The Synthesis of Tritium-Labeled 16α,17α-Cyclohex-3′-eno-progesterone as Probe for the Study of Steroid–Receptor Binding

Шевченко, В. П.; Nagaev, I. Yu.; Myasoedov, N. F.; Kamernitsky, A. V.; Левина, И. С.; Куликова, Л. Е.; Pokrovskaya, E. V.; Shchelkunova, T. A.; Смирнов, А. Н.

doi:10.1006/bioo.1999.1128

Bioorganic Chemistry

1999

DOI: 10.1006/bioo.1999.1128

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The Synthesis of Tritium-Labeled 16α,17α-Cyclohex-3′-eno-progesterone as Probe for the Study of Steroid–Receptor Binding

В. П. Шевченко

I. Yu. Nagaev

N. F. Myasoedov

et al.

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Cited by 6 publications

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Pregna-D′-pentaranes, progestins and antiprogestins: I. Separation of biological functions of steroid hormones

2005

Russ J Bioorg Chem

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The synthesis, modification, structure, and biological activity in vivo of the 16 α ,17 α -cycloalkanoprogesterone (pregna-D'-pentarane) analogues of progesterone are described. A possibility of separation of their biological functions has been demonstrated. A systematic synthesis of a set of uniform compounds that differ in a limited number of alterable parameters was developed. It resulted in an instrument useful for the investigation of pathways and mechanisms by which the steroid hormones fulfill their biological functions and for the probable discovery of new functions masked by the wide effects of native compounds.

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Pregna-D′-pentaranes, progestins and antiprogestins: I. Separation of biological functions of steroid hormones

2005

Russ J Bioorg Chem

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DNA slows dissociation of progesterone receptor–steroid ligand complexes

et al. 2003

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Смирнов

Pokrovskaya

Левина

et al. 2001

Biochemistry (Moscow)

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The interaction of 6alpha-methyl-[1,2-3H]16alpha,17alpha-cyclohexanoprogesterone with rat serum proteins has been studied. Specific binding of this ligand characterized by Kd = 0.36 +/- 0.10 microM and concentration of binding sites (Bmax) of about 1 microM (27.8 +/- 12.5 pmol/mg total protein) was found. According to competitive analysis, the affinity of the studied progestins to a protein that differs from transcortin was to some extent correlated with their hydrophobicity. The dissociation kinetics of 3H-ligand-protein complexes were biphasic, the binding sites forming stable and labile complexes with 3H-ligand being eluted in the same region during ion-exchange chromatography. In overall properties, the serum protein differs from the progesterone receptor and the pregna-D'-pentarane-specific protein from rat uterus. It is suggested that the revealed protein may provide high progestagenic activity of 6alpha-methyl-16alpha,17alpha-cyclohexanoprogesterone by prolonging its retention in the bloodstream.

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The Synthesis of Tritium-Labeled 16α,17α-Cyclohex-3′-eno-progesterone as Probe for the Study of Steroid–Receptor Binding

Cited by 6 publications

References 5 publications

Pregna-D′-pentaranes, progestins and antiprogestins: I. Separation of biological functions of steroid hormones

Pregna-D′-pentaranes, progestins and antiprogestins: I. Separation of biological functions of steroid hormones

DNA slows dissociation of progesterone receptor–steroid ligand complexes

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