Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
J Biol Chem
2018 Oct 19;29342:16217-16225. doi: 10.1074/jbc.RA118.004362.
Show Gene links
Show Anatomy links
The epithelial Na+ channel γ subunit autoinhibitory tract suppresses channel activity by binding the γ subunit's finger-thumb domain interface.
Balchak DM
,
Thompson RN
,
Kashlan OB
.
???displayArticle.abstract???
Epithelial Na+ channel (ENaC) maturation and activation require proteolysis of both the α and γ subunits. Cleavage at multiple sites in the finger domain of each subunit liberates their autoinhibitory tracts. Synthetic peptides derived from the proteolytically released fragments inhibit the channel, likely by reconstituting key interactions removed by the proteolysis. We previously showed that a peptide derived from the α subunit's autoinhibitory sequence (α-8) binds at the α subunit's finger-thumb domain interface. Despite low sequence similarity between the α and γ subunit finger domains, we hypothesized that a peptide derived from the γ subunit's autoinhibitory sequence (γ-11) inhibits the channel through an analogous mechanism. Using Xenopus oocytes, we found here that channels lacking a γ subunit thumb domain were no longer sensitive to γ-11, but remained sensitive to α-8. We identified finger domain sites in the γ subunit that dramatically reduced γ-11 inhibition. Using cysteines and sulfhydryl reactive cross-linkers introduced into both the peptide and the subunit, we also could cross-link γ-11 to both the finger domain and the thumb domain of the γ subunit. Our results suggest that α-8 and γ-11 occupy similar binding pockets within their respective subunits, and that proteolysis of the α and γ subunits activate the channel through analogous mechanisms.
Adebamiro,
A segment of gamma ENaC mediates elastase activation of Na+ transport.
2007, Pubmed
Adebamiro,
A segment of gamma ENaC mediates elastase activation of Na+ transport.
2007,
Pubmed
Ahn,
Cloning and functional expression of the mouse epithelial sodium channel.
1999,
Pubmed
,
Xenbase
Baconguis,
Structural plasticity and dynamic selectivity of acid-sensing ion channel-spider toxin complexes.
2012,
Pubmed
Baconguis,
X-ray structure of acid-sensing ion channel 1-snake toxin complex reveals open state of a Na(+)-selective channel.
2014,
Pubmed
Bize,
Sodium self-inhibition of human epithelial sodium channel: selectivity and affinity of the extracellular sodium sensing site.
2007,
Pubmed
,
Xenbase
Blobner,
Conserved cysteines in the finger domain of the epithelial Na+ channel α and γ subunits are proximal to the dynamic finger-thumb domain interface.
2018,
Pubmed
,
Xenbase
Bruns,
Epithelial Na+ channels are fully activated by furin- and prostasin-dependent release of an inhibitory peptide from the gamma-subunit.
2007,
Pubmed
,
Xenbase
Butterworth,
Activation of the epithelial sodium channel (ENaC) by the alkaline protease from Pseudomonas aeruginosa.
2012,
Pubmed
Carattino,
Proteolytic processing of the epithelial sodium channel gamma subunit has a dominant role in channel activation.
2008,
Pubmed
,
Xenbase
Carattino,
The epithelial Na+ channel is inhibited by a peptide derived from proteolytic processing of its alpha subunit.
2006,
Pubmed
,
Xenbase
Collier,
Intersubunit conformational changes mediate epithelial sodium channel gating.
2014,
Pubmed
,
Xenbase
Collier,
Identification of extracellular domain residues required for epithelial Na+ channel activation by acidic pH.
2012,
Pubmed
,
Xenbase
Collier,
Identification of epithelial Na+ channel (ENaC) intersubunit Cl- inhibitory residues suggests a trimeric alpha gamma beta channel architecture.
2011,
Pubmed
,
Xenbase
Donaldson,
Regulation of the epithelial sodium channel by serine proteases in human airways.
2002,
Pubmed
,
Xenbase
Frindt,
Regulation of ENaC trafficking in rat kidney.
2016,
Pubmed
Hughey,
Epithelial sodium channels are activated by furin-dependent proteolysis.
