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    IN VIVO METHOD FOR THE EVALUATION OF A COMPOUND-TARGET INTERACTION
    1.
    发明申请
    IN VIVO METHOD FOR THE EVALUATION OF A COMPOUND-TARGET INTERACTION 审中-公开
    用于评估化合物 - 目标相互作用的体内方法

    公开(公告)号：US20130210030A1

    公开(公告)日：2013-08-15

    申请号：US13809811

    申请日：2011-06-20

    申请人： Gerard Drewes ,  Carsten Hopf ,  Gitte Neubauer ,  Ulrich Kruse

    发明人： Gerard Drewes ,  Carsten Hopf ,  Gitte Neubauer ,  Ulrich Kruse

    IPC分类号： G01N33/573

    CPC分类号： G01N33/573 ,  G01N33/5088 ,  G01N2333/91215 ,  G01N2500/00

    摘要： The invention relates to a method for evaluation of a compound-target interaction in vivo, comprising the steps of administering the compound to an animal, taking a body fluid sample of the animal, determining the concentration of the compound in the body fluid sample, taking a cellular sample of the animal containing the target, preparing a protein preparation of said cellular sample, providing an immobilised ligand capable of binding to the target, contacting the protein preparation with the immobilised ligand under conditions allowing the formation of a complex between the immobilised ligand and the target, determining the amount of complexes formed in step, and correlating the amount of complexes with the concentration of the compound in the body fluid sample.

    摘要翻译： 本发明涉及一种用于评价体内化合物 - 靶相互作用的方法，包括以下步骤：向动物施用化合物，服用动物的体液样品，测定体液样品中化合物的浓度，取 制备含有靶标的动物的细胞样品，制备所述细胞样品的蛋白质制剂，提供能够结合靶标的固定配体，使蛋白质制剂与固定的配体在允许形成固定化配体之间的复合物的条件下接触 和靶标，测定步骤中形成的复合物的量，并将复合物的量与体液样品中化合物的浓度相关联。

    Protein kinase (NPK-110)
    5.
    发明授权
    Protein kinase (NPK-110) 失效
    蛋白激酶（NPK-110）

    公开(公告)号：US07485712B2

    公开(公告)日：2009-02-03

    申请号：US10440435

    申请日：2003-05-16

    申请人： Eckhard Mandelkow ,  Eva-Marie Mandelkow ,  Jacek Biernat ,  Gerard Drewes

    发明人： Eckhard Mandelkow ,  Eva-Marie Mandelkow ,  Jacek Biernat ,  Gerard Drewes

    IPC分类号： C12N15/54 ,  C12N9/12

    CPC分类号： C12N9/1205 ,  A61K38/00 ,  C07K14/4711

    摘要： The present invention relates to a DNA sequence encoding a novel neuronal protein kinase (NPK) which phosphorylates tau proteins as well as other microtubule associated proteins (MAPs) in positions crucial for the binding to microtubules. The invention further relates to Serine or Theorine residues and epitopes comprising said residues phosphorylated by said NPK on said MAPs, to antibodies specifically binding to said protein kinase, pharmaceutical compositions comprising inhibitors to said protein kinase, in particular for the treatment of Alzheimer's disease and cancer, to diagnostic kits and to in vitro diagnostic methods for the detection of Alzheimer's disease and cancer.

    摘要翻译： 本发明涉及编码新型神经元蛋白激酶（NPK）的DNA序列，其在与微管结合至关重要的位置磷酸化tau蛋白以及其它微管相关蛋白（MAP）。 本发明进一步涉及丝氨酸或Theorine残基和表位，其包含由所述MAP上的所述NPK磷酸化的所述残基，特异性结合所述蛋白激酶的抗体，包含所述蛋白激酶抑制剂的药物组合物，特别是用于治疗阿尔茨海默氏病和癌症 ，诊断试剂盒和用于检测阿尔茨海默病和癌症的体外诊断方法。

    METHODS FOR THE IDENTIFICATION OF ZAP-70 INTERACTING MOLECULES AND FOR THE PURIFICATION OF ZAP-70
    8.
    发明申请
    METHODS FOR THE IDENTIFICATION OF ZAP-70 INTERACTING MOLECULES AND FOR THE PURIFICATION OF ZAP-70 审中-公开

    公开(公告)号：US20120178180A1

    公开(公告)日：2012-07-12

    申请号：US12302711

    申请日：2007-06-01

    申请人： Ulrich Kruse ,  Nigel Ramsden ,  Gerard Drewes ,  Dirk Eberhard

    发明人： Ulrich Kruse ,  Nigel Ramsden ,  Gerard Drewes ,  Dirk Eberhard

    IPC分类号： G01N33/53 ,  G01N30/02

    CPC分类号： C12Q1/485 ,  C12N9/1205 ,  G01N33/57426 ,  G01N2333/91215 ,  G01N2500/02 ,  G01N2500/10

    摘要： The invention provides in a first aspect a method for the identification of an ZAP-70 interacting compound, comprising the steps of a) providing a protein preparation containing phosphorylated ZAP-70, b) contacting the protein preparation with aminopyrido-pyrimidine ligand 24 immobilized on a solid support under conditions allowing the formation of an aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex, c) incubating the aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex with a given compound, and d) determining whether the compound is able to separate phosphorylated ZAP-70 from the immobilized aminopyrido-pyrimidine ligand 24. In a second aspect, the present invention relates to A method for the identification of an ZAP-70 interacting compound, comprising the steps of a) providing a protein preparation containing