Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship
- Autores
- Galigniana, Mario Daniel; Piwien Pilipuk, Graciela
- Año de publicación
- 2004
- Idioma
- inglés
- Tipo de recurso
- artículo
- Estado
- versión publicada
- Descripción
- 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.
Fil: Galigniana, Mario Daniel. University of Michigan; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Piwien Pilipuk, Graciela. University of Michigan; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina - Materia
-
Aldosterone
Natriuresis
Mineralcorticoids
Molecular Conformation - Nivel de accesibilidad
- acceso abierto
- Condiciones de uso
- https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
- Repositorio
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/29122
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Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationshipGaligniana, Mario DanielPiwien Pilipuk, GracielaAldosteroneNatriuresisMineralcorticoidsMolecular Conformationhttps://purl.org/becyt/ford/3.1https://purl.org/becyt/ford/3The 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.Fil: Galigniana, Mario Daniel. University of Michigan; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Piwien Pilipuk, Graciela. University of Michigan; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaElsevier Inc2004info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/29122Galigniana, 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; 31-680083-67290083-6729CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0083672904690029?via%3Dihubinfo:eu-repo/semantics/altIdentifier/doi/10.1016/S0083-6729(04)69002-9info:eu-repo/semantics/altIdentifier/pmid/15196878info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:33:01Zoai:ri.conicet.gov.ar:11336/29122instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 10:33:01.333CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse |
dc.title.none.fl_str_mv |
Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship |
title |
Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship |
spellingShingle |
Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship Galigniana, Mario Daniel Aldosterone Natriuresis Mineralcorticoids Molecular Conformation |
title_short |
Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship |
title_full |
Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship |
title_fullStr |
Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship |
title_full_unstemmed |
Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship |
title_sort |
Activation of the ligand-mineralocorticoid receptor functional unit by ancient, classical, and novel ligands: structure-activity relationship |
dc.creator.none.fl_str_mv |
Galigniana, Mario Daniel Piwien Pilipuk, Graciela |
author |
Galigniana, Mario Daniel |
author_facet |
Galigniana, Mario Daniel Piwien Pilipuk, Graciela |
author_role |
author |
author2 |
Piwien Pilipuk, Graciela |
author2_role |
author |
dc.subject.none.fl_str_mv |
Aldosterone Natriuresis Mineralcorticoids Molecular Conformation |
topic |
Aldosterone Natriuresis Mineralcorticoids Molecular Conformation |
purl_subject.fl_str_mv |
https://purl.org/becyt/ford/3.1 https://purl.org/becyt/ford/3 |
dc.description.none.fl_txt_mv |
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. Fil: Galigniana, Mario Daniel. University of Michigan; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Piwien Pilipuk, Graciela. University of Michigan; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina |
description |
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. |
publishDate |
2004 |
dc.date.none.fl_str_mv |
2004 |
dc.type.none.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion http://purl.org/coar/resource_type/c_6501 info:ar-repo/semantics/articulo |
format |
article |
status_str |
publishedVersion |
dc.identifier.none.fl_str_mv |
http://hdl.handle.net/11336/29122 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 0083-6729 0083-6729 CONICET Digital CONICET |
url |
http://hdl.handle.net/11336/29122 |
identifier_str_mv |
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 0083-6729 CONICET Digital CONICET |
dc.language.none.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0083672904690029?via%3Dihub info:eu-repo/semantics/altIdentifier/doi/10.1016/S0083-6729(04)69002-9 info:eu-repo/semantics/altIdentifier/pmid/15196878 |
dc.rights.none.fl_str_mv |
info:eu-repo/semantics/openAccess https://creativecommons.org/licenses/by-nc-nd/2.5/ar/ |
eu_rights_str_mv |
openAccess |
rights_invalid_str_mv |
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/ |
dc.format.none.fl_str_mv |
application/pdf application/pdf |
dc.publisher.none.fl_str_mv |
Elsevier Inc |
publisher.none.fl_str_mv |
Elsevier Inc |
dc.source.none.fl_str_mv |
reponame:CONICET Digital (CONICET) instname:Consejo Nacional de Investigaciones Científicas y Técnicas |
reponame_str |
CONICET Digital (CONICET) |
collection |
CONICET Digital (CONICET) |
instname_str |
Consejo Nacional de Investigaciones Científicas y Técnicas |
repository.name.fl_str_mv |
CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas |
repository.mail.fl_str_mv |
dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar |
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13.070432 |