INHIBITION OF A DNA POLYMERASE FROM BACILLUS-SUBTILIS BY HYDROXYPHENYLAZOPYRIMIDINES

INHIBITION OF A DNA POLYMERASE FROM BACILLUS-SUBTILIS BY HYDROXYPHENYLAZOPYRIMIDINES
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DOI:
10.1073/pnas.70.1.103
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发表时间:
1973-01-01
影响因子:
11.1
通讯作者:
COZZARELLI, NR
COZZARELLI, NR
中科院分区:
综合性期刊1区
文献类型:
--
作者:
GASS, KB;LOW, RL;COZZARELLI, NR

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抗菌剂6-(对羟基苯偶氮)-尿嘧啶对枯草芽孢杆菌DNA聚合酶III具有明显的抑制作用,其Ki值小于1μM。这种抑制作用需要预先还原药物,是可逆的,并且与dGTP具有竞争性。高剂量的dATP可防止与之密切相关的药物6-(对羟基苯偶氮)-异胞嘧啶的抑制作用。提出了一种模型,其中抑制剂与模板碱基配对,而与酶形成三元络合物的一部分。这些结果表明DNA聚合酶III OFB。染色体复制所必需的精华。
The antimicrobial agent, 6-(p-hydroxyphenylazo)-uracil, specifically inhibits DNA polymerase III ofBacillus subtiliswith aKiof less than 1 μM. The inhibition requires prior reduction of the drug, is reversible, and is competitive with dGTP. High amounts of dATP prevent inhibition by the closely related drug, 6-(p-hydroxyphenylazo)-isocytosine. A model is presented in which the inhibitors base-pair with the template while part of a ternary complex with the enzyme. These results imply that DNA polymerase III ofB. subtilisis necessary for chromosomal replication.