抑肽素衍生物对DNA聚合酶α的抑制作用。
Inhibition of DNA polymerase alpha by aphidicolin derivatives.
作者信息
Arabshahi L, Brown N, Khan N, Wright G
机构信息
Department of Pharmacology, University of Massachusetts Medical School, Worcester 01655.
出版信息
Nucleic Acids Res. 1988 Jun 10;16(11):5107-13. doi: 10.1093/nar/16.11.5107.
Abstract
17-Acetylaphidicolin was 10-fold weaker and two derivatives lacking hydroxyl groups at the 16 and 17 positions were 100-fold weaker than aphidicolin as inhibitors of DNA polymerase alpha from HeLa and Chinese hamster ovary cells. 17,18-Diacetyl, 3,17,18-triacetyl and 3-epi derivatives of aphidicolin were inactive. Active compounds were, like aphidicolin, competitive with dCTP and did not inhibit aphidicolin-resistant DNA polymerases.
摘要
17-乙酰基杀稻瘟菌素的抑制活性比杀稻瘟菌素弱10倍，而在16和17位缺少羟基的两种衍生物作为来自HeLa细胞和中国仓鼠卵巢细胞的DNA聚合酶α抑制剂，其抑制活性比杀稻瘟菌素弱100倍。杀稻瘟菌素的17,18-二乙酰基、3,17,18-三乙酰基和3-表位衍生物无活性。与杀稻瘟菌素一样，活性化合物与dCTP具有竞争性，且不抑制抗杀稻瘟菌素的DNA聚合酶。
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