The relative binding affinity of diethylstilbestrol to uterine nuclear estrogen receptor: effect of serum and serum albumin.
The relative binding affinity (RBA) of diethylstilbestrol (DES) was determined in nuclear fractions of the rat uterus. DES displayed a two- to threefold greater affinity (RBA = 245 +/- 36) than estradiol (RBA = 100) for nuclear E receptor. The RBA of DES to nuclear E receptor was lowered significantly in the presence of rat serum (43 +/- 1) or human serum (52 +/- 7). Dilution of human serum resulted in a progressive increase in the RBA of DES which approached that observed in the absence of serum. Addition of purified human serum albumin mimicked the decrease in RBA of DES that was observed with serum. The IC50 of estradiol was not changed in the presence of either rat serum or albumin. These data show that DES possesses a greater affinity for nuclear E receptor than estradiol and that serum albumin can modulate DES binding to uterine E receptor.
D000818:Animals; D001667:Binding, Competitive; D001769:Blood; D002467:Cell Nucleus / Q000378:metabolism; D004054:Diethylstilbestrol / Q000378:metabolism*; D004958:Estradiol / Q000378:metabolism; D005260:Female; D006801:Humans; D051381:Rats; D011919:Rats, Inbred Strains; D011960:Receptors, Estrogen / Q000187:drug effects / Q000378:metabolism*; D012709:Serum Albumin / Q000494:pharmacology*; D012738:Sex Hormone-Binding Globulin / Q000378:metabolism; D014599:Uterus / Q000378:metabolism*
D011960:Receptors, Estrogen; D012709:Serum Albumin; D012738:Sex Hormone-Binding Globulin; D004958:Estradiol; D004054:Diethylstilbestrol