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Method for identifying agonists and antagonists of dna replication using an (in vitro) mammalian dna replication system

机译:使用(体外)哺乳动物dna复制系统鉴定dna复制的激动剂和拮抗剂的方法

摘要

The present invention relates to an in vitro mammalian DNA replication system and to a method for identifying agonists and antagonists of DNA replication. The method comprises contacting in vitro a plasmid with a mixture comprising nuclear or cytoplasmic extracts from HeLa cells, the drug and a mixture of nucleotides, assessing the stimulation or the inhibition of initiation of DNA replication and the elongation of nascent DNA produced by the drug, and identifying the essential structures of the drug by quantitative structure-activity relationship (QSAR) analysis deriving relationships between the structural features of the drug and biological responses produced by the binding of the drug to the target receptor. The plasmid has a target receptor and comprises a specific mammalian origin of DNA replication.
机译:本发明涉及体外哺乳动物DNA复制系统和鉴定DNA复制的激动剂和拮抗剂的方法。该方法包括使质粒与包含HeLa细胞核或细胞质提取物,药物和核苷酸混合物的混合物在体外接触,评估对DNA复制起始的刺激或抑制以及药物产生的新生DNA的延伸,并通过定量结构-活性关系(QSAR)分析鉴定药物的基本结构,该定量分析推导了药物的结构特征与药物与靶标受体结合产生的生物学反应之间的关系。该质粒具有靶受体,并包含DNA复制的特定哺乳动物来源。

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