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Binding of 2-Hydroxybenzo(a)pyrene to Estrogen Receptors in Rat Cytosol

Department of Microbiology and Molecular Genetics [R. H. E.], and Dana-Farber Cancer Institute [J. R. W., L. B. C.], Harvard Medical School, Boston, Massachusetts, 02115

The potent carcinogen 2-hydroxybenzo(a)pyrene (2-OH-BP) competes for binding to the estrogen receptor in the cytosol of rat uterus and liver. The dissociation constant (K_i) for this interaction is 2 x 10^-5 M. In contrast, 4-hydroxybenzo(a)pyrene does not bind to the estrogen receptor; 1-hydroxybenzo(a)pyrene, 5-hydroxybenzo(a)pyrene, 6-hydroxybenzo-(a)pyrene, and 12-hydroxybenzo(a)pyrene bind less tightly than does 2-OH-BP. These five chemicals are not carcinogenic. We suggest that the estrogen receptor may mediate the carcinogenic effect of 2-OH-BP or of related chemicals. One possibility is that the receptor might convey 2-OH-BP to specific sites in DNA.

¹ Supported in part by NIH Grants RR-01032 and CA22659.

² Supported in part by National Cancer Institute Grant CA22659.

Received 9/ 5/85. Revised 1/14/86. Accepted 2/ 7/86.

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