Finerenone impedes aldosterone-dependent nuclear import of the mineralocorticoid receptor and prevents genomic recruitment of steroid receptor coactivator-1 - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Journal of Biological Chemistry Année : 2015

Finerenone impedes aldosterone-dependent nuclear import of the mineralocorticoid receptor and prevents genomic recruitment of steroid receptor coactivator-1

Peter Kolkhof
  • Fonction : Auteur
Michel R. Fay
  • Fonction : Auteur
Junaid A. Khan
  • Fonction : Auteur
Alexander Hillisch
  • Fonction : Auteur
Marie Edith Rafestin-Oblin
  • Fonction : Auteur

Résumé

© 2015 by The American Society for Biochemistry and Molecular Biology, Inc. Background: Finerenone is a novel nonsteroidal mineralocorticoid antagonist, currently in clinical phase IIb trials. Results: Finerenone delays mineralocorticoid receptor nuclear import and inhibits its binding and transcriptional coactivator recruitment onto target gene promoters. Conclusion: Finerenone impedes three critical steps of the mineralocorticoid receptor signaling pathway. Significance: Finerenone, which behaves differently from currently available mineralocorticoid antagonists, is potentially a promising molecule to treat cardiorenal diseases.
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Dates et versions

hal-03464100 , version 1 (03-12-2021)

Identifiants

Citer

L. Amazit, Florian Le Billan, Peter Kolkhof, Khadija Lamribet, Say Viengchareun, et al.. Finerenone impedes aldosterone-dependent nuclear import of the mineralocorticoid receptor and prevents genomic recruitment of steroid receptor coactivator-1. Journal of Biological Chemistry, 2015, ⟨10.1074/jbc.M115.657957⟩. ⟨hal-03464100⟩
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