Competitive inhibition of (TH)dexamethasone binding to mammary glucocorticoid receptor by leupeptin
The inhibitory effect of leupeptin on (TH)dexamethasone binding to the glucocorticoid receptor from lactating goat mammary cytosol has been studied. Leupeptin (10 mM) caused a significant (about 35%) inhibition of (TH)dexamethasone binding to glucocorticoid receptor. Binding inhibition is further increased following filtration of unlabeled cytosolic receptor through a Bio-Gel A 0.5-m column. Binding inhibition was partially reversed by monothioglycerol at 10 mM concentration. A double reciprocal plot revealed that leupeptin appears to be a competitive inhibitor of (TH)dexamethasone binding to the glucocorticoid receptor. Low salt sucrose density gradient centrifugation revealed that the leupeptin-treated sample formed a slightly larger (approximately 9 S) receptor complex (leupeptin-free complex sediments at 8 S).
- Research Organization:
- Univ. of Southern California, Los Angeles
- OSTI ID:
- 6358757
- Journal Information:
- Proc. Soc. Exp. Biol. Med.; (United States), Vol. 184:3
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
DEXAMETHASONE
BIOCHEMICAL REACTION KINETICS
ENZYME INHIBITORS
BIOLOGICAL EFFECTS
COMPLEXES
GOATS
INHIBITION
MAMMARY GLANDS
RECEPTORS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ADRENAL HORMONES
ANIMALS
BODY
CORTICOSTEROIDS
DOMESTIC ANIMALS
GLANDS
GLUCOCORTICOIDS
HORMONES
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
KETONES
KINETICS
LABELLED COMPOUNDS
MAMMALS
ORGANIC COMPOUNDS
ORGANS
PREGNANES
REACTION KINETICS
RUMINANTS
STEROID HORMONES
STEROIDS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques