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新型核苷酸类似物作为TMPK（齐多夫定代谢中的关键酶）的潜在底物。

Novel nucleotide analogues as potential substrates for TMPK, a key enzyme in the metabolism of AZT.

作者信息

Müller H C, Meier C, Balzarini J, Reinstein J

机构信息

Institute of Organic Chemistry, University of Hamburg, Hamburg, Germany.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):821-3. doi: 10.1081/NCN-120022662.

DOI:10.1081/NCN-120022662
PMID:14565287
Abstract

Novel cyclic and acyclic analogues of dTMP and AZTMP were synthesized from the corresponding cycloSal-phosphotriesters. This method yielded the nucleotides in good yields with a simple work-up. Investigation of the substrate properties of the modified nucleotides towards TmpK showed, that they are very poor substrates for this key enzyme in the bioactivation of AZT.

摘要

新型dTMP和AZTMP的环状及非环状类似物由相应的环Sal-磷酸三酯合成。该方法通过简单的后处理以良好产率得到核苷酸。对修饰核苷酸针对TmpK的底物性质研究表明，它们是AZT生物活化中该关键酶的非常差的底物。

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