Defining an inhibitory domain in the gamma subunit of the epithelial sodium channel

Am J Physiol Renal Physiol. 2010 Oct;299(4):F854-61. doi: 10.1152/ajprenal.00316.2010. Epub 2010 Jul 14.

Abstract

Proteases activate the epithelial sodium channel (ENaC) by cleaving the large extracellular domains of the α- and γ-subunits and releasing peptides with inhibitory properties. Furin and prostasin activate mouse ENaC by cleaving the γ-subunit at sites flanking a 43 residue inhibitory tract (γE144-K186). To determine whether there is a minimal inhibitory region within this 43 residue tract, we generated serial deletions in the inhibitory tract of the γ-subunit in channels resistant to cleavage by furin and prostasin. We found that partial or complete deletion of a short segment in the γ-subunit, R158-N171, enhanced channel activity. Synthetic peptides overlapping this segment in the γ-subunit further identified a key 11-mer tract, R158-F168 (RFLNLIPLLVF), which inhibited wild-type ENaC expressed in Xenopus laevis oocytes, and endogenous channels in mpkCCD cells and human airway epithelia. Further studies with amino acid-substituted peptides defined residues that are required for inhibition in this key 11-mer tract. The presence of the native γ inhibitory tract in ENaC weakened the intrinsic binding constant of the 11-mer peptide inhibitor, suggesting that the γ inhibitory tract and the 11-mer peptide interact at overlapping sites within the channel.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Cells, Cultured
  • Epithelial Sodium Channels / analysis*
  • Epithelial Sodium Channels / drug effects
  • Epithelial Sodium Channels / metabolism
  • Female
  • Furin / pharmacology
  • Humans
  • Kidney Tubules, Collecting / cytology
  • Kidney Tubules, Collecting / metabolism
  • Mice
  • Oocytes / cytology
  • Oocytes / metabolism
  • Protein Structure, Tertiary*
  • Respiratory Mucosa / cytology
  • Respiratory Mucosa / metabolism
  • Serine Endopeptidases / pharmacology
  • Xenopus laevis

Substances

  • Epithelial Sodium Channels
  • Serine Endopeptidases
  • prostasin
  • Furin