Butyl-p-hydroxybenzoate stimulates cystic fibrosis transmembrane conductance regulator Cl- transport / 药学学报
Acta Pharmaceutica Sinica
;
(12): 32-37, 2009.
Artigo
em Chinês
| WPRIM
| ID: wpr-232602
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 delta 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.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Parabenos
/
Farmacologia
/
Ratos Endogâmicos F344
/
Glândula Tireoide
/
Ativação do Canal Iônico
/
Linhagem Celular
/
Regulador de Condutância Transmembrana em Fibrose Cística
/
Biologia Celular
/
Proteínas de Fluorescência Verde
/
Relação Dose-Resposta a Droga
Limite:
Animais
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2009
Tipo de documento:
Artigo
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