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SELECTIVE EXPRESSION INHIBITOR FOR AURORA KINASE A AND AURORA KINASE B GENES

机译:极光激酶A和极光激酶B基因的选择性表达抑制剂

摘要

A drug containing a pyrrole-imidazole polyamide comprising an N-methylpyrrole unit (hereinafter sometimes referred to as Py), an N-methylimidazole unit (hereinafter sometimes referred to as Im) and a γ-aminobutyric acid unit which can be folded at the γ-aminobutyric acid unit to form a U-shape conformation within the minor groove in the double strand region (hereinafter referred to as the target region) containing a part of the -100 to -70 positions (SEQ ID NO:2) in the base sequence of human aurora kinase A (hereinafter sometimes referred to as hAURKA) promoter or the whole thereof and a chain that is complementary thereto, and in which the C-G base pair corresponds to the Py/Im pair, the G-C base pair corresponds to the Im/Py pair and the A-T and T-A base pairs correspond each to the Py/Py pair.
机译:包含含有N-甲基吡咯单元(以下有时称为Py),N-甲基咪唑单元(以下有时称为Im)和可以在γ处折叠的γ-氨基丁酸单元的吡咯-咪唑聚酰胺的药物-氨基丁酸单元以在双链区(以下称为靶标区)的小沟内形成U形构象,该双链区在碱基中包含-100至-70位(SEQ ID NO:2)的一部分人极光激酶A(以下有时称为hAURKA)启动子的序列或其整体以及与其互补的链,其中CG碱基对对应于Py / Im对,GC碱基对对应于Im / Py对以及AT和TA碱基对分别对应于Py / Py对。

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