PMID: 8967457May 1, 1996Paper

Delta F508-CFTR channels: kinetics, activation by forskolin, and potentiation by xanthines

The American Journal of Physiology
C M HawsJ J Wine

Abstract

Trafficking, activation, and kinetics of delta F508-cystic fibrosis transmembrane conductance regulator (CFTR) and CFTR were compared in stably transduced C127I mouse mammary epithelial cells. Western blots detected a small amount of fully glycosylated delta F508-CFTR Efflux of 125I was stimulated by forskolin with the same mean effective concentration (EC50; approximately 0.5 microM) for CFTR and delta F508-CFTR cells, but the maximum response was reduced more than fivefold and its latency increased approximately threefold in delta F508-CFTR cells. In delta F508-CFTR cells, 3-isobutyl-1-methylxanthine (IBMX; EC50 = 1.45 microM) and 8-cyclopentyl-1,3-dipropylxanthine (CPX; EC50 = 58 microM) increased the peak forskolin-stimulated efflux rate approximately 2.5-fold and decreased the time to peak. A sevenfold increase in intracellular adenosine 3',5'-cyclic monophosphate (cAMP) levels accompanied potentiation of forskolin-induced 125I efflux by IBMX but not by CPX. Elevation of intracellular cAMP increased linear voltage-independent whole cell currents 30-fold in CFTR and 4-fold in delta F508-CFTR cells; the response rate in delta F508-CFTR cells was much slower. Single-channel currents were detected in 57 of 68 cell-attached pat...Continue Reading

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Citations

Oct 1, 1998·The American Journal of Physiology·Z HeW W Reenstra
Jul 13, 2000·Microscopy Research and Technique·A Dragomir, G M Roomans
Dec 12, 2000·The Journal of Biological Chemistry·J V WuJ J Wine
Dec 21, 2000·American Journal of Physiology. Cell Physiology·G D HedaC R Marino
Jan 22, 2002·Pediatric Pulmonology·Nael A McCartyRichard C Ahrens
Oct 3, 2002·British Journal of Pharmacology·Olga Zegarra-MoranLuis J V Galietta
Jan 15, 2004·American Journal of Respiratory Medicine : Drugs, Devices, and Other Interventions·Godfried M Roomans
Jun 28, 2014·The Journal of Pharmacology and Experimental Therapeutics·Clément BoinotFrédéric Becq
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Mar 19, 2004·American Journal of Physiology. Cell Physiology·Lane L ClarkeElmer M Price
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Jul 2, 2003·The Journal of Biological Chemistry·Hong YangA S Verkman
Sep 19, 2007·The Journal of Membrane Biology·Loretta FerreraOscar Moran
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Apr 24, 2008·Clinical and Experimental Pharmacology & Physiology·Li-Na XuTong-Hui Ma
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