Article
CFTR inhibition by glibenclamide requires a positive charge in cytoplasmic loop three.
Biochimica et biophysica acta - 1 Oct 2007
Melin Patricia, Hosy Eric, Vivaudou Michel, Becq Frédéric
Abstract excerpt
The sulfonylurea glibenclamide is widely used as an open-channel blocker of the CFTR chloride channel. Here, we used site-directed mutagenesis to identify glibenclamide site of interaction: a positively charged residue K978, located in the cytoplasmic loop 3. Charge-neutralizing mutations K978A, K978Q, K978S abolished the inhibition of forskolin-activated CFTR chloride current by glibenclamide but not by...
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