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Molecular Pharmacology

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Research ArticleArticle

Diethylstilbestrol Is a Potent Inhibitor of Store-Operated Channels and Capacitative Ca2+ Influx

Sergey I. Zakharov, Tarik Smani, Yuliya Dobrydneva, Francisco Monje, Craig Fichandler, Peter F. Blackmore and Victoria M. Bolotina
Molecular Pharmacology September 2004, 66 (3) 702-707;
Sergey I. Zakharov
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Tarik Smani
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Yuliya Dobrydneva
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Francisco Monje
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Craig Fichandler
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Peter F. Blackmore
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Victoria M. Bolotina
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Abstract

We have recently found that diethylstilbestrol (DES), a synthetic estrogen agonist, inhibits thrombin-induced Ca2+ influx in human platelets, but it remains unclear to what extend this effect might be related to the store-operated Ca2+ influx pathway. To study the effect of DES on store-operated channels and capacitative Ca2+ influx, we used rat basophilic leukemia (RBL) cells, vascular smooth muscle cells (SMC), and human platelets, and recorded whole-cell Ca2+ release-activated Ca2+ (CRAC) currents and thapsigargin (TG)-induced capacitative Ca2+ influx. In this study, we demonstrate that extracellular DES produces a dose-dependent and reversible inhibition of CRAC currents in RBL cells (IC50, ∼0.5 μM), whereas intracellular DES (25 μM) has no effect. Extracellular DES (up to 30 μM) inhibited only CRAC but did not affect a whole-cell monovalent cation current mediated by TRPM7 channels. DES effectively inhibited TG-induced capacitative Ca2+ influx in a dose-dependent manner with an IC50 values of ∼0.1 μM in RBL cells, <0.1 μM in SMC, and ∼1 μM in human platelets. It is noteworthy that trans-stilbene, a close structural analog of DES that lacks hydroxyl and ethyl groups, had no effect on CRAC current and on store-operated Ca2+ influx. Thus, we found DES to be a very effective inhibitor of store-operated channels and Ca2+ influx in a variety of cell types.

  • Received January 22, 2004.
  • Accepted June 16, 2004.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 66 (3)
Molecular Pharmacology
Vol. 66, Issue 3
1 Sep 2004
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Research ArticleArticle

Diethylstilbestrol Is a Potent Inhibitor of Store-Operated Channels and Capacitative Ca2+ Influx

Sergey I. Zakharov, Tarik Smani, Yuliya Dobrydneva, Francisco Monje, Craig Fichandler, Peter F. Blackmore and Victoria M. Bolotina
Molecular Pharmacology September 1, 2004, 66 (3) 702-707;

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Research ArticleArticle

Diethylstilbestrol Is a Potent Inhibitor of Store-Operated Channels and Capacitative Ca2+ Influx

Sergey I. Zakharov, Tarik Smani, Yuliya Dobrydneva, Francisco Monje, Craig Fichandler, Peter F. Blackmore and Victoria M. Bolotina
Molecular Pharmacology September 1, 2004, 66 (3) 702-707;
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