GE Gong, Hou-Ting-Ting, Sun-Juan-Juan, Yang- Gong. Butyl-p-hydroxybenzoate stimulates cystic fibrosis transmembrane conductance regulator Cl- transportJ. 药学学报, 2009,44(1): 32-37.
Citation: GE Gong, Hou-Ting-Ting, Sun-Juan-Juan, Yang- Gong. Butyl-p-hydroxybenzoate stimulates cystic fibrosis transmembrane conductance regulator Cl- transportJ. 药学学报, 2009,44(1): 32-37.
shu

Butyl-p-hydroxybenzoate stimulates cystic fibrosis transmembrane conductance regulator Cl- transport

    Abstract
  • This study is to investigate the activation effect of butyl-p-hydroxybenzoate (Bpb) on cAMP-dependent cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel gating.  A stably transfected Fischer rat thyroid (FRT) epithelial cell lines co-expressing human CFTR and a green fluorescent protein mutant with ultra-high halide sensitivity (EYFP) were used to measure CFTR-mediated iodide influx rates.  Bpb was identified as an effective activator of wild-type CFTR chloride channel, it can correct ?F508-CFTR gating defects but not processing defect.  Bpb can’t potentiate G551D-CFTR channel gating.  The activity was reversible and dose-dependent.  The study also provided clues that Bpb activates CFTR chloride channel through a direct binding mechanism.  Our study identified Bpb as a novel structure CFTR activator.  Bpb may be useful for probing CFTR channel gating mechanisms and as a lead compound to develop pharmacological therapy for CFTR-related disease.
    • FullText(HTML)
  • loading
    • References (0)
    • Relative Articles
  • Supplements (0)

Catalog

    Turn off MathJax
    Article Contents

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return