Eicar (5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide). A novel potent inhibitor of inosinate dehydrogenase activity and guanylate biosynthesis.
作者： J Balzarini , A Karlsson , L Wang , C Bohman , K Horská
DOI: 10.1016/S0021-9258(19)74507-4
关键词:
摘要: EICAR (5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide) is a cytostatic agent that inhibits murine leukemia L1210 and human lymphocyte CEM cells at 50% inhibitory concentration of 0.80-1.4 microM, respectively. causes rapid marked inhibition inosinate (IMP) dehydrogenase (EC 1.1.1.205) activity in intact reflected by concentration-dependent accumulation IMP depletion GTP dGTP levels. 5'-monophosphate potent inhibitor purified cell (Ki/Km 0.06). Inhibition competitive with respect to IMP. were selected for resistance the action proved be adenosine kinase-deficient. Also, studies other mutant lines revealed kinase, as well an alternative pathway, may responsible conversion its 5'-monophosphate. Purified 2'-deoxycytidine 2'-deoxyguanosine cytosolic 5'-nucleotidase, nicotinamide dinucleotide (NAD) pyrophosphorylase do not seem markedly involved metabolism EICAR.
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