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Specific Estrogen Receptor Binding and Biological Effects of 16-Iodoestradiol on Human Breast Cancer Cells¹

Medicine Branch, National Cancer Institute, Bethesda, Maryland 20205 [M. E. L., H. M. T. D.], and Departments of Obstetrics and Gynecology, Molecular Biophysics, and Biochemistry, Yale University School of Medicine, New Haven, Connecticut 06510 [R. B. H.]

16-lodoestradiol was evaluated as an estrogen in MCF-7 and ZR-75-1 human breast cancer cells. 16-[¹²⁵I]lodoestradiol binds to equivalent numbers of specific estrogen receptors with a comparable binding affinity and similar sucrose density gradient behavior. 16-lodoestradiol translocates receptor sites to the nucleus and induces a full range of estrogenic effects including thymidine incorporation, cell growth, and progesterone receptor. Because of its high specific activity, this compound may have unique applications on imaging of estrogen receptor-containing cells and specific receptor-mediated cytotoxicity.

¹ This research supported in part by USPHS Grants R01 CA-29591 and K04 CA-00752 and by a grant from the Orentrich Foundation for the Advancement of Science.

² To whom requests for reprints should be addressed.

Received 3/27/80. Accepted 5/13/81.