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The anti-tumor drug adriamycin, when added to the culture medium, increases the activity of DNA methyltransferase (MTase) in tissue culture cells. The effect is of long duration, lasting more than 4 hours and becoming maximal at 100 nM adriamycin, while with higher concentrations the increase in MTase activity subsides. The effect of adriamycin is concentration-dependent and can be produced without addition of the drug to the cell medium. It is blocked by the antioxidant ditiothreitol, but not by chelating agents. Tamoxifen, an anti-estrogen hormone, also stimulates MTase activity, though the magnitude of the response is less than that obtained with adriamycin. Tamoxifen-induced MTase activity becomes maximal in 10 min, and persists for at least 1 hour. Furthermore, the effect of tamoxifen is inhibited by the anti-estrogen aglycone of tamoxifen, estradiol, but not by the basic steroidal structure of the molecule. These observations suggest that adriamycin and tamoxif