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16α,17α-Cycloalkane Derivatives of Progesterone Intensively Bind to a Rat Serum Protein

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Abstract

The interaction of 6α-methyl-[1,2-3H]16α,17α-cyclohexanoprogesterone with rat serum proteins has been studied. Specific binding of this ligand characterized by K d = 0.36 ± 0.10 μM and concentration of binding sites (Bmax) of about 1 μM (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 6α-methyl-16α,17α-cyclohexanoprogesterone by prolonging its retention in the bloodstream.

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Authors and Affiliations

  1. Laboratory of Endocrinology, School of Biology, Lomonosov Moscow State University, Moscow, 119899, Russia

    A. N. Smirnov & E. V. Pokrovskaya

  2. Group of Chemistry of Steroids and Oxylipines, Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Leninski pr. 47, Moscow, 117913, Russia

    I. S. Levina, L. E. Kulikova & A. V. Kamernitzky

  3. Laboratory of Isotope-Modified and Physiologically Active Compounds, Institute of Molecular Genetics, Russian Academy of Sciences, pl. Akademika Kurchatova 2, Moscow, 123182, Russia

    V. P. Shevchenko

Authors
  1. A. N. Smirnov
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  2. E. V. Pokrovskaya
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  3. I. S. Levina
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  4. L. E. Kulikova
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  5. A. V. Kamernitzky
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  6. V. P. Shevchenko
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Smirnov, A.N., Pokrovskaya, E.V., Levina, I.S. et al. 16α,17α-Cycloalkane Derivatives of Progesterone Intensively Bind to a Rat Serum Protein. Biochemistry (Moscow) 66, 688–692 (2001). https://doi.org/10.1023/A:1010219617134

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