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- W2077763739 abstract "The naturally occurring pyranonaphthoquinone (PNQ) antibiotic lactoquinomycin and related aglycones were found to be selective inhibitors of the serine-threonine kinase AKT. A set of synthetic PNQs were prepared and a minimum active feature set and preliminary SAR were determined. PNQ lactones inhibit the proliferation of human tumor cell lines containing constitutively activated AKT and show expected effects on cellular biomarkers. Biochemical data are presented supporting a proposed bioreductive alkylation mechanism of action." @default.
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- W2077763739 date "2009-03-23" @default.
- W2077763739 modified "2023-10-16" @default.
- W2077763739 title "Pyranonaphthoquinone Lactones: A New Class of AKT Selective Kinase Inhibitors Alkylate a Regulatory Loop Cysteine" @default.
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- W2077763739 doi "https://doi.org/10.1021/jm900075g" @default.
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