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Scientific article
English

Two compounds commonly used for phospholipase C inhibition activate the nuclear estrogen receptors

Contributors

Cenni, Bruno; Picard, Didier

Published in

Biochemical and biophysical research communications, vol. 261, no. 2, p. 340-344

Publication date

1999

Abstract

The aminosteroid U73122 is generally used as a specific inhibitor of phosphoinositide specific phospholipase C (PLC) and typically, the structurally related compound U73343 is used as control, since it lacks PLC inhibitory activity. We have found that both compounds possess strong estrogenic activity and that this activity is mediated by the estrogen receptors (ER) alpha and beta. Although no direct evidence for binding of U73122 and U73343 to the ER could be provided, the estrogenic activity of the aminosteroids requires an intact ER hormone binding pocket. Given the chemical structure of the two aminosteroids, they may be converted to an estrogenic derivative by chemical degradation or an enzymatic metabolization reaction. Our data indicate that additional care should be taken in the interpretation of the effects of U73122 in cells expressing ER.

Keywords

  • Cell Line
  • Cell Nucleus/metabolism
  • Enzyme Inhibitors/chemistry/metabolism/pharmacology
  • Estradiol Congeners/chemistry/metabolism/pharmacology
  • Estrenes/chemistry/metabolism/pharmacology
  • Humans
  • Pyrrolidinones/chemistry/metabolism/pharmacology
  • Receptors, Estrogen/agonists/genetics/metabolism
  • Transfection
  • Type C Phospholipases/antagonists & inhibitors

UNIGE affiliation entities

Citation (ISO format)

CENNI, Bruno, PICARD, Didier. Two compounds commonly used for phospholipase C inhibition activate the nuclear estrogen receptors. In: Biochemical and biophysical research communications, 1999, vol. 261, n° 2, p. 340–344. doi: 10.1006/bbrc.1999.1017

Main files (1)

Article (Published version)

Identifiers

Journal ISSN

0006-291X
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Technical informations

Creation

08/12/2009 16:27:00

First validation

08/12/2009 16:27:00

Update

14/03/2023 15:19:32

Status update

14/03/2023 15:19:32

Last indexation

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