Izuta S, Saneyoshi M
Nucleic Acids Symp Ser. 1984(15):73-6.
Starting from 1-beta-D-arabinofuranosyluracil, several 5-substituted derivatives were synthesized via 5-mercuri intermediate. The resulting nucleosides were converted into their corresponding 5'-triphosphates and examined for their inhibitory effects on DNA-dependent DNA polymerases alpha and beta from developing cherry salmon (Oncorhynchus masou) testes. The following results were obtained. All the compounds tested showed remarkable inhibitory effects on DNA polymerase alpha, but lesser extent on DNA polymerase beta. The inhibitory action of the hydrophobic 5-substituents against DNA polymerase alpha was stronger than against DNA polymerase beta. For example, Ki/Ki of 5-(E)-3-amino-styryl-Ara UTP is 0.32 and Ki/Km for pol alpha/Ki/Km for pol beta is 0.19. For that reason, we chose this compound as a candidate for a ligand which is applicable to selective affinity chromatography for DNA polymerase alpha.
从1-β-D-阿拉伯呋喃糖基尿嘧啶出发，通过5-汞中间体合成了几种5-取代衍生物。将所得核苷转化为其相应的5'-三磷酸酯，并检测它们对发育中的樱鳟（Oncorhynchus masou）睾丸中依赖DNA的DNA聚合酶α和β的抑制作用。得到以下结果。所有测试化合物对DNA聚合酶α均表现出显著的抑制作用，但对DNA聚合酶β的抑制作用较小。疏水性5-取代基对DNA聚合酶α的抑制作用强于对DNA聚合酶β的抑制作用。例如，5-(E)-3-氨基苯乙烯基-Ara UTP的Ki/Ki为0.32，pol α的Ki/Km与pol β的Ki/Km之比为0.19。因此，我们选择该化合物作为适用于DNA聚合酶α选择性亲和色谱的配体候选物。
