The physiological significance of the cardiotonic steroid/ouabain-binding site of the Na,K-ATPase.
The physiological significance of the cardiotonic steroid/ouabain-binding site of the Na,K-ATPase.
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DOI：
10.1146/annurev-physiol-021909-135725
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发表时间：
2010
影响因子：
18.2
通讯作者：
Lingrel JB
中科院分区：
文献类型：
--
作者：
Lingrel JB
Na，K-ATP酶是膜“泵”，其产生穿过质膜的Na+和K+梯度，从而驱动许多生理过程。这种酶对强心类固醇的抑制非常敏感，最值得注意的是洋地黄/哇巴因类化合物，几个世纪以来一直用于治疗充血性心力衰竭和心律失常。构成哇巴因结合位点的氨基酸在整个进化谱中高度保守。这可能是偶然的，也可能是由于该位点具有重要的生物学功能而被保守。使用基因工程小鼠的新生理学方法正被用于定义Na，K-ATP酶的“受体功能”的生物学意义及其通过潜在的内源性强心类固醇样化合物的调节。这些研究扩展了涉及内源性调节配体的生化纯化的早期研究的范围。
The Na,K-ATPase is the membrane “pump” that generates the Na+ and K+ gradients across the plasma membrane that drives many physiological processes. This enzyme is highly sensitive to inhibition by cardiotonic steroids, most notably the digitalis/ouabain class of compounds, which have been used for centuries to treat congestive heart failure and arrhythmias. The amino acids that constitute the ouabain-binding site are highly conserved across the evolutionary spectrum. This could be fortuitous or could result from this site being conserved because it has an important biological function. New physiological approaches using genetically engineered mice are being used to define the biological significance of the “receptor function” of the Na,K-ATPase and its regulation by potential endogenous cardiotonic steroid-like compounds. These studies extend the reach of earlier studies involving the biochemical purification of endogenous regulatory ligands.
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