Binding of 2-hydroxybenzo(a)pyrene to estrogen receptors in rat cytosol.

Ebright, RH, Wong JR, Chen LB.  1986.  

Journal:

Cancer research

Volume Number:

46

Issue Number:

5

Pages:

2349-51

Abstract:

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 (K1) for this interaction is congruent to 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.

Citation:
Ebright, RH, Wong JR, Chen LB.  1986.  Binding of 2-hydroxybenzo(a)pyrene to estrogen receptors in rat cytosol.. Cancer research. 46(5):2349-51.