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 journalArticle

14 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 languageEnglish
Pages (from-to)152-156
Number of pages5
JournalJournal of Pharmacological Sciences
Volume109
Issue number1
DOIs
Publication statusPublished - 2009

Fingerprint

Estrogens
Estradiol Receptors
Estriol
Estrone
HEK293 Cells
Estrogen Receptors
Estradiol
Down-Regulation
estrone sulfate

Keywords

  • Estrogen
  • Heart
  • K channel (hERG)

ASJC Scopus subject areas

  • Pharmacology
  • Molecular Medicine

Cite this

Kakusaka, S., Asayama, M., Kaihara, A., Sasano, T., Suzuki, T., Kurokawa, J., & Furukawa, T. (2009). A receptor-independent effect of estrone sulfate on the hERG channel. Journal of Pharmacological Sciences, 109(1), 152-156. https://doi.org/10.1254/jphs.08257SC

A receptor-independent effect of estrone sulfate on the hERG channel. / Kakusaka, Shoko; Asayama, Mahoko; Kaihara, Asami; Sasano, Tetsuo; Suzuki, Takeshi; Kurokawa, Junko; Furukawa, Tetsushi.

In: Journal of Pharmacological Sciences, Vol. 109, No. 1, 2009, p. 152-156.

Research output: Contribution to journalArticle

Kakusaka, S, Asayama, M, Kaihara, A, Sasano, T, Suzuki, T, Kurokawa, J & Furukawa, T 2009, 'A receptor-independent effect of estrone sulfate on the hERG channel', Journal of Pharmacological Sciences, vol. 109, no. 1, pp. 152-156. https://doi.org/10.1254/jphs.08257SC
Kakusaka, Shoko ; Asayama, Mahoko ; Kaihara, Asami ; Sasano, Tetsuo ; Suzuki, Takeshi ; Kurokawa, Junko ; Furukawa, Tetsushi. / A receptor-independent effect of estrone sulfate on the hERG channel. In: Journal of Pharmacological Sciences. 2009 ; Vol. 109, No. 1. pp. 152-156.
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