Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: DrugBank:EXPT01586 (G418)
 2,237 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

This research ws carried out to construct a medicine screening system targeting at human promoter of CCR5. The gene Human promoter of CCR5 was inserted into the rebuilt vector pGL3-neo. The pGL3-neo-CCR5 plasmids were transfected into Jurkat cells (the cell line of acute T lymphocyte leukemia). The lasting transfected cells were screened by G418. After seven kinds of traditional Chinese medicine had acted separately on the lasting transfected cells for 16h, the expression levels of CCR5 promoter in the cells were detected. The results showed that the level of luciferase activity of Shuanghuanglian-injectio group was remarkably lower than that of control (P < 0.05), and the levels of luciferase activity of Chuanhuning group, Baical skullcap root group, and Milkvetch root group were remarkably higher than that of control (P < 0.01). Shuanghuanglian-injectio depressed the activity of the transfected CCR5 promoter in cells cultivated in vitro; Chuanhuning, Baical skullcap root and Milkvetch root boosted the activity of the transfected CCR5 promoter in cells cultivated in vitro. Thus a medicine screening system based on Human promoter of CCR5 was initially constructed.
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PMID:[Establishment and initial application of a medicine screening technique based on human promoter of CCR5]. 1994 86

Chemokine receptors belong to a superfamily of proteins that signal through coupled heterotrimeric G proteins. Chemokine receptor CCR5 is the major co-receptor essential for HIV entry into host cells, and now chemokine CCR5 receptor has become an important target in searching for anti-HIV drugs. Here, we describe the establishment of a human embryonic kidney (HEK) 293/CCR5-HA cell line stably expressing CCR5 receptor with influenza hemagglutinin (HA) tag at the N termini on the membrane surface of HEK293 cells. Plasmid pcDNA3.0-CCR5-HA was transfected into HEK293 cells, and monoclonal HEK293 cell lines expressing CCR5 receptor were generated under G418 selection. The expression of functional CCR5 receptor was tested by GTP?S assay, and the results showed about 5 monoclonal HEK293 cell lines expressed functional CCR5 receptor, and of which No.7 monoclonal cell line is the best. The FACS analysis results further confirmed that CCR5 receptor was positive in 96.89% of No.7 monoclonal HEK293/CCR5-HA cell line. Further results showed that RANTES significantly stimulated GTP?S binding in the dose-dependent manner, and CCR5 antagonist Sch-351125 inhibited RANTES stimulated GTP?S binding in the dose-dependent manner in No.7 monoclonal HEK293/CCR5-HA cell line. Our results suggest that the established HEK293/CCR5-HA cell line is suitable for highthroughput screening and is feasible to identify CCR5 receptor antagonists.
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PMID:Establishment of a new cell line for high-throughput evaluation of chemokine CCR5 receptor antagonists. 2249 60