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

|View full text |Cite

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.

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2001

2005

Publication Types

Select...

Article5

Relationship

Self Cite0

Independent5

Authors

Journals

Cited by 6 publications

References 5 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

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

2005

Russ J Bioorg Chem

View full text Add to dashboard Cite

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.

show abstract

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

2005

Russ J Bioorg Chem

View full text Add to dashboard Cite

show abstract

DNA slows dissociation of progesterone receptor–steroid ligand complexes

et al. 2003

View full text Add to dashboard Cite

Untitled

Смирнов

Pokrovskaya

Левина

et al. 2001

Biochemistry (Moscow)

View full text Add to dashboard Cite

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.

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

hi@scite.ai

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

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

Untitled

Contact Info

Product

Resources

About