The development of new anti-cancer therapeutic agents is necessary to
improve antitumor efficacy and reduce toxicities. Here we report using a systematic
anticancer drug screening approach we developed previously, to concurrently screen
colon and glioma cancer cell lines for 2000 compounds with known bioactivity and
1920 compounds with unknown activity. The hits specific to each tumor cell line were
then selected, and further tested with the same cells transfected with EGFP (Enhanced Green Fluorescent Protein) alone.
By comparing the percentage of signal reduction from the same cells transfected with the sensor-conjugated reporter
system; hits preferably causing apoptosis were identified. Among the known lead compounds, many cardiac glycosides
used as cardiotonic drugs were found to effectively and specifically kill colon cancer cells, while statins (hypolipidemic
agents) used as cholesterol lowering drugs were relatively more effective in killing glioma cells.
Keywords: Drug discovery, colorectal cancer, glioma; carditonic, HTS, statins.
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