Synthetic protease substrate n-benzoyl-L-argininyl-p-nitroanilide activates specific binding of (/sup 3/H)estradiol to a protein in rat pancreas: relationship of structure to activity
N-benzoyl-L-argininyl-p-nitroanilide (BAN), a synthetic substrate for trypsin-like proteolytic enzymes, is a potent activator of (/sup 3/H)estradiol-binding to a protein present in rat pancreas. When partially purified, this protein is almost devoid of (/sup 3/H)estradiol-binding activity in the absence of an endogenous accessory factor. BAN can mimic the natural coligand in this steroid binding reaction. The effect of BAN is specific since a number of derivatives of this substance are inactive or may even inhibit steroid binding. It is unlikely that BAN exerts this stimulatory action indirectly, possibly by preventing proteolytic inactivation of the (/sup 3/H)estradiol-binding protein, since preincubation of the protein in the absence of BAN resulted neither in reduced rate, nor extent, of steroid binding following BAN addition. Also, a number of protease inhibitors had no effect on the binding reaction. Of those inhibitors tested, only antipain significantly enhanced binding of (/sup 3/H)estradiol, but only about 20 percent as effectively as BAN. 13 references, 1 figure, 2 tables.
- Research Organization:
- New York Univ. Medical Center, NY
- OSTI ID:
- 6168723
- Journal Information:
- Life Sci.; (United States), Vol. 35:22
- Country of Publication:
- United States
- Language:
- English
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ESTRADIOL
BIOCHEMICAL REACTION KINETICS
SUBSTRATES
BIOLOGICAL EFFECTS
CHEMICAL BONDS
ENZYME INHIBITORS
ENZYMES
ORGANIC NITROGEN COMPOUNDS
PANCREAS
PROTEINS
RATS
STRUCTURE-ACTIVITY RELATIONSHIPS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMALS
BODY
DIGESTIVE SYSTEM
ENDOCRINE GLANDS
ESTRANES
ESTROGENS
GLANDS
HORMONES
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
ORGANIC COMPOUNDS
ORGANS
REACTION KINETICS
RODENTS
STEROID HORMONES
STEROIDS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques