Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P51532 (transcriptional activator)
 6,546 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

This study describes the screening of a plant extract library for inhibitors of signal transduction pathways mediated by the cholecystokinin receptor, CCK1. CCK1 receptors are coupled to Galpha(q/11)-proteins, localized mainly in the gastrointestinal tract, and implicated in the regulation of various digestive functions. A primary screen was performed using a cell-based assay that used the beta-lactamase gene reporter controlled by the transcriptional activator NFAT. The assay was validated with the CCK1 receptor antagonist, lorglumide, and automated by the use of a liquid-handling robot MultiProbe II. Off-target hits were triaged by counterscreening against gene reporter cells activated by a combination of thapsigargin and phorbol ester. Purification of active compounds was guided by the beta-lactamase gene reporter and Ca2+ mobilization assays. Pure compounds were characterized by Ca2+ mobilization, radioligand binding, inositol-1 phosphate formation, and Eu-GTP binding assays. The selectivity of inhibition was tested against a panel of Galpha(q/11), Galpha(s), and Galpha(i/0)-coupled receptors. These studies led to the identification of a novel Galpha(q/11)-selective inhibitor.
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PMID:Screening a plant extract library for inhibitors of cholecystokinin receptor CCK1 pathways. 2046 Feb 49

A stable recombinant Atlantic Salmon Kidney cell line ASK for use as an inducible expression system was isolated, cloned and characterised. The cells were transfected with the pTet-Off plasmid from the Tet On/Off Clontech system, carrying a G418 resistance gene. Several G418-resistant clones were sub-cultured and characterised by qPCR and by transient transfection. The level of expression of transcriptional activator (tTA) was measured by qPCR in a number of isolated clones. Transient transfection with a pTRE2-hyg-LUC plasmid was used to evaluate the inducibility of these clones. Two clones were chosen for their compromise between cell growth and inducibility. This genetically engineered cell line is a valuable tool for the fish research community especially in research areas investigating the biological function of viral proteins.
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PMID:Establishment of an Atlantic salmon kidney cell line with an inducible gene expression system. 2164 Jul 69

We have isolated a stable recombinant cell line CHSE-TOF5 derived from the Chinook salmon (Oncorhynchus tshawytscha) embryo cells for use as an inducible expression system. The cells were transfected with the pTet-Off plasmid from the Tet On/Off Clontech system, carrying a G418 resistance gene. Several G418-resistant clones were subcultured and characterised by quantitative PCR (qPCR) and by transient transfection. The level of expression of transcriptional activator was measured by qPCR in a number of isolated clones, and transient transfection with a pTRE2-hyg-LUC plasmid was used to evaluate the inducibility of these clones. A clone was selected for its relative fast cell growth and good level of inducibility. This genetically engineered cell line is a valuable tool for the fish research community especially in research areas investigating the biological function of proteins from fish or fish pathogens.
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PMID:Establishment of a Chinook salmon cell line with an inducible gene expression system. 2208 98

The tetracycline-controlled Tet-Off and Tet-On gene expression systems are used to regulate the activity of genes in eukaryotic cells in diverse settings, varying from basic biological research to biotechnology and gene therapy applications. These systems are based on regulatory elements that control the activity of the tetracycline-resistance operon in bacteria. The Tet-Off system allows silencing of gene expression by administration of tetracycline (Tc) or tetracycline-derivatives like doxycycline (dox), whereas the Tet-On system allows activation of gene expression by dox. Since the initial design and construction of the original Tet-system, these bacterium-derived systems have been significantly improved for their function in eukaryotic cells. We here review how a dox-controlled HIV-1 variant was designed and used to greatly improve the activity and dox-sensitivity of the rtTA transcriptional activator component of the Tet-On system. These optimized rtTA variants require less dox for activation, which will reduce side effects and allow gene control in tissues where a relatively low dox level can be reached, such as the brain.
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PMID:Tet-On Systems For Doxycycline-inducible Gene Expression. 2721 14