Bisubstrate fluorescent probes for protein kinase CK2
    10.
    发明公开
    Bisubstrate fluorescent probes for protein kinase CK2 审中-公开
    Bisubstrate荧光探针用于蛋白激酶CK2

    公开(公告)号:EP2700946A1

    公开(公告)日:2014-02-26

    申请号:EP12181818.1

    申请日:2012-08-24

    Abstract: This invention relates to fluorescent probes for screening and characterization of compounds binding to protein kinase CK2, measurement of concentration of the catalytically active form of CK2 and imaging of CK2 activity in cells and tissues. The CK2-selective probe of the present invention interacts with binding sites of both substrates of the catalytic subunit of CK2 and therefore can be used for characterization of all inhibitors binding to the active site of CK2 in the binding/displacement assay. The high affinity of the probe affords the detection of the enzyme at low concentration and characterization of inhibitors in a wide affinity range.

    Abstract translation: 本发明涉及用于筛选和表征与蛋白激酶CK2结合的化合物,测量CK2催化活性形式浓度和细胞和组织中CK2活性成像的荧光探针。 本发明的CK2选择性探针与CK2的催化亚基的两个底物的结合位点相互作用,因此可用于在结合/置换测定中鉴定与CK2的活性位点结合的所有抑制剂。 探针的高亲和力提供了低浓度酶的检测和广泛亲和力范围内抑制剂的表征。

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