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

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;...

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Veröffentlicht in:	Cancer research (Chicago, Ill.) Ill.), 1986-05, Vol.46 (5), p.2349-2351
Hauptverfasser:	EBRIGHT, R. H, WONG, J. R, CHEN, L. B
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzopyrenes - metabolism Binding, Competitive Biological and medical sciences Carcinogenesis, carcinogens and anticarcinogens Chemical agents Cytosol - metabolism Estradiol - metabolism Female Medical sciences Rats Receptors, Estrogen - metabolism Structure-Activity Relationship Tumors Uterus - metabolism
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Zusammenfassung:	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.
ISSN:	0008-5472 1538-7445