Kupfer D, Bulger W H
Res Commun Chem Pathol Pharmacol. 1977 Mar;16(3):451-62.
The in vitro effect of o, p'DDT on the binding of 3H-estradiol-17beta (3H-E2) to the high affinity estrogen-binding protein(EBP) in cytosol derived from human mammary and uterine tumors was examined. o,p'DDT inhibited the binding of 3H-E2 to EBP in both breast and uterine tumors. Using Scatchard and Linweaver-Burk plot analyses, the inhibition by o,p'DDT of 3H-E2 binding to mammary tumors EBP appears to result from competition for the 8S moiety binding sites and not from deactivation of the binding sites. The KI for the inhibition by o,p.'DDT with EI binding was determined, yielding a value of 0.5 +/- 0.1 muM. The possible relevance of these findings to human population exposed to DDT derivatives is discussed.
研究了邻,对滴滴涕(o,p'DDT)对从人乳腺和子宫肿瘤中提取的胞质溶胶中高亲和力雌激素结合蛋白(EBP)与3H-雌二醇-17β(3H-E2)结合的体外作用。o,p'DDT抑制了3H-E2与乳腺和子宫肿瘤中EBP的结合。通过Scatchard和Linweaver-Burk作图分析,o,p'DDT对3H-E2与乳腺肿瘤EBP结合的抑制作用似乎是由于对8S部分结合位点的竞争,而不是结合位点的失活。测定了o,p'DDT对EI结合抑制的抑制常数(KI),得出的值为0.5±0.1μM。讨论了这些发现与接触DDT衍生物的人群的可能相关性。