Article
Lucanthone and its derivative hycanthone inhibit apurinic endonuclease-1 (APE1) by direct protein binding.
PloS one - 1 Jan 2011
Naidu Mamta D, Agarwal Rakhi, Pena Louis A, Cunha Luis, Mezei Mihaly, Shen Min, Wilson David M, Liu Yuan, Sanchez Zina, Chaudhary Pankaj, Wilson Samuel H, Waring Michael J
Abstract excerpt
Lucanthone and hycanthone are thioxanthenone DNA intercalators used in the 1980s as antitumor agents. Lucanthone is in Phase I clinical trial, whereas hycanthone was pulled out of Phase II trials. Their potential mechanism of action includes DNA intercalation, inhibition of nucleic acid biosyntheses, and inhibition of enzymes like topoisomerases and the dual function base excision repair enzyme apurinic...
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