Combinatorial Chemistry & High Throughput Screening

Rathnam Chaguturu 
iDDPartners, 3 Edith Court
Princeton Junction
NJ 08550
USA

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High Throughput Screening for Colorectal Cancer Specific Compounds

Author(s): Jingping Xie, Chunxia Wang, John C. Gore.

Abstract:

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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Article Details

VOLUME: 19
ISSUE: 3
Year: 2016
Page: [180 - 188]
Pages: 9
DOI: 10.2174/1386207319666160202120928
Price: $58