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Influence of calf serum on glucocorticoid-responses of certain progesterone derivatives

The following in vitro glucocorticoid (GC) parameters of progesterone (P), 1-ene progesterone (ΔP), 11 β-hydroxyprogesterone (HOP), 11 β-1-ene progesterone (ΔHOP) and dexamethasone (Dexa) were assayed in the presence or absence of bovine calf serum (BCS): binding to thymus cytosol, dissociation of t...

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Published in:The Journal of steroid biochemistry and molecular biology 1998-08, Vol.66 (4), p.211-216
Main Authors: Vicent, G.P., Burton, G., Ghini, A., Lantos, C.P., Galigniana, M.D.
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cited_by cdi_FETCH-LOGICAL-c389t-ed65408f6f734217e8ec904efba6a7bade29dfff76abe97e1740efcabc4de77f3
cites cdi_FETCH-LOGICAL-c389t-ed65408f6f734217e8ec904efba6a7bade29dfff76abe97e1740efcabc4de77f3
container_end_page 216
container_issue 4
container_start_page 211
container_title The Journal of steroid biochemistry and molecular biology
container_volume 66
creator Vicent, G.P.
Burton, G.
Ghini, A.
Lantos, C.P.
Galigniana, M.D.
description The following in vitro glucocorticoid (GC) parameters of progesterone (P), 1-ene progesterone (ΔP), 11 β-hydroxyprogesterone (HOP), 11 β-1-ene progesterone (ΔHOP) and dexamethasone (Dexa) were assayed in the presence or absence of bovine calf serum (BCS): binding to thymus cytosol, dissociation of the glucocorticoid receptor (GR)–heat shock protein 9O (hsp90) complex (diss.), tyrosine aminotransferase (TAT) induction in hepatocytes and the inhibition of 3H-uridine and 35S-methionine uptake by thymocytes. Without BCS, steroids were in most cases active in this general order: Dex>ΔHOP>HOP>ΔP>P. BCS abolished all activities in P and ΔP, but left them unaltered in all other steroids, except diss. in HOP, which diminished intermediately. Binding of P, ΔP, HOP and ΔHOP to GR and CBG paralleled their in vivo activating effects on glycogen deposition. Conclusions: in this steroid series, BCS, but not CBG, inhibits GC responses of P and ΔP. 11- β hydroxylation frees those molecules from the inhibitory effects of BCS.
doi_str_mv 10.1016/S0960-0760(98)00040-5
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subjects Adrenalectomy
Animals
Biological and medical sciences
Blood
Cattle
Cell physiology
Cells, Cultured
Corticosterone - metabolism
Cytosol - metabolism
Dexamethasone - pharmacology
Enzyme Induction
Fundamental and applied biological sciences. Psychology
Hormonal regulation
HSP90 Heat-Shock Proteins - metabolism
Liver - drug effects
Liver - enzymology
Liver - metabolism
Liver Glycogen - biosynthesis
Male
Methionine - metabolism
Mice
Mice, Inbred BALB C
Molecular and cellular biology
Progesterone - analogs & derivatives
Progesterone - pharmacology
Rats
Rats, Sprague-Dawley
Receptors, Glucocorticoid - metabolism
Structure-Activity Relationship
Thymus Gland - drug effects
Thymus Gland - metabolism
Transcortin - metabolism
Tyrosine Transaminase - biosynthesis
Uridine - metabolism
title Influence of calf serum on glucocorticoid-responses of certain progesterone derivatives
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