Anti-Inflammatory Drug Spawns Potent Anticancer Drug
By Biotechdaily staff writers
Posted on 19 Jul 2004
Researchers have transformed an anti-inflammatory agent with mild antitumor properties into a potent anticancer drug that triggers apoptosis in treated cancer cells.Posted on 19 Jul 2004
Investigators at Ohio State University (Columbus, USA) employed structure-activity analysis together with molecular modeling to generate derivatives of the cyclo-oxygenase 2 (COX-2) inhibitor celecoxib that were effective in inhibiting 3-phosphoinositide-dependent kinase-1 (PDK-1 kinase) activity. Two compounds were generated, OSU-03012 and OSU-03013, that were each 10 times more potent than celecoxib in inducing cancer cell death. These findings were reported in the June 15, 2004, issue of Cancer Research.
"This new agent works by inhibiting a fundamental signaling point in cancer cells, making it potentially effective in a wide range of cancer types,” said senior author Dr. Ching-Shih Chen, professor of pharmacy at Ohio State University. "We also have evidence that it may sensitize leukemia, and breast and lung cancers to conventional chemotherapy.”
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