Document Detail


Genetic recombination as a reporter for screening steroid receptor agonists and antagonists.
MedLine Citation:
PMID:  9527854     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Reporter cell lines are often used for high throughput screening of chemical libraries to identify new receptor ligands. Here we show how Cre recombinase can be used in mammalian cells to screen for steroid receptor ligands. A translational fusion of Cre recombinase and the ligand binding domain of the human glucocorticoid receptor was transfected into mammalian cells with a loxP/luciferase reporter gene. The recombinase function of the fusion is dependent on ligand binding to the receptor, and Cre-mediated recombination results in constitutive expression of luciferase from the reporter gene. A stable transfected clone was isolated and used to characterize the kinetics, ligand specificity, and dose response to various receptor ligands. The Cre fusion system, unlike a transcriptional reporter using the mouse mammary tumor virus promoter, can detect binding of the receptor antagonist RU486. We also studied the Cre reporter in a sensitive, miniaturized, assay format using an 864-well plate and show that as few as 560 cells per assay well was sufficient to measure a dose response to ligand.
Authors:
J M Dias; N F Go; C P Hart; L C Mattheakis
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Analytical biochemistry     Volume:  258     ISSN:  0003-2697     ISO Abbreviation:  Anal. Biochem.     Publication Date:  1998 Apr 
Date Detail:
Created Date:  1998-04-28     Completed Date:  1998-04-28     Revised Date:  2006-08-24    
Medline Journal Info:
Nlm Unique ID:  0370535     Medline TA:  Anal Biochem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  96-102     Citation Subset:  IM    
Copyright Information:
Copyright 1998 Academic Press.
Affiliation:
Affymax Research Institute, 4001 Miranda Avenue, Palo Alto, California 94304, USA.
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MeSH Terms
Descriptor/Qualifier:
Amino Acid Sequence
Animals
Base Sequence
CHO Cells
Cricetinae
DNA, Recombinant / genetics
Genes, Reporter*
Hormone Antagonists / metabolism
Humans
Integrases / genetics
Kinetics
Ligands
Luciferases / genetics
Mice
Mifepristone / metabolism
Molecular Sequence Data
Plasmids / genetics
Receptors, Glucocorticoid / genetics,  metabolism
Receptors, Steroid / agonists*,  antagonists & inhibitors*
Recombination, Genetic*
Transfection
Viral Proteins*
Chemical
Reg. No./Substance:
0/DNA, Recombinant; 0/Hormone Antagonists; 0/Ligands; 0/Receptors, Glucocorticoid; 0/Receptors, Steroid; 0/Viral Proteins; 84371-65-3/Mifepristone; EC 1.13.12.-/Luciferases; EC 2.7.7.-/Cre recombinase; EC 2.7.7.-/Integrases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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