UNIGE document Scientific Article
previous document  unige:4633  next document
add to browser collection

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

Cenni, Bruno
Published in Biochemical and Biophysical Research Communications. 1999, vol. 261, no. 2, p. 340-4
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 LineCell Nucleus/metabolismEnzyme Inhibitors/chemistry/metabolism/pharmacologyEstradiol Congeners/chemistry/metabolism/pharmacologyEstrenes/chemistry/metabolism/pharmacologyHumansPyrrolidinones/chemistry/metabolism/pharmacologyReceptors, Estrogen/agonists/genetics/metabolismTransfectionType C Phospholipases/antagonists & inhibitors
PMID: 10425187
Full text
Article (Published version) (73 Kb) - document accessible for UNIGE members only Limited access to UNIGE
(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. 340-4. https://archive-ouverte.unige.ch/unige:4633

161 hits

1 download


Deposited on : 2009-12-08

Export document
Format :
Citation style :