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Unusual estrogen-binding liver protein: additional data on the structural determinants of androgenic ligands

Journal Article · · Biochemistry (Engl. Transl.); (United States)
OSTI ID:5856532
; ;
The relative competitive activity of a number of androstane derivatives was determined according to the 50% displacement of (/sup 3/H) estradiol from complexes with an unusual estrogen-binding protein (UEBP) of the liver of male rats. It was shown that: (1) the bulk of the energy of the bond of the steroid to protein is due to hydrophobic interactions; (2) the real ability to form specific complexes with the UEBP at androgen concentrations close to the physiological is determined by the 17..beta..-hydroxyl and is enhanced by the 3..cap alpha..- or 2..cap alpha..-hydroxy group; (3) the 3- and 17-keto groups weaken the interaction of androgens with the UEBP; (4) cis-coupling of the A and B rings in the molecule of androgens does not prevent the binding of the steroids to protein. These data substantially refine the concepts of the mechanisms of the interaction of androgens with the UEBP and may promote an elucidation of the physiological function of this protein.
Research Organization:
M.V. Lomonosov Moscow State Univ., USSR
OSTI ID:
5856532
Journal Information:
Biochemistry (Engl. Transl.); (United States), Journal Name: Biochemistry (Engl. Transl.); (United States) Vol. 51:5; ISSN BIORA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANDROGENS
ANDROSTANES
ANIMALS
BINDING ENERGY
BIOCHEMISTRY
BIOLOGICAL FUNCTIONS
BODY
CHEMICAL BONDS
CHEMISTRY
COMPLEXOMETRY
DIGESTIVE SYSTEM
ENERGY
ESTRADIOL
ESTRANES
ESTROGENS
FUNCTIONS
GLANDS
HORMONES
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
LABELLING
LIGANDS
LIVER
MAMMALS
MEMBRANE PROTEINS
METABOLISM
ORGANIC COMPOUNDS
ORGANS
PROTEINS
RADIORECEPTOR ASSAY
RATS
RECEPTORS
RODENTS
STEROID HORMONES
STEROIDS
STRUCTURAL CHEMICAL ANALYSIS
STRUCTURE-ACTIVITY RELATIONSHIPS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES