公开(公告)号：US08420335B2

公开(公告)日：2013-04-16

申请号：US12282485

申请日：2007-03-14

申请人： Paul Cloos ,  Karl Agger ,  Jesper Christensen ,  Klaus H. Hansen ,  Kristian Helin

发明人： Paul Cloos ,  Karl Agger ,  Jesper Christensen ,  Klaus H. Hansen ,  Kristian Helin

IPC分类号： G01N33/53 ,  G01N31/00

CPC分类号： C12Q1/48 ,  G01N33/6875 ,  G01N2333/91011 ,  G01N2500/00 ,  Y10T436/10

摘要： The present invention provides a method of testing the ability of a test compound to bind to and optionally modulate the activity of a protein of the JMJD2 subfamily of Jumonji proteins. The method comprises incubating a test compound with a protein of the JMJD2 subfamily of Jumonji proteins, a co-factor of said protein and, optionally, a substrate for demethylation. The method of the invention can be used for screening large numbers of compounds to identify a group of compounds that are candidate compounds for clinical use for treatment of certain cancers especially prostate cancers. Other compounds that do not have activity in the screening assays can be eliminated from further consideration as candidate compounds. The method of the invention therefore has utility in the pharmaceutical industry.

摘要翻译： 本发明提供了测试化合物与Jumonji蛋白的JMJD2亚家族蛋白质结合并任选调节其活性的能力的方法。 该方法包括将测试化合物与Jumonji蛋白的JMJD2亚族蛋白质的蛋白质，所述蛋白质的辅因子和任选的脱甲基化底物一起孵育。 本发明的方法可用于筛选大量化合物以鉴定作为临床用于治疗某些癌症，特别是前列腺癌的候选化合物的一组化合物。 在筛选测定中不具有活性的其它化合物可以从作为候选化合物的进一步考虑中消除。 因此，本发明的方法在制药工业中具有效用。

公开(公告)号：US20090162945A1

公开(公告)日：2009-06-25

申请号：US12282485

申请日：2007-03-14

申请人： Paul Cloos ,  Karl Agger ,  Jesper Christensen ,  Klaus H. Hansen ,  Kristian Helin

发明人： Paul Cloos ,  Karl Agger ,  Jesper Christensen ,  Klaus H. Hansen ,  Kristian Helin

IPC分类号： G01N33/68 ,  G01N33/53

CPC分类号： C12Q1/48 ,  G01N33/6875 ,  G01N2333/91011 ,  G01N2500/00 ,  Y10T436/10

摘要： The present invention provides a method of testing the ability of a test compound to bind to and optionally modulate the activity of a protein of the JMJD2 subfamily of Jumonji proteins. The method comprises incubating a test compound with a protein of the JMJD2 subfamily of Jumonji proteins, a co-factor of said protein and, optionally, a substrate for demethylation. The method of the invention can be used for screening large numbers of compounds to identify a group of compounds that are candidate compounds for clinical use for treatment of certain cancers especially prostate cancers. Other compounds that do not have activity in the screening assays can be eliminated from further consideration as candidate compounds. The method of the invention therefore has utility in the pharmaceutical industry.

摘要翻译： 本发明提供了测试化合物与Jumonji蛋白的JMJD2亚家族蛋白质结合并任选调节其活性的能力的方法。 该方法包括将测试化合物与Jumonji蛋白的JMJD2亚族蛋白质的蛋白质，所述蛋白质的辅因子和任选的脱甲基化底物一起孵育。 本发明的方法可用于筛选大量化合物以鉴定作为临床用于治疗某些癌症，特别是前列腺癌的候选化合物的一组化合物。 在筛选测定中不具有活性的其它化合物可以从作为候选化合物的进一步考虑中消除。 因此，本发明的方法在制药工业中具有效用。