Introduction of the alpha-P-borano-group into deoxynucleoside triphosphates increases their selectivity to HIV-1 reverse transcriptase relative to DNA polymerases.
Introduction of the alpha-P-borano-group into deoxynucleoside triphosphates increases their selectivity to HIV-1 reverse transcriptase relative to DNA polymerases.
复制标题
将α-P-硼烷基引入脱氧核苷三磷酸中，相对于DNA聚合酶，增加了它们对HIV-1逆转录酶的选择性。
DOI：
10.1081/ncn-120021427
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发表时间：
2003
期刊：
影响因子：
--
通讯作者：
Shaw,BarbaraRamsay
中科院分区：
文献类型：
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作者：
Dobrikov,MikhailI;Grady,KristenM;Shaw,BarbaraRamsay
一系列2′-脱氧核苷5′-三磷酸（dNTPs）及其α-P-硫代或α-P-硼烷类似物，即，研究了（Sp-dNTPαS）、（Rp-dNTPαB）和（Sp-dNTPαB）作为DNA依赖性DNA聚合酶和HIV-1逆转录酶（RT）的底物。对于HIV-1 RT，Rp-dNTP αB异构体是比天然dNTP好1.2倍的底物。对于DNA聚合酶，它们的掺入效率比dNTP低3倍（Klenow，Sequenase）和5倍（Taq）。因此，相对于细菌DNA聚合酶，在dNTP中引入α-硼烷基磷酸基团增加了它们对HIV-1 RT的选择性。
A series of 2′-deoxynucleoside 5′-triphosphates (dNTPs) and their α-P-thio or α-P-borano analogues, i.e., (Sp-dNTPαS), (Rp-dNTPαB) and (Sp-dNTPαB) were studied as substrates for DNA dependent DNA polymerases and HIV-1 reverse transcriptase (RT). For HIV-1 RT theRp-dNTPαB isomers are 1.2-fold better substrates than natural dNTPs. For DNA polymerases their efficiencies of incorporation are 3-fold (Klenow, Sequenase) and 5-fold (Taq) lower than for dNTPs. Thus, introduction of the α-boranophosphate group into dNTPs increases their selectivity to HIV-1 RT relative to bacterial DNA polymerases.