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      Selectivity of digitalis glycosides for isoforms of human Na,K-ATPase.

      The Journal of Biological Chemistry

      Cardiac Glycosides, metabolism, Cell Membrane, Digitalis Glycosides, Humans, Ions, Kinetics, Models, Biological, Models, Statistical, Myocardium, Pichia, Potassium, chemistry, Protein Binding, Protein Isoforms, Sodium-Potassium-Exchanging ATPase, Time Factors

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          Abstract

          There are four isoforms of the alpha subunit (alpha1-4) and three isoforms of the beta subunit (beta1-3) of Na,K-ATPase, with distinct tissue-specific distribution and physiological functions. alpha2 is thought to play a key role in cardiac and smooth muscle contraction and be an important target of cardiac glycosides. An alpha2-selective cardiac glycoside could provide important insights into physiological and pharmacological properties of alpha2. The isoform selectivity of a large number of cardiac glycosides has been assessed utilizing alpha1beta1, alpha2beta1, and alpha3beta1 isoforms of human Na,K-ATPase expressed in Pichia pastoris and the purified detergent-soluble isoform proteins. Binding affinities of the digitalis glycosides, digoxin, beta-methyl digoxin, and digitoxin show moderate but highly significant selectivity (up to 4-fold) for alpha2/alpha3 over alpha1 (K(D) alpha1 > alpha2 = alpha3). By contrast, ouabain shows moderate selectivity ( approximately 2.5-fold) for alpha1 over alpha2 (K(D) alpha1

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          Author and article information

          Journal
          20388710
          10.1074/jbc.M110.119248
          2885237

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