lother A. Approaches towards tissue‐selective pharmacology of the mineralocorticoid receptor. BRITISH JOURNAL OF PHARMACOLOGY. 2022;179(13):3235–49.
- IEEE
- [1]D. Clarisse, L. Deng, K. De Bosscher, and A. Lother, “Approaches towards tissue‐selective pharmacology of the mineralocorticoid receptor,” BRITISH JOURNAL OF PHARMACOLOGY, vol. 179, no. 13, pp. 3235–3249, 2022.
@article{8730035,
abstract = {{Mineralocorticoid receptor antagonists (MRAs) are highly effective therapies for cardiovascular and renal disease. However, the widespread clinical use of currently available MRAs in cardiorenal medicine is hampered by an increased risk of hyperkalaemia. The mineralocorticoid receptor (MR) is a nuclear receptor responsible for fluid and electrolyte homeostasis in epithelial tissues, whereas pathophysiological MR activation in nonepithelial tissues leads to undesirable pro-inflammatory and profibrotic effects. Therefore, new strategies that selectively target the deleterious effects of the MR but spare its physiological function are needed. In this review, we discuss recent pharmacological developments starting from novel non-steroidal MRAs, such as finerenone or esaxerenone, that are now entering clinical use, to concepts arising from the current knowledge of the MR signalling pathway, aiming at receptor-coregulator interaction, epigenetics or downstream effectors of the MR.}},
author = {{Clarisse, Dorien and Deng, Lisa and De Bosscher, Karolien and Lother, Achim}},
issn = {{0007-1188}},
journal = {{BRITISH JOURNAL OF PHARMACOLOGY}},
keywords = {{Pharmacology,drug discovery,heart failure,hyperkalemia,kidney disease,mineralocorticoid receptor,GELATINASE-ASSOCIATED LIPOCALIN,ALDOSTERONE-REGULATED GENES,GLUCOCORTICOID-RECEPTOR,HEART-FAILURE,CONCISE GUIDE,MEDIATED TRANSACTIVATION,CORTICOSTEROID RECEPTORS,CARDIAC INFLAMMATION,BINDING DOMAIN,KIDNEY-DISEASE}},
language = {{eng}},
number = {{13}},
pages = {{3235--3249}},
title = {{Approaches towards tissue‐selective pharmacology of the mineralocorticoid receptor}},
url = {{http://doi.org/10.1111/bph.15719}},
volume = {{179}},
year = {{2022}},
}
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