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含有修饰碱基的寡核苷酸。I. 部分硫醇化的寡聚胞苷酸对DNA和RNA聚合酶的抑制作用。

Oligonucleotides containing modified bases. I. Inhibition of DNA and RNA polymerases by partially thiolated oligocytidylic acids.

作者信息

Ho Y K, Kung M P, Bardos T J

机构信息

Department of Medicinal Chemistry, State University of New York at Buffalo, Buffalo, NY 14214, USA.

出版信息

Biochem Biophys Res Commun. 1976 Dec 20;73(4):903-10. doi: 10.1016/0006-291x(76)90207-2.

DOI:10.1016/0006-291x(76)90207-2
PMID:15633263
Abstract

A series of oligomers of cytidylic acid were prepared and partially (6-9% of the bases) thiolated in the 5 positions. The modified oligomers showed increasing inhibition with increasing chain length of both the DNA polymerase-alpha from regenerating rat liver and the DNA-dependent RNA polymerase of E. coli, but the minimum chain length for observable inhibitory activity was 5 nucleotide units for the DNA polymerase-alpha and 16 units for the RNA polymerase.

摘要

制备了一系列胞苷酸寡聚物,并在5位进行了部分(6 - 9%的碱基)硫醇化修饰。修饰后的寡聚物对再生大鼠肝脏中的DNA聚合酶α和大肠杆菌的DNA依赖性RNA聚合酶的抑制作用均随链长增加而增强,但对于DNA聚合酶α,可观察到抑制活性的最小链长为5个核苷酸单位,对于RNA聚合酶则为16个单位。

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Biochem Biophys Res Commun. 1976 Dec 20;73(4):903-10. doi: 10.1016/0006-291x(76)90207-2.
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引用本文的文献

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Nucleic Acids Res. 1980 Jul 25;8(14):3175-91. doi: 10.1093/nar/8.14.3175.
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Synthesis and properties of poly 5-methylthiouridylic acid.聚5-甲基硫代尿苷酸的合成与性质
Nucleic Acids Res. 1984 Oct 11;12(19):7599-614. doi: 10.1093/nar/12.19.7599.
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Structure-activity relationships and mode of action of 5-mercapto-substituted oligo- and polynucleotides as antitemplates inhibiting replication of human immunodeficiency virus type 1.
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