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dc.contributor.author
Galigniana, Mario Daniel
dc.contributor.author
Piwien Pilipuk, Graciela
dc.date.available
2017-11-26T16:17:28Z
dc.date.issued
2004
dc.identifier.citation
Galigniana, Mario Daniel; Piwien Pilipuk, Graciela; Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship; Elsevier Inc; Vitamins And Hormones Series; 69; -1-2004; 31-68
dc.identifier.issn
0083-6729
dc.identifier.uri
http://hdl.handle.net/11336/29122
dc.description.abstract
The mineralocorticoid effect on epithelial cells is the resultant of an intricate net of biochemical regulations that ultimately leads to the maintenance of electrolyte homeostasis. Two key protagonists in this plot are the ligand, which broadcasts the information, and the receptor, which functions as a receiver and transducer. Therefore, the responsibility for the final biological effect is not limited to each individual component but to both of them, so they constitute a functional unit. In addition, several prereceptor regulatory mechanisms are also determinant factors for the final biological response. Because steroids are present in both animals and plants and are derived from common precursors, it is intriguing how these simple molecules have acquired specialization to shape biological development and differentiation. This is particularly true for the function of aldosterone in mammals, which is mimicked by glucocorticoids or progesterone in some particular cases. Inasmuch as the most potent mineralocorticoid in nature, aldosterone, shows a poorly angled steroid nucleus at the A?B-ring junction, and because steroids that possess identical functional groups and different steroidal frames elicit different mineralocorticoid effects, we postulate that a planar conformation of the ligand is a key requirement to acquire potent sodium retention properties. The model takes into consideration all the mechanisms involved in the regulation of the final biological effect, although it does not provide a definitive answer to the original question. It is also discussed how the use of novel mineralocorticoid ligands may shed light on the still obscure mechanism of action of the mineralocorticoid receptor.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier Inc
dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.subject
Aldosterone
dc.subject
Natriuresis
dc.subject
Mineralcorticoids
dc.subject
Molecular Conformation
dc.subject.classification
Bioquímica y Biología Molecular
dc.subject.classification
Medicina Básica
dc.subject.classification
CIENCIAS MÉDICAS Y DE LA SALUD
dc.title
Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2017-11-16T15:13:32Z
dc.identifier.eissn
0083-6729
dc.journal.volume
69
dc.journal.pagination
31-68
dc.journal.pais
Países Bajos
dc.journal.ciudad
Amsterdam
dc.description.fil
Fil: Galigniana, Mario Daniel. University of Michigan; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Piwien Pilipuk, Graciela. University of Michigan; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.journal.title
Vitamins And Hormones Series
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0083672904690029?via%3Dihub
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/S0083-6729(04)69002-9
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/pmid/15196878


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