2004,
Pubmed
,
Xenbase
Jasti,
Structure of acid-sensing ion channel 1 at 1.9 A resolution and low pH.
2007,
Pubmed
Jiang,
Altered fluid transport across airway epithelium in cystic fibrosis.
1993,
Pubmed
Kashlan,
ENaC structure and function in the wake of a resolved structure of a family member.
2011,
Pubmed
Kashlan,
Inhibitory tract traps the epithelial Na+ channel in a low activity conformation.
2012,
Pubmed
Kashlan,
Constraint-based, homology model of the extracellular domain of the epithelial Na+ channel α subunit reveals a mechanism of channel activation by proteases.
2011,
Pubmed
Kashlan,
Na+ inhibits the epithelial Na+ channel by binding to a site in an extracellular acidic cleft.
2015,
Pubmed
,
Xenbase
Kashlan,
Allosteric inhibition of the epithelial Na+ channel through peptide binding at peripheral finger and thumb domains.
2010,
Pubmed
,
Xenbase
Kleyman,
ENaC at the cutting edge: regulation of epithelial sodium channels by proteases.
2009,
Pubmed
Kota,
Energetic and structural basis for activation of the epithelial sodium channel by matriptase.
2012,
Pubmed
,
Xenbase
Krauson,
Independent contribution of extracellular proton binding sites to ASIC1a activation.
2013,
Pubmed
,
Xenbase
Ma,
Anionic phospholipids regulate native and expressed epithelial sodium channel (ENaC).
2002,
Pubmed
,
Xenbase
Maarouf,
Novel determinants of epithelial sodium channel gating within extracellular thumb domains.
2009,
Pubmed
,
Xenbase
Narikiyo,
Regulation of prostasin by aldosterone in the kidney.
2002,
Pubmed
,
Xenbase
Passero,
Plasmin activates epithelial Na+ channels by cleaving the gamma subunit.
2008,
Pubmed
,
Xenbase
Passero,
TMPRSS4-dependent activation of the epithelial sodium channel requires cleavage of the γ-subunit distal to the furin cleavage site.
2012,
Pubmed
,
Xenbase
Passero,
Defining an inhibitory domain in the gamma subunit of the epithelial sodium channel.
2010,
Pubmed
,
Xenbase
Patel,
Tissue kallikrein activation of the epithelial Na channel.
2012,
Pubmed
,
Xenbase
Pearce,
Collecting duct principal cell transport processes and their regulation.
2015,
Pubmed
Sheng,
Extracellular Zn2+ activates epithelial Na+ channels by eliminating Na+ self-inhibition.
2004,
Pubmed
,
Xenbase
Sheng,
Thumb domains of the three epithelial Na+ channel subunits have distinct functions.
2018,
Pubmed
,
Xenbase
Sheng,
Furin cleavage activates the epithelial Na+ channel by relieving Na+ self-inhibition.
2006,
Pubmed
,
Xenbase
Sheng,
External nickel inhibits epithelial sodium channel by binding to histidine residues within the extracellular domains of alpha and gamma subunits and reducing channel open probability.
2002,
Pubmed
,
Xenbase
Sheng,
Extracellular histidine residues crucial for Na+ self-inhibition of epithelial Na+ channels.
2004,
Pubmed
,
Xenbase
Shi,
Extracellular finger domain modulates the response of the epithelial sodium channel to shear stress.
2012,
Pubmed
,
Xenbase
Snyder,
A pore segment in DEG/ENaC Na(+) channels.
1999,
Pubmed
Suh,
PIP2 is a necessary cofactor for ion channel function: how and why?
2008,
Pubmed
Svenningsen,
Plasmin in nephrotic urine activates the epithelial sodium channel.
2009,
Pubmed
,
Xenbase
Winarski,
Extracellular allosteric regulatory subdomain within the gamma subunit of the epithelial Na+ channel.
2010,
Pubmed
,
Xenbase
Yue,
Phosphatidylinositol 4,5-bisphosphate (PIP2) stimulates epithelial sodium channel activity in A6 cells.
2002,
Pubmed
,
Xenbase