Abstract

We present a live cell-based high throughput screening (HTS) system that enables the identification of compounds that have the ability to modify targeted metabolic pathways in pathogenic cells. In the assay, a specified “input” metabolite is added to the cell and changes in the “output” metabolite concentration, which represent changes in the targeted pathway, are recorded in situ using fluorescence detection. This metabolic pathway-oriented screening system was applied to glycolysis and amino acid metabolism, and it revealed novel activities of the current drugs, 6-BIO and regorafenib, that result in changes in the metabolic fates of tumor cells.

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