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 |
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container_title | The Journal of steroid biochemistry and molecular biology |
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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 |
format | Article |
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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
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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.</description><subject>Animals</subject><subject>Binding, Competitive</subject><subject>Cell Line</subject><subject>DNA - genetics</subject><subject>Gene Expression Regulation - drug effects</subject><subject>Glucocorticoids - pharmacology</subject><subject>Humans</subject><subject>Receptors, Glucocorticoid - drug effects</subject><subject>Receptors, Glucocorticoid - genetics</subject><subject>Receptors, Glucocorticoid - metabolism</subject><subject>Structure-Activity Relationship</subject><subject>Transcriptional Activation</subject><subject>Transfection</subject><issn>0960-0760</issn><issn>1879-1220</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1992</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kM9LwzAUx4Moc07_A4WeRA_VvDRpm4sgY-pg6EXPIU3TLdI1M0kV_3szOxQ8eHqH74_33gehU8BXgCG_xjzHKS5yfMHJJccUaDrbQ2MoC54CIXgfjX8sh-jI-1eMcZZBMUIjYDlhtBijx3kXtJMqGNsltkmWba-ssi4YZU2dyE62dtlrn3yYsErCSierfi27vz6nld4E647RQSNbr092c4Je7mbP04d08XQ_n94uUpWxIqQlVFVRQ9bkkANTjGU1o7XKCeel4gQkpqWsYidQyKiWjMdjIeMAGOcQgxN0PvRunH2L5wWxNl7ptpWdtr0XBSk5xSSLRjoYlbPeO92IjTNr6T4FYLHFKLaMxJaR4ER8YxSzGDvb9ffVWte_oYFb1G8GXccn3412wiujO6VrE1EEUVvz_4IvUdOBRA</recordid><startdate>19920301</startdate><enddate>19920301</enddate><creator>Berger, Tina S.</creator><creator>Parandoosh, Zahra</creator><creator>Perry, Bruce W.</creator><creator>Stein, Robert B.</creator><general>Elsevier Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19920301</creationdate><title>Interaction of glucocorticoid analogues with the human glucocorticoid receptor</title><author>Berger, Tina S. ; Parandoosh, Zahra ; Perry, Bruce W. ; Stein, Robert B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c357t-81bb7d13f61615c553d54dc62998c921a048abece14134ea59547139110061d13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1992</creationdate><topic>Animals</topic><topic>Binding, Competitive</topic><topic>Cell Line</topic><topic>DNA - genetics</topic><topic>Gene Expression Regulation - drug effects</topic><topic>Glucocorticoids - pharmacology</topic><topic>Humans</topic><topic>Receptors, Glucocorticoid - drug effects</topic><topic>Receptors, Glucocorticoid - genetics</topic><topic>Receptors, Glucocorticoid - metabolism</topic><topic>Structure-Activity Relationship</topic><topic>Transcriptional Activation</topic><topic>Transfection</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Berger, Tina S.</creatorcontrib><creatorcontrib>Parandoosh, Zahra</creatorcontrib><creatorcontrib>Perry, Bruce W.</creatorcontrib><creatorcontrib>Stein, Robert B.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>The Journal of steroid biochemistry and molecular biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Berger, Tina S.</au><au>Parandoosh, Zahra</au><au>Perry, Bruce W.</au><au>Stein, Robert B.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Interaction of glucocorticoid analogues with the human glucocorticoid receptor</atitle><jtitle>The Journal of steroid biochemistry and molecular biology</jtitle><addtitle>J Steroid Biochem Mol Biol</addtitle><date>1992-03-01</date><risdate>1992</risdate><volume>41</volume><issue>3</issue><spage>733</spage><epage>738</epage><pages>733-738</pages><issn>0960-0760</issn><eissn>1879-1220</eissn><abstract>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
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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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