2'-脱氧-2'-氟尿苷-5'-磷酸：大肠杆菌K12胸苷酸合成酶的一种替代底物。
2'-Deoxy-2'-fluorouridine-5'-phosphate: an alternative substrate for thymidylate synthetase from Escherichia coli K12.
作者信息
Wohlrab F, Haertlé T, Trichtinger T, Guschlbauer W
出版信息
Nucleic Acids Res. 1978 Dec;5(12):4753-9. doi: 10.1093/nar/5.12.4753.
Abstract
The substrate specificity of 2'-deoxy-2'-substituted uridines and their 5'-phosphates towards thymidylate synthetase from Escherichia coli K12 was investigated. Besides the natural substrate 2'-deoxyuridine-5'-phosphate (dUMP), only 2'-deoxy-2'-fluorouridine-5'-phosphate (dUflMP) was a substrate. The KM of dUflMP is 11 times higher than that of dUMP, while the Vmax values are virtually the same. It is concluded that the size of the 2'-substituent and not its polarity (and the concomitant conformational change) determines substrate specificity of thymidylate synthetase.
摘要
研究了2'-脱氧-2'-取代尿苷及其5'-磷酸酯对大肠杆菌K12胸苷酸合成酶的底物特异性。除了天然底物2'-脱氧尿苷-5'-磷酸（dUMP）外，只有2'-脱氧-2'-氟尿苷-5'-磷酸（dUflMP）是底物。dUflMP的KM比dUMP高11倍，而Vmax值实际上相同。得出的结论是，2'-取代基的大小而非其极性（以及随之而来的构象变化）决定了胸苷酸合成酶的底物特异性。
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