A receptor-independent effect of estrone sulfate on the hERG channel

Shoko Kakusaka; Mahoko Asayama; Asami Kaihara; Tetsuo Sasano; Takeshi Suzuki; Junko Kurokawa; Tetsushi Furukawa

doi:10.1254/jphs.08257SC

A receptor-independent effect of estrone sulfate on the hERG channel

Shoko Kakusaka, Mahoko Asayama, Asami Kaihara, Tetsuo Sasano, Takeshi Suzuki, Junko Kurokawa, Tetsushi Furukawa

Research output: Contribution to journal › Article › peer-review

17 Citations (Scopus)

Abstract

We recently reported that physiological concentrations of 17β-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 17β-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.

Original language	English
Pages (from-to)	152-156
Number of pages	5
Journal	Journal of Pharmacological Sciences
Volume	109
Issue number	1
DOIs	https://doi.org/10.1254/jphs.08257SC
Publication status	Published - 2009
Externally published	Yes

Keywords

Estrogen
Heart
K channel (hERG)

ASJC Scopus subject areas

Molecular Medicine
Pharmacology

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10.1254/jphs.08257SC

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abstract = "We recently reported that physiological concentrations of 17β-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 17β-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.",

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AU - Kakusaka, Shoko

AU - Asayama, Mahoko

AU - Kaihara, Asami

AU - Sasano, Tetsuo

AU - Suzuki, Takeshi

AU - Kurokawa, Junko

AU - Furukawa, Tetsushi

PY - 2009

Y1 - 2009

N2 - We recently reported that physiological concentrations of 17β-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 17β-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.

AB - We recently reported that physiological concentrations of 17β-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 17β-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.

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KW - Heart

KW - K channel (hERG)

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A receptor-independent effect of estrone sulfate on the hERG channel

Abstract

Keywords

ASJC Scopus subject areas

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