A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel

A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel

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 inv...

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Main Authors: Shoko Kakusaka, Mahoko Asayama, Asami Kaihara, Tetsuo Sasano, Takeshi Suzuki, Junko Kurokawa, Tetsushi Furukawa
Format: Article
Language:English
Published: Elsevier 2009-01-01
Series:Journal of Pharmacological Sciences
Online Access:http://www.sciencedirect.com/science/article/pii/S1347861319341210
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spelling doaj-8f6515e03e42490a977fe5be563c89652020-11-24T22:01:18ZengElsevierJournal of Pharmacological Sciences1347-86132009-01-011091152156A Receptor-Independent Effect of Estrone Sulfate on the hERG ChannelShoko Kakusaka0Mahoko Asayama1Asami Kaihara2Tetsuo Sasano3Takeshi Suzuki4Junko Kurokawa5Tetsushi Furukawa6Department of Bio-Informational Pharmacology, Medical Research Institute, Tokyo Medical and Dental University, Bunkyo-ku, Tokyo 113-8510, Japan; Division of Basic Biological Sciences, Faculty of Pharmacy, Keio University, Minato-ku, Tokyo 105-8512, JapanDepartment of Bio-Informational Pharmacology, Medical Research Institute, Tokyo Medical and Dental University, Bunkyo-ku, Tokyo 113-8510, Japan; Mitsubishi Tanabe Pharma Corporation, Safety Research Division, Kisarazu, Chiba 292-0818, JapanDepartment of Bio-Informational Pharmacology, Medical Research Institute, Tokyo Medical and Dental University, Bunkyo-ku, Tokyo 113-8510, JapanDepartment of Bio-Informational Pharmacology, Medical Research Institute, Tokyo Medical and Dental University, Bunkyo-ku, Tokyo 113-8510, JapanDivision of Basic Biological Sciences, Faculty of Pharmacy, Keio University, Minato-ku, Tokyo 105-8512, JapanDepartment of Bio-Informational Pharmacology, Medical Research Institute, Tokyo Medical and Dental University, Bunkyo-ku, Tokyo 113-8510, Japan; Corresponding author. junkokuro.bip@mri.tmd.ac.jpDepartment of Bio-Informational Pharmacology, Medical Research Institute, Tokyo Medical and Dental University, Bunkyo-ku, Tokyo 113-8510, JapanWe 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. Keywords:: estrogen, K+ channel (hERG), hearthttp://www.sciencedirect.com/science/article/pii/S1347861319341210
collection DOAJ
language English
format Article
sources DOAJ
author Shoko Kakusaka
Mahoko Asayama
Asami Kaihara
Tetsuo Sasano
Takeshi Suzuki
Junko Kurokawa
Tetsushi Furukawa
spellingShingle Shoko Kakusaka
Mahoko Asayama
Asami Kaihara
Tetsuo Sasano
Takeshi Suzuki
Junko Kurokawa
Tetsushi Furukawa
A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel
Journal of Pharmacological Sciences
author_facet Shoko Kakusaka
Mahoko Asayama
Asami Kaihara
Tetsuo Sasano
Takeshi Suzuki
Junko Kurokawa
Tetsushi Furukawa
author_sort Shoko Kakusaka
title A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel
title_short A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel
title_full A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel
title_fullStr A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel
title_full_unstemmed A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel
title_sort receptor-independent effect of estrone sulfate on the herg channel
publisher Elsevier
series Journal of Pharmacological Sciences
issn 1347-8613
publishDate 2009-01-01
description 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. Keywords:: estrogen, K+ channel (hERG), heart
url http://www.sciencedirect.com/science/article/pii/S1347861319341210
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