Saneyoshi M, Tohyama J, Nakayama C, Takiya S, Iwabuchi M
Nucleic Acids Res. 1981 Jul 10;9(13):3129-38. doi: 10.1093/nar/9.13.3129.
3'-Deoxycytidine 5'-triphosphate and 3'-deoxyuridine 5'-triphosphate were synthesized starting from cordycepin in good yield. The inhibitory effects of these nucleotides were examined in comparison with that of cordycepin 5'-triphosphate (3'-dATP) using purified DNA-dependent RNA polymerases I and II from Dictyostelium discoideum cells. Both nucleotide analogues strongly and competitively inhibited the incorporations of CTP and UTP into RNA by the RNA polymerases. The Km and Ki values for CTP and 3'-dCTP were 6.3 micro M and 3.0 micro M, respectively, and those for UTP and 3'-dUTP were 6.3 micro M and 2.0 micro M, respectively. These two analogues will be useful in studies at the molecular level on the relationship of template and substrate in RNA synthesis with chromatin, isolated nuclei or permeable cells, because they do not have any effect on poly (rA) synthesis.
以虫草素为原料,高产率合成了3'-脱氧胞苷5'-三磷酸和3'-脱氧尿苷5'-三磷酸。使用从盘基网柄菌细胞中纯化的依赖DNA的RNA聚合酶I和II,将这些核苷酸的抑制作用与虫草素5'-三磷酸(3'-dATP)的抑制作用进行了比较。这两种核苷酸类似物均强烈且竞争性地抑制RNA聚合酶将CTP和UTP掺入RNA中。CTP和3'-dCTP的Km和Ki值分别为6.3微摩尔和3.0微摩尔,UTP和3'-dUTP的Km和Ki值分别为6.3微摩尔和2.0微摩尔。这两种类似物在研究RNA与染色质、分离的细胞核或可渗透细胞合成过程中模板与底物之间的分子水平关系时将很有用,因为它们对聚(rA)合成没有任何影响。