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    • 1. 发明申请
    • Methods for identifying small molecules that modulate premature translation termination and nonsense mediated mrna decay
    • 用于鉴定调节过早翻译终止和废话介导的mrna衰变的小分子的方法
    • US20060257866A1
    • 2006-11-16
    • US10521775
    • 2003-07-24
    • Ellen WelchNeil AlmsteadRobert RandoMathew Pellegrini
    • Ellen WelchNeil AlmsteadRobert RandoMathew Pellegrini
    • C40B30/06C12Q1/68
    • B82Y30/00G01N33/5308G01N2500/04
    • The present invention relates to a method for screening and identifying compounds that modulate premature translation termination and/or nonsense-mediated messenger ribonucleic acid (“mRNA”) by interacting with a preselected target ribonucleic acid (“RNA”). In particular, the present invention relates to identifying compounds that bind to regions of the 28S ribosomal RNA (“rRNA”) and analogs thereof. Direct, noncompetitive binding assays are advantageously used to screen libraries of compounds for those that selectively bind to a preselected target RNA. Binding of target RNA molecules to a particular compound is detected using any physical method that measures the altered physical property of the target RNA bound to a compound. The structure of the compound attached to the labeled RNA is also determined. The methods used will depend, in part, on the nature of the library screened. The methods of the present invention provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads.
    • 本发明涉及通过与预选的靶核糖核酸(“RNA”)相互作用来筛选和鉴定调节过早翻译终止和/或无义介导的信使核糖核酸(“mRNA”)的化合物的方法。 特别地,本发明涉及鉴定结合28S核糖体RNA(“rRNA”)的区域的化合物及其类似物。 直接的非竞争性结合测定法有利地用于筛选选择性结合预选靶RNA的化合物文库。 使用测量与化合物结合的靶RNA的改变的物理性质的任何物理方法检测靶RNA分子与特定化合物的结合。 还测定了附着于标记的RNA的化合物的结构。 所使用的方法部分取决于所筛选图书馆的性质。 本发明的方法提供了用于识别药物引线的化合物文库的高通量筛选的简单,灵敏的测定。
    • 2. 发明申请
    • Methods for identifying small molecules that bind specific RNA structural motifs
    • 鉴定结合特异性RNA结构基序的小分子的方法
    • US20060228730A1
    • 2006-10-12
    • US11347748
    • 2006-02-03
    • Robert RandoEllen Welch
    • Robert RandoEllen Welch
    • C40B40/08
    • G01N33/5308G01N33/58
    • The present invention relates to a method for screening and identifying test compounds that bind to a preselected target ribonucleic acid (“RNA”). Direct, non-competitive binding assays are advantageously used to screen libraries of compounds for those that selectively bind to a preselected target RNA. Binding of target RNA molecules to a particular test compound is detected using any physical method that measures the altered physical property of the target RNA bound to a test compound. The structure of the test compound attached to the labeled RNA is also determined. The methods used will depend, in part, on the nature of the library screened. The methods of the present invention provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads.
    • 本发明涉及筛选和鉴定结合预选靶核糖核酸(“RNA”)的测试化合物的方法。 直接的非竞争性结合测定法有利地用于筛选选择性结合预选靶RNA的化合物文库。 使用测量与测试化合物结合的靶RNA的改变的物理性质的任何物理方法检测靶RNA分子与特定测试化合物的结合。 还测定了附着于标记的RNA的测试化合物的结构。 所使用的方法部分取决于所筛选图书馆的性质。 本发明的方法提供了用于识别药物引线的化合物文库的高通量筛选的简单,灵敏的测定。
    • 6. 发明授权
    • Methods for identifying small molecules that modulate premature translation termination and nonsense mRNA decay
    • 用于鉴定调节过早翻译终止和无义mRNA衰变的小分子的方法
    • US07291461B2
    • 2007-11-06
    • US10519243
    • 2003-06-23
    • Ellen WelchJin Zhuo
    • Ellen WelchJin Zhuo
    • C12Q1/68C07H21/02C07H21/04
    • C12Q1/6897
    • The present invention relates to methods for identifying compounds that modulate premature translation termination and/or nonsense-mediated mRNA decay by screening and identifying compounds that modulate the post-transcriptional expression of any gene with a premature translation stop codon. The invention particularly relates to using any gene encoding a premature stop codon to identify compounds that modulate premature translation termination and/or nonsense-mediated mRNA decay. A compound that modulates premature translation termination and/or nonsense-mediated mRNA decay of a target gene is identified using standard methods known in the art to measure changes in translation or mRNA stability of the gene product or mRNA of the gene with the premature stop codon. The methods of the present invention provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads.
    • 本发明涉及通过筛选和鉴定调节具有过早翻译终止密码子的任何基因的转录后表达的化合物来鉴定调节过早翻译终止和/或无义介导的mRNA衰变的化合物的方法。 本发明特别涉及使用编码过早终止密码子的任何基因来鉴定调节过早翻译终止和/或无义介导的mRNA衰变的化合物。 使用本领域已知的标准方法鉴定调节前体转录终止和/或无义介导的mRNA基因的衰老的化合物,以测量基因产物或基因mRNA的mRNA稳定性的变化,所述基因产物或mRNA的早期终止密码子 。 本发明的方法提供了用于识别药物引线的化合物文库的高通量筛选的简单,灵敏的测定。