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Antimicrob Agents Chemother ; 60(1): 640-5, 2016 01.
Article in English | MEDLINE | ID: mdl-26503663

ABSTRACT

Here we describe the development and validation of an intracellular high-throughput screening assay for finding new antituberculosis compounds active in human macrophages. The assay consists of a luciferase-based primary identification assay, followed by a green fluorescent protein-based secondary profiling assay. Standard tuberculosis drugs and 158 previously recognized active antimycobacterial compounds were used to evaluate assay robustness. Data show that the assay developed is a short and valuable tool for the discovery of new antimycobacterial compounds.


Subject(s)
Antitubercular Agents/pharmacology , High-Throughput Screening Assays , Macrophages/drug effects , Mycobacterium tuberculosis/drug effects , Antitubercular Agents/chemistry , Cell Line , Gene Expression , Genes, Reporter , Green Fluorescent Proteins/genetics , Green Fluorescent Proteins/metabolism , Hep G2 Cells , Humans , Luciferases/genetics , Luciferases/metabolism , Macrophages/microbiology , Microbial Sensitivity Tests , Mycobacterium tuberculosis/growth & development , Structure-Activity Relationship
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