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    Inhibitors of phosphoserine and phosphothreonine-proline-specific isomerases
    1.
    发明授权
    Inhibitors of phosphoserine and phosphothreonine-proline-specific isomerases 失效
    磷酸丝氨酸和磷酸苏氨酸 - 脯氨酸特异性异构酶的抑制剂

    公开(公告)号：US06462173B1

    公开(公告)日：2002-10-08

    申请号：US08988842

    申请日：1997-12-11

    Applicant: Kun Ping Lu ,  Lewis Cantley ,  Michael Yaffe ,  Gunter Fischer

    Inventor： Kun Ping Lu ,  Lewis Cantley ,  Michael Yaffe ,  Gunter Fischer

    IPC: C07K700

    CPC classification number: C07K1/047 ,  A61K38/00 ,  C07K1/006 ,  C07K14/001

    Abstract: Inhibitors of phosphoserine- or posphothreonine-specific peptidyl prolyl isomerases are described. Such inhibitors include molecules that mimic the structure and conformation of the pSer/pThr-Pro peptide moiety of the isomerase substrate when the substrate is bound into the active site of the isomerase. For example, a protein, peptide or peptide mimetic including xSer/ThrY where x is a negatively charged tetra or pentavalent moiety and Y is a Pro or a Pro analog. Methods of inhibiting cell growth and methods of identifying phosphoserine- or phosphothreonine-proline specific peptidyl-prolyl isomerase inhibitors are also included in the invention.

    Abstract translation: 描述了磷酸丝氨酸或磷酸苏氨酸特异性肽基脯氨酰异构酶的抑制剂。 这种抑制剂包括当底物结合到异构酶的活性位点时模拟异构酶底物的pSer / pThr-Pro肽部分的结构和构象的分子。 例如，包括xSer / ThrY的蛋白质，肽或肽模拟物，其中x是带负电荷的四价或五价部分，Y是Pro或Pro类似物。 抑制细胞生长的方法以及鉴定磷酸丝氨酸或磷酸腺嘌呤 - 脯氨酸特异性肽基 - 脯氨酰异构酶抑制剂的方法也包括在本发明中。

    Cell-based screening methods
    5.
    发明授权
    Cell-based screening methods 失效
    基于细胞的筛选方法

    公开(公告)号：US06730492B2

    公开(公告)日：2004-05-04

    申请号：US10093945

    申请日：2002-03-09

    Applicant: Michael H. Cardone ,  Michael Yaffe

    Inventor： Michael H. Cardone ,  Michael Yaffe

    IPC: C12Q148

    CPC classification number: C12Q1/25 ,  C12Q1/485 ,  G01N2500/00

    Abstract: Cell-based screening methods for determining kinase activity are provided. The methods utilize existing cellular pathways that are regulated by kinases. In one embodiment, various components of a ubiquitin-mediated degradation pathway are modified to create an assay that can be used to screen for a molecule that modulates the activity of a kinase of interest that otherwise does not regulate the degradation pathway. In another embodiment, various components of a protein translocation pathway are modified to screen for a molecule that modulates the activity of a kinase of interest that otherwise does not regulate the translocation pathway.

    Abstract translation: 提供了用于确定激酶活性的基于细胞的筛选方法。 该方法利用由激酶调控的现有细胞途径。 在一个实施方案中，修饰泛素介导的降解途径的各种组分以产生可用于筛选否则不调节降解途径的调节感兴趣的激酶的活性的分子的测定。 在另一个实施方案中，修饰蛋白质易位途径的各种组分以筛选调节感兴趣的激酶（否则不调节易位途径）的活性的分子。

    Cell-based screening methods
    6.
    发明授权
    Cell-based screening methods 失效

    公开(公告)号：US07083938B2

    公开(公告)日：2006-08-01

    申请号：US10771035

    申请日：2004-02-03

    Applicant: Michael H. Cardone ,  Michael Yaffe

    Inventor： Michael H. Cardone ,  Michael Yaffe

    IPC: C12Q1/48 ,  C12N9/00 ,  C12P21/06 ,  C07K1/00

    CPC classification number: C12Q1/25 ,  C12Q1/485 ,  G01N2500/00

    Abstract: Cell-based screening methods for determining kinase activity are provided. The methods utilize existing cellular pathways that are regulated by kinases. In one embodiment, various components of a ubiquitin-mediated degradation pathway are modified to create an assay that can be used to screen for a molecule that modulates the activity of a kinase of interest that otherwise does not regulate the degradation pathway. In another embodiment, various components of a protein translocation pathway are modified to screen for a molecule that modulates the activity of a kinase of interest that otherwise does not regulate the translocation pathway.

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