Ouabain Interactions with the H5-H6 Hairpin of the Na,K-ATPase Reveal a Possible Inhibition Mechanism via the Cation Binding Domain
Population
Na,K-ATPase alpha subunit (DNA sequence encoding amino acids between Lys-691 and Lys-945)
Design
Preclinical
Authors
Discussion
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Member takes
Implication
No immediate change to cardiac glycoside use; leaves open structural determinants of inhibition for future modeling.
Structured PICO
P
Population
Na,K-ATPase alpha subunit (DNA sequence encoding amino acids between Lys-691 and Lys-945)
I
Intervention
Random mutagenesis of residues Phe-786, Leu-793, and Phe-863
O
Outcome
Inhibition of Na,K-ATPase activity (I50 of cardiac glycosides)surrogate
Identifies a new region of the Na,K-ATPase containing the H5-H6 hairpin and H7 transmembrane segment as a major determinant of ouabain inhibition, suggesting a structural mechanism for cardiac glycoside action.
Cite This Study
Palasis et al. (1996) studied this question.