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Cantharidin

Although the mode of action was unknown at the time, an inhibitor of PP1-PP6 actually represent one of the oldest treatments for cancer in recorded history. Writings dating back over 2,000 years describe the use of a concoction, "Mylabris", that is produced from the dried body of the Chinese blister beetle (Mylabris phalerata or Mylabris cichorii) for the treatment of both cancer and warts (Wang et al. 1989). The active constituent of Mylabris is exo, exo-2,3-di-methyl-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid anhydride, which is commonly referred to as cantharidin (Fig. 2). Cantharidin is a natural vesicant produced by as many as 1,500 different species of beetles belonging to the order Coleoptera, which produce it as a mechanism for defense.

Fig. 2A-D Structures of natural products with inhibitory activity against PP1, PP2A, PP4, PP5, and PP6. A Cantharidin (exo, exo-2,3-dimethyl-7-oxabicyclo[2.2.1]heptane-2,3-di-carboxylic acid anhydride). B Fostriecin {2H-pyran-2-one, 5, 6-dihydro-6-[3,6,13-trihy-droxy-3-methyl-4-(phosphonooxy)-1,7,9,11-tridecatetraenyl]}. C Okadaic acid. D Micro-cystin-LR

Fig. 2A-D Structures of natural products with inhibitory activity against PP1, PP2A, PP4, PP5, and PP6. A Cantharidin (exo, exo-2,3-dimethyl-7-oxabicyclo[2.2.1]heptane-2,3-di-carboxylic acid anhydride). B Fostriecin {2H-pyran-2-one, 5, 6-dihydro-6-[3,6,13-trihy-droxy-3-methyl-4-(phosphonooxy)-1,7,9,11-tridecatetraenyl]}. C Okadaic acid. D Micro-cystin-LR

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