Effects of anti-oestrogens and β-estradiol on calcium uptake by cardiac sarcoplasmic reticulum

1. Tamoxifen and a group of structurally similar non-steroidal, triphenolic compounds inhibit the oestrogen receptor. In addition to this action, these anti-oestrogens are known to inhibit some types of plasma membrane ion channels and other proteins through mechanisms that do not appear to involve...

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Main Authors: Dodds, Marnie L, Kargacin, Margaret E, Kargacin, Gary J
Formato: Artigo
Idioma:English
Publicado em: 2001
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Papers
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC1572683/
https://ncbi.nlm.nih.gov/pubmed/11264229
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/sj.bjp.0703924
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spelling pubmed-15726832008-01-10 Effects of anti-oestrogens and β-estradiol on calcium uptake by cardiac sarcoplasmic reticulum Dodds, Marnie L Kargacin, Margaret E Kargacin, Gary J Br J Pharmacol Papers 1. Tamoxifen and a group of structurally similar non-steroidal, triphenolic compounds inhibit the oestrogen receptor. In addition to this action, these anti-oestrogens are known to inhibit some types of plasma membrane ion channels and other proteins through mechanisms that do not appear to involve their interactions with the estrogen receptor but could be the result of their effect on membrane lipid structure or fluidity. 2. We studied the effects of β-estradiol and three anti-oestrogens (tamoxifen, 4-hydroxytamoxifen and clomiphene) on Ca(2+) uptake into sarcoplasmic reticulum (SR) vesicles isolated from canine cardiac ventricular tissue. 3. The antiestrogens all inhibit SR Ca(2+) uptake in a concentration-dependent manner (order of potency: tamoxifen > 4-hydroxytamoxifen ⩾ clomiphene). Although these compounds rapidly inhibit net Ca(2+) uptake they do not have a similar rapid effect on the ATPase activity of the SR Ca pump. β-estradiol has no effect on Ca(2+) uptake nor does it alter the inhibitory action of tamoxifen on the SR. 4. The differences in the effects of β-estradiol and the anti-oestrogens on cardiac SR Ca(2+) uptake do not correlate with differences in the ways in which these compounds have been reported to interact with membrane lipids. Our results are consistent, however, with direct effects on a membrane protein (possibly an SR Cl(−) or K(+) channel). 2001-04 /pmc/articles/PMC1572683/ /pubmed/11264229 http://dx.doi.org/10.1038/sj.bjp.0703924 Text en Copyright 2001, Nature Publishing Group
institution US National Library of Medicine
collection PubMed Central
language English
format Article
topic Papers
spellingShingle Papers
Dodds, Marnie L
Kargacin, Margaret E
Kargacin, Gary J
Effects of anti-oestrogens and β-estradiol on calcium uptake by cardiac sarcoplasmic reticulum
description 1. Tamoxifen and a group of structurally similar non-steroidal, triphenolic compounds inhibit the oestrogen receptor. In addition to this action, these anti-oestrogens are known to inhibit some types of plasma membrane ion channels and other proteins through mechanisms that do not appear to involve their interactions with the estrogen receptor but could be the result of their effect on membrane lipid structure or fluidity. 2. We studied the effects of β-estradiol and three anti-oestrogens (tamoxifen, 4-hydroxytamoxifen and clomiphene) on Ca(2+) uptake into sarcoplasmic reticulum (SR) vesicles isolated from canine cardiac ventricular tissue. 3. The antiestrogens all inhibit SR Ca(2+) uptake in a concentration-dependent manner (order of potency: tamoxifen > 4-hydroxytamoxifen ⩾ clomiphene). Although these compounds rapidly inhibit net Ca(2+) uptake they do not have a similar rapid effect on the ATPase activity of the SR Ca pump. β-estradiol has no effect on Ca(2+) uptake nor does it alter the inhibitory action of tamoxifen on the SR. 4. The differences in the effects of β-estradiol and the anti-oestrogens on cardiac SR Ca(2+) uptake do not correlate with differences in the ways in which these compounds have been reported to interact with membrane lipids. Our results are consistent, however, with direct effects on a membrane protein (possibly an SR Cl(−) or K(+) channel).
author Dodds, Marnie L
Kargacin, Margaret E
Kargacin, Gary J
author_facet Dodds, Marnie L
Kargacin, Margaret E
Kargacin, Gary J
author_sort Dodds, Marnie L
title Effects of anti-oestrogens and β-estradiol on calcium uptake by cardiac sarcoplasmic reticulum
title_short Effects of anti-oestrogens and β-estradiol on calcium uptake by cardiac sarcoplasmic reticulum
title_full Effects of anti-oestrogens and β-estradiol on calcium uptake by cardiac sarcoplasmic reticulum
title_fullStr Effects of anti-oestrogens and β-estradiol on calcium uptake by cardiac sarcoplasmic reticulum
title_full_unstemmed Effects of anti-oestrogens and β-estradiol on calcium uptake by cardiac sarcoplasmic reticulum
title_sort effects of anti-oestrogens and β-estradiol on calcium uptake by cardiac sarcoplasmic reticulum
publishDate 2001
url https://ncbi.nlm.nih.gov/pmc/articles/PMC1572683/
https://ncbi.nlm.nih.gov/pubmed/11264229
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/sj.bjp.0703924
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