Permeabilization via the P2X(7) purinoreceptor reveals the presence of a Ca2+-activated Cl- conductance in the apical membrane of murine tracheal epithelial cells

Gabriel, SE; Makhlina, M; Martsen, E; Thomas, EJ; Lethem, MI; Boucher, RC

HERO ID

2789349

Reference Type

Journal Article

Year

2000

Language

English

PMID

10944530

HERO ID 2789349
In Press No
Year 2000
Title Permeabilization via the P2X(7) purinoreceptor reveals the presence of a Ca2+-activated Cl- conductance in the apical membrane of murine tracheal epithelial cells
Authors Gabriel, SE; Makhlina, M; Martsen, E; Thomas, EJ; Lethem, MI; Boucher, RC
Journal Journal of Biological Chemistry
Volume 275
Issue 45
Page Numbers 35028-35033
Abstract Calcium-activated Cl(-) secretion is an important modulator of regulated ion transport in murine airway epithelium and is mediated by an unidentified Ca(2+)-stimulated Cl(-) channel. We have transfected immortalized murine tracheal epithelial cells with the cDNA encoding the permeabilizing P2X(7) purinoreceptor (P2X(7)-R) to selectively permeabilize the basolateral membrane and thereby isolate the apical membrane Ca(2+)-activated Cl(-) current. In P2X(7)-R-permeabilized cells, we have demonstrated that UTP stimulates a Cl(-) current across the apical membrane of CF and normal murine tracheal epithelial cells. The magnitude of the UTP-stimulated current was significantly greater in CF than in normal cells. Ion substitution studies demonstrated that the current exhibited a permselectivity sequence of Cl(-) > I(-) > Br(-) > gluconate(-). We have also determined a rank order of potency for putative Cl(-) channel blockers: niflumic acid > or = 5-nitro-2-(3-phenylpropylamino)benzoic acid > 4, 4'-diisothiocyanostilbene-2,2'-disulfonate > glybenclamide > diphenlyamine-2-carboxylate, tamoxifen, and p-tetra-sulfonato-tetra-methoxy-calix[4]arene. Complete characterization of this current and the corresponding single channel properties could lead to the development of a new therapy to correct the defective airway surface liquid in cystic fibrosis patients.
Doi 10.1074/jbc.M004953200
Pmid 10944530
Wosid WOS:000165422800029
Is Certified Translation No
Dupe Override No
Is Public Yes
Language Text English