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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.

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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