Epidermal growth factor receptor/extracellular signal-regulated kinase pathway enhances mineralocorticoid receptor transcriptional activity through protein stabilization

Mol Cell Endocrinol. 2018 Sep 15:473:89-99. doi: 10.1016/j.mce.2018.01.007. Epub 2018 Jan 31.

Abstract

Activation of mineralocorticoid receptor (MR) is evoked by aldosterone, and it induces hypertension and cardiovascular disease when it's concomitant with excessive salt loading. We have proposed the notion of "MR-associated hypertension", in which add-on therapy of MR blockers is effective even though serum aldosterone level is within normal range. To elucidate its underlying molecular mechanism, we focused on the effect of epidermal growth factor receptor (EGFR)/extracellular signal-regulated kinase (ERK) activation on MR activity. Epidermal growth factor (EGF) administration increased MR transcriptional activity through EGFR/ERK pathway and increased protein level by counteracting MR ubiquitylation in vitro. EGF administration in vivo also increased MR protein level and target gene expression in kidney, which were decreased by EGFR inhibitor. In addition, the administration of EGFR inhibitor lowered systolic blood pressure and MR activity in DOCA/salt-treated mice. In conclusion, EGFR/ERK pathway activation is considered as one of the underlying mechanisms of aberrant MR activation and EGFR/ERK pathway blockade could be an alternative approach for the prevention of MR-related cardiovascular events.

Keywords: Epidermal growth factor receptor; Extracellular signal-regulated kinase pathway; Mineralocorticoid receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldosterone / pharmacology
  • Animals
  • Blood Pressure / drug effects
  • COS Cells
  • Chlorocebus aethiops
  • Epidermal Growth Factor / administration & dosage
  • Epidermal Growth Factor / pharmacology
  • ErbB Receptors / antagonists & inhibitors
  • ErbB Receptors / metabolism*
  • Gene Expression Regulation / drug effects
  • Gene Knockdown Techniques
  • HEK293 Cells
  • Humans
  • MAP Kinase Signaling System* / drug effects
  • Male
  • Mice, Inbred C57BL
  • Protein Stability
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • RNA, Small Interfering / metabolism
  • Receptors, Mineralocorticoid / genetics*
  • Receptors, Mineralocorticoid / metabolism
  • Systole / drug effects
  • Transcription, Genetic* / drug effects
  • Ubiquitination / drug effects

Substances

  • RNA, Messenger
  • RNA, Small Interfering
  • Receptors, Mineralocorticoid
  • Aldosterone
  • Epidermal Growth Factor
  • ErbB Receptors