斑蝥素
化学
部分
戒指(化学)
立体化学
庚烷
磷酸酶
蛋白磷酸酶2
生物化学
有机化学
酶
作者
Adam McCluskey,Mirella A. Keane,Lisa-Maree Mudgee,Alistair T. R. Sim,Jennette A. Sakoff,Ronald J. Quinn
标识
DOI:10.1016/s0223-5234(00)00186-0
摘要
A series of anhydride modified cantharidin analogues have been synthesised and screened for their ability to inhibit protein phosphatase 2A. Surprisingly only analogues capable of undergoing a facile ring opening of the anhydride moiety displayed any significant inhibition. Subsequent NMR experiments indicated that 7-oxobicyclo[2.2.1]heptane-2,3-dicarboxylic acid was the major (sole) species under assay conditions. The ability of these modified anhydro-cantharidin analogues to inhibit protein phosphatase 2A varies from 4 (16) to 100% (8) at 100 microM test concentration.
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