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喹诺酮类抗生素可抑制真核生物DNA聚合酶α和β、末端脱氧核苷酸转移酶,但不抑制DNA连接酶。

Quinolone antibiotics inhibit eucaryotic DNA polymerase alpha and beta, terminal deoxynucleotidyl transferase but not DNA ligase.

作者信息

Rusquet R, Bonhommet M, David J C

出版信息

Biochem Biophys Res Commun. 1984 Jun 29;121(3):762-9. doi: 10.1016/0006-291x(84)90744-7.

Abstract

DNA polymerases alpha and beta, Terminal deoxynucleotidyl Transferase and DNA ligases from chicken thymus were purified to homogeneity. Quinolone antibiotics (nalidixic acid, oxolinic acid and pefloxacin ) known to inhibit DNA replication were tested for their effects on these enzymes. DNA ligase activity was not affected by the three drugs. DNA polymerases alpha and beta were inhibited by competitive mechanisms. Surprisingly, Terminal deoxynucleotidyl Transferase was strongly inhibited by the three compounds and more efficiently by nalidixic acid. The significance of these results is discussed in terms of the possible involvement of the enzymes in the respective DNA replication and repair processes.

摘要

从鸡胸腺中纯化出了α和β DNA聚合酶、末端脱氧核苷酸转移酶以及DNA连接酶,使其达到了均一性。对已知可抑制DNA复制的喹诺酮类抗生素(萘啶酸、恶喹酸和培氟沙星)对这些酶的作用进行了测试。DNA连接酶的活性不受这三种药物的影响。α和β DNA聚合酶受到竞争性机制的抑制。令人惊讶的是,末端脱氧核苷酸转移酶受到这三种化合物的强烈抑制,且萘啶酸的抑制效果更显著。根据这些酶可能参与各自的DNA复制和修复过程,对这些结果的意义进行了讨论。

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