PMID: 6984076Jan 1, 1981Paper

Effect of quinoline-type antimalarial drugs on the binding of oestradiol-17 beta and progesterone by rabbit and human uterine cytosols

Journal of Receptor Research
T A ScottW B Mujaji

Abstract

Rabbit and human uterine cytosol, prepared and tested in phosphate buffer, bound less oestradiol-17 beta or progesterone than cytosol from the same source prepared and tested in Tris-HCl buffer. Dissociation constants were the same in both buffer systems, and the difference in binding was due to a difference in the number of binding sites. Three quinoline-type antimalarial drugs, chloroquine, quinine and mefloquine, and the quinoline derivative, 4-(4'-hydroxy-1'-methylbutylamino)-7-chloroquinoline, increased the steroid binding capacity of phosphate-buffered cytosol to that of Tris-buffered cytosol, the optimal concentration of quinoline derivative being 1.4-1.6 mM. Tris (50 mM) increased the binding capacity of phosphate-buffered cytosol to that of Tris-buffered cytosol. The effects of Tris and quinoline derivatives were not additive. By gel chromatography and sucrose density gradient centrifugation it was shown that the molecular size and sedimentation behaviour of the oestradiol and progesterone receptors were not affected by the quinoline derivatives. Two types of binding site are proposed, one requiring the presence of low molecular weight, basic compounds. The uterine levels of chloroquine attained by normal pharmacologic...Continue Reading

References

May 1, 1977·Analytical Biochemistry·J J Sedmak, S E Grossberg
Jan 1, 1978·Cancer Chemotherapy and Pharmacology·J S MacdonaldP S Schein
Jun 1, 1979·Biochemical Society Transactions·J P RaynaudT Ojasoo
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Jan 15, 1974·Biochemistry·G C ChamnessW L McGuire

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Citations

Jan 1, 1988·Journal of Steroid Biochemistry·M Ayub, T A Scott

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