氟阿糖腺苷单磷酸是胞质5'-核苷酸酶II（cN-II）的底物：酶促去磷酸化的高效液相色谱和核磁共振研究。
F-ara-AMP is a substrate of cytoplasmic 5'-nucleotidase II (cN-II): HPLC and NMR studies of enzymatic dephosphorylation.
作者信息
Jordheim Lars P, Cros Emeline, Galmarini Carlos M, Dumontet Charles, Bretonnet Anne-Sophie, Krimm Isabelle, Lancelin Jean-Marc, Gagnieu Marie-Claude
机构信息
INSERM U590, Laboratoire de Cytologie Analytique, Faculté de Médecine Rockefeller, Université Claude Bernard Lyon I, Lyon, France.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2006 Mar;25(3):289-97. doi: 10.1080/15257770500458027.
Intracellular accumulation of triphosphorylated derivatives is essential for the cytotoxic activity of nucleoside analogues. Different mechanisms opposing this accumulation have been described. We have investigated the dephosphorylation of monophosphorylated fludarabine (F-ara-AMP) by the purified cytoplasmic 5'-nucleotidase cN-II using HPLC and NMR. These studies clearly showed that cN-II was able to convert F-ara-AMP into its non phosphorylated form, F-ara-A, with a Km in the millimolar range and Vmax = 35 nmol/min/mg, with both methods. Cytoplasmic 5'-nucleotidase cN-II can degrade this clinically useful cytotoxic nucleoside analogue and its overexpression is thus likely to be involved in resistance to this compound.
三磷酸化衍生物的细胞内积累对于核苷类似物的细胞毒性活性至关重要。已经描述了多种对抗这种积累的机制。我们使用高效液相色谱法（HPLC）和核磁共振（NMR）研究了纯化的细胞质5'-核苷酸酶cN-II对单磷酸氟达拉滨（F-ara-AMP）的去磷酸化作用。这些研究清楚地表明，cN-II能够将F-ara-AMP转化为其非磷酸化形式F-ara-A，两种方法测得的米氏常数（Km）在毫摩尔范围内，最大反应速度（Vmax）= 35 nmol/分钟/毫克。细胞质5'-核苷酸酶cN-II可以降解这种临床上有用的细胞毒性核苷类似物，因此其过表达可能与对该化合物的耐药性有关。
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