BuPdGTP和BuAdATP对人胎盘DNA聚合酶δ和α的差异抑制作用。
Differential inhibition of human placental DNA polymerases delta and alpha by BuPdGTP and BuAdATP.
作者信息
Lee M Y, Toomey N L, Wright G E
出版信息
Nucleic Acids Res. 1985 Dec 9;13(23):8623-30. doi: 10.1093/nar/13.23.8623.
Abstract
The p-n-butylphenyl- and p-n-butylanilino- substituted analogs of dGTP and dATP, respectively, were tested as inhibitors of purified human placental DNA polymerases alpha and delta. It was observed that DNA polymerase alpha activity was potently inhibited by these analogs with I0.5 values as low as the nanomolar range, whereas DNA polymerase delta activity was poorly inhibited, with I0.5 values of ca. 100 micromolar. These results argue for a distinct identity of these two enzymes, and demonstrate the usefulness of these analogs as probes of DNA polymerase structures. In addition, these analogs provide a rapid method for the discrimination of the two enzyme activities and a means for the selective assay of DNA polymerase delta. Aphidicolin inhibited both DNA polymerases.
摘要
分别测试了dGTP和dATP的对正丁基苯基和对正丁基苯胺基取代类似物作为纯化的人胎盘DNA聚合酶α和δ的抑制剂的效果。结果发现，这些类似物能有效抑制DNA聚合酶α的活性，其半数抑制浓度（I0.5）低至纳摩尔范围，而对DNA聚合酶δ的活性抑制较弱，I0.5值约为100微摩尔。这些结果表明这两种酶具有明显的差异，也证明了这些类似物作为DNA聚合酶结构探针的实用性。此外，这些类似物提供了一种快速区分这两种酶活性的方法以及一种选择性检测DNA聚合酶δ的手段。阿非科林对两种DNA聚合酶均有抑制作用。
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