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[Cancer Research 45, 2462-2465, June 1, 1985]
© 1985 American Association for Cancer Research
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Inhibition of Protein Kinase C by Tamoxifen1

Catherine A. O'Brian2, Rob M. Liskamp, David H. Solomon and I. Bernard Weinstein

Division of Environmental Sciences and Institute of Cancer Research, Columbia University, New York, New York 10032

The antiestrogen drug tamoxifen inhibits rat brain protein kinase C in vitro, whether the enzyme is activated by Ca2+ and phospholipid (50% inhibitory dose, 100 µM), 12-O-tetradecanoylphorbol-13-acetate and phospholipid (50% inhibitory dose, 40 µM), or teleocidin and phospholipid. Tamoxifen does not inhibit the Ca2+ - and phospholipid-independent phosphorylation of protamine sulfate by protein kinase C, indicating that the drug does not interact with the active site of the enzyme. The binding of [3H]phorbol dibutyrate to high-affinity membrane receptors of cultured mouse fibroblast cells is inhibited by tamoxifen (50% inhibitory dose, 5 µM). Our findings suggest that the growth-inhibitory and cytotoxic effects of tamoxifen, which have been observed at µM concentrations of the drug, may be in part due to its effects on protein kinase C.

1 This work was supported by National Cancer Institute Grant CA-26056 and the Netherlands Cancer Foundation.

2 To whom requests for reprints should be addressed.

Received 10/29/84. Revised 1/22/85. Accepted 3/13/85.




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HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH TABLE OF CONTENTS
Cancer Research Clinical Cancer Research
Cancer Epidemiology Biomarkers & Prevention Molecular Cancer Therapeutics
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Annual Meeting Education Book Meeting Abstracts Online
Copyright © 1985 by the American Association for Cancer Research.