HOMOGENEOUS AND HETEROGENEOUS ASSAY METHODS USING NUCLEATION CENTERS AND NOVEL COVALENT CHEMISTRIES FOR THE RAPID MEASUREMENT OF PHOSPHORYLATION AND DE-PHOSPHORYLATION
    1.
    发明申请
    HOMOGENEOUS AND HETEROGENEOUS ASSAY METHODS USING NUCLEATION CENTERS AND NOVEL COVALENT CHEMISTRIES FOR THE RAPID MEASUREMENT OF PHOSPHORYLATION AND DE-PHOSPHORYLATION 审中-公开
    使用核化中心和新颖的合成化学品进行均相和异质性测定方法,用于快速测定磷化氢和脱磷酸

    公开(公告)号:WO2004089295A2

    公开(公告)日:2004-10-21

    申请号:PCT/US2004/010289

    申请日:2004-04-01

    IPC: A61K

    Abstract: Novel chemistries, methods and assays are described for the rapid detection and measurement of phosphorylation or de-phosphorylation of polypeptides, oligonucleotides or lipids based upon the use of phosphoryl, phosphoroamino or phosphorothioate specific hetero-bifunctional linkers combined with fluorescence polarization or fluorogenic detection. Homogeneous assay applications possible using these novel chemistries and methods include in vitro fluorescence polarization assays for the detection of general and isoform­ specific polypeptide, oligonucleotide and lipid kinase and phosphatase enzymes. Heterogeneous assay applications possible using the same novel chemistries and assaymethods enable development of in vitro and in vivo fluorogenic assays of general or specific kinase or phosphatase enzyme activities in cell lysates or serum. In all cases, these new chemistries, methods and assays enable simultaneous multi-kinase detection and profiling.

    Abstract translation: 描述了基于使用与荧光偏振或荧光检测结合的磷酰基,磷酰氨基或硫代磷酸酯特异性异双功能连接物快速检测和测量多肽,寡核苷酸或脂质的磷酸化或去磷酸化的新型化学,方法和测定法。 使用这些新颖化学和方法可能的均相测定应用包括用于检测一般和同种型特异性多肽,寡核苷酸和脂质激酶和磷酸酶的体外荧光偏振测定。 使用相同的新颖化学和测定方法可能的非均相测定应用使得能够开发在细胞裂解物或血清中的一般或特异性激酶或磷酸酶活性的体外和体内荧光测定。 在所有情况下,这些新的化学成分,方法和测定可以同时进行多激酶检测和分析。

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