Low free drug concentration prevents inhibition of F508del CFTR functional expression by the potentiator VX‐770 (ivacaftor)

BACKGROUND AND PURPOSE: The most common cystic fibrosis (CF) mutation F508del inhibits the gating and surface expression of CFTR, a plasma membrane anion channel. Optimal pharmacotherapies will probably require both a ‘potentiator’ to increase channel open probability and a ‘corrector’ that improves...

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Bibliografiske detaljer
Udgivet i:Br J Pharmacol
Main Authors: Matthes, Elizabeth, Goepp, Julie, Carlile, Graeme W, Luo, Yishan, Dejgaard, Kurt, Billet, Arnaud, Robert, Renaud, Thomas, David Y, Hanrahan, John W
Format: Artigo
Sprog:Inglês
Udgivet: John Wiley and Sons Inc. 2016
Fag:
Research Papers
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4728415/
https://ncbi.nlm.nih.gov/pubmed/26492939
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1111/bph.13365
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