T Yamaguchi, M Kawarai, Y Takeshita, F Ishikawa, M Saneyoshi
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引用次数: 3
摘要
端粒酶是一种逆转录酶，在真核细胞中合成端粒DNA。为了阐明端粒酶对碱基上带有疏水性基团的5'-三磷酸核苷的敏感性，我们使用定量“拉伸PCR”方法研究了2'，3'-二脱氧-5-苯基尿苷5'-三磷酸类似物和9-(β -d -阿拉伯糖基)-2-(对-正丁基苯基)嘌呤5'-三磷酸类似物对端粒酶活性的抑制作用。2'，3'-二脱氧-5-苯基尿嘧啶5'-三磷酸(StddUTP)比2'，3'-二脱氧胸腺嘧啶5'-三磷酸(ddTTP)具有更强的抑制作用。另一方面，9-(β - d -阿拉伯糖基)-2-(对正丁基苯基)鸟嘌呤5'-三磷酸(BuParaGTP)没有抑制作用，尽管9-(β - d -阿拉伯糖基)鸟嘌呤5'-三磷酸(araGTP)是端粒酶的有效抑制剂。描述了核苷酸碱基上疏水取代基对端粒酶的影响。
Inhibition of human telomerase by nucleotide analogues bearing a hydrophobic group.
Telomerase, which synthesizes telomeric DNA in eukaryotic cells, is classified as a reverse transcriptase. To clarify the susceptibility of telomerase to nucleoside 5'-triphosphates bearing a hydrophobic group on the base moiety, we studied the inhibitory effects of 2',3'-dideoxy-5-styryluridine 5'-triphosphate analogues and 9-(beta-D-arabinofuranosyl)-2-(p-n-butylanilino)purine 5'-triphosphate analogues on telomerase activity using a quantitative 'stretch PCR' assay. 2',3'-Dideoxy-5-styryluridine 5'-triphosphate (StddUTP) showed more potent inhibition than 2',3'-dideoxythymidine 5'-triphosphate (ddTTP). On the other hand, 9-(beta-D-arabinofuranosyl)-2-(p-n-butylphenyl)guanine 5'-triphosphate (BuParaGTP) showed no inhibition, even though 9-(beta-D-arabinofuranosyl)guanine 5'-triphosphate (araGTP) is a potent inhibitor of telomerase. The influence on telomerase of hydrophobic substituents on the base moieties of nucleotides is described.
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