Interaction of glucocorticoid analogues with the human glucocorticoid receptor

Transient co-transfection of receptor cDNA and suitable reporter genes was used to study human glucocorticoid receptor (hGR) function in a neutral mammalian cell background. A variety of natural and synthetic steroids were analyzed for their ability to activate gene expression through the hGR and to...

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Veröffentlicht in:The Journal of steroid biochemistry and molecular biology 1992-03, Vol.41 (3), p.733-738
Hauptverfasser: Berger, Tina S., Parandoosh, Zahra, Perry, Bruce W., Stein, Robert B.
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container_issue 3
container_start_page 733
container_title The Journal of steroid biochemistry and molecular biology
container_volume 41
creator Berger, Tina S.
Parandoosh, Zahra
Perry, Bruce W.
Stein, Robert B.
description Transient co-transfection of receptor cDNA and suitable reporter genes was used to study human glucocorticoid receptor (hGR) function in a neutral mammalian cell background. A variety of natural and synthetic steroids were analyzed for their ability to activate gene expression through the hGR and to bind to extracts of cells expressing the hGR cDNA. There was very good correlation between these two in vitro parameters for these compounds. Furthermore, correlation of these data with reported in vivo anti-inflammatory potencies was surprisingly close, with two exceptions. The in vitro data suggest an explanation for the discrepant compounds, consistent with published data on their metabolic fate in vivo. The co-transfection assay has utility as a quantitative predictor of in vivo glucocorticoid pharmacology.
doi_str_mv 10.1016/0960-0760(92)90414-E
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source MEDLINE; ScienceDirect Journals (5 years ago - present)
subjects Animals
Binding, Competitive
Cell Line
DNA - genetics
Gene Expression Regulation - drug effects
Glucocorticoids - pharmacology
Humans
Receptors, Glucocorticoid - drug effects
Receptors, Glucocorticoid - genetics
Receptors, Glucocorticoid - metabolism
Structure-Activity Relationship
Transcriptional Activation
Transfection
title Interaction of glucocorticoid analogues with the human glucocorticoid receptor
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