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

  • Larbi Amazit
  • , Florian Le Billan
  • , Peter Kolkhof
  • , Khadija Lamribet
  • , Say Viengchareun
  • , Michel R. Fay
  • , Junaid A. Khan
  • , Alexander Hillisch
  • , Marc Lombès
  • , Marie Edith Rafestin-Oblin
  • , Jérôme Fagart

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)21876-21889
Number of pages14
JournalJournal of Biological Chemistry
Volume290
Issue number36
DOIs
Publication statusPublished - 4 Sept 2015
Externally publishedYes

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