A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel
A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel
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DOI：
10.1254/jphs.08257sc
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发表时间：
2009-01-01
影响因子：
3.5
通讯作者：
Furukawa, Tetsushi
中科院分区：
文献类型：
--
作者：
Kakusaka, Shoko;Asayama, Mahoko;Furukawa, Tetsushi
我们最近报道了17 β -雌二醇的生理浓度部分下调心脏快速激活的延迟整流K+电流（hERG电流），独立于雌激素受体信号传导。为了确定其他雌激素是否具有与17 β -雌二醇相同的作用，我们研究了雌酮、雌酮3-硫酸酯和雌三醇对贴片钳型雌激素阴性HEK293细胞中hERG电流的受体独立效应。只有雌酮3-硫酸通过改变门控以受体无关的方式部分抑制hERG电流。雌酮3-硫酸的浓度依赖性表明，生理水平的循环雌酮3-硫酸可以最大程度地调节任何年龄的女性和男性的hERG电流。
We recently reported that physiological concentrations of 17 beta-estradiol partially down-regulate cardiac rapidly-activating delayed rectifier K+ currents (hERG currents) independently of estrogen-receptor signaling. To determine if other estrogens have the same effect as that of 17 beta-estradiol, we investigated receptor-independent effects of estrone, estrone 3-sulfate, and estriol on hERG currents in patch-clamped estrogen-negative HEK293 cells. Only estrone 3-sulfate partially suppressed hERG currents in a receptor-independent manner by modifying the gating. The concentration-dependence of estrone 3-sulfate revealed that physiological levels of circulating estrone 3-sulfate can modulate hERG currents to the maximal extent in both women and men at any age.