Introduction of the α-P-borano-group into deoxynucleoside triphosphates increases their selectivity to HIV-1 reverse transcriptase relative to DNA Polymerases

被引：16

作者：

Dobrikov, MI ^{[1
]}

Grady, KM ^{[1
]}

Shaw, BR ^{[1
]}

机构：

[1] Duke Univ, Dept Chem, Paul M Gross Chem Lab, Durham, NC 27708 USA

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2003年 / 22卷 / 03期

关键词：

boranophosphates; HIV-1 reverse transcriptase; DNA polymerase; steady-state kinetics;

D O I：

10.1081/NCN-120021427

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 2'-deoxynucleoside 5'-triphosphates (dNTPs) and their alpha-P-thio or alpha-beta-borano analogues, i.e., (Sp-dNTPalphaS), (Rp-dNTPalphaB) and (Sp-dNTPalphaB) were studied as substrates for DNA dependent DNA polymerases and HIV-1 reverse transcriptase (RT). For HIV-1 RT the Rp-dNTPalphaB isomers are 1.2-fold better substrates than natural dNTPs. For DNA polymerases their efficiencies of incorporation are Mold (Klenow, Sequenase) and 5-fold (Taq) lower than for dNTPs. Thus, introduction of the alpha-boranophosphate group into dNTPs increases their selectivity to HIV-1 RT relative to bacterial DNA polymerases.

引用

页码：275 / 282

页数：8

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