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Biochem Biophys Res Commun. 1992 May 15;184(3):1432-40.

Antagonistic effect of triphenylethylenic antiestrogens on the association of estrogen receptor to calmodulin.

Author information

1
Institut Jules Bordet, Service de Médecine, Laboratoire J.C. Heuson de Cancérologie Mammaire et d'Endocrinologie, Brussels, Belgium.

Abstract

Binding of (3H)-estradiol labeled estrogen receptor from uterine cytosol to calmodulin was demonstrated by both affinity chromatography and sucrose gradient sedimentation. Triphenylethylene antiestrogens (tamoxifen family) with strong antagonistic activity against the calmodulin-dependent c-AMP phosphodiesterase largely reduced the binding of the receptor. Relevance of this observation with regard to the major antiproliferative activity (cytotoxicity) of these drugs is discussed.

PMID:
1590802
DOI:
10.1016/s0006-291x(05)80043-9
[Indexed for MEDLINE]

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