Stimulation of Airway and Intestinal Mucosal Secretion by Natural Coumarin CFTR Activators

Mutations of cystic fibrosis (CF) transmembrane conductance regulator (CFTR) cause lethal hereditary disease CF that involves extensive destruction and dysfunction of serous epithelium. Possible pharmacological therapy includes correction of defective intracellular processing and abnormal channel ga...

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Bibliographic Details
Published in:Frontiers in pharmacology 2011-01, Vol.2, p.52-52
Main Authors: Yang, Hong, Xu, Li-Na, Sui, Yu-Jie, Liu, Xin, He, Cheng-Yan, Fang, Rou-Yu, Liu, Jia, Hao, Feng, Ma, Tong-Hui
Format: Article
Language:English
Subjects:
activator
airway
CFTR
Colon
Coumarins
Mucosa
Pharmacology
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Summary:Mutations of cystic fibrosis (CF) transmembrane conductance regulator (CFTR) cause lethal hereditary disease CF that involves extensive destruction and dysfunction of serous epithelium. Possible pharmacological therapy includes correction of defective intracellular processing and abnormal channel gating. In a previous study, we identified five natural coumarin potentiators of ΔF508-CFTR including osthole, imperatorin, isopsoralen, praeruptorin A, and scoparone. The present study was designed to determine the activity of these coumarine compounds on CFTR activity in animal tissues as a primary evaluation of their therapeutic potential. In the present study, we analyzed the affinity of these coumarin potentiators in activating wild-type CFTR and found that they are all potent activators. Osthole showed the highest affinity with K(d) values
ISSN:1663-9812
1663-9812
DOI:10.3389/fphar.2011.00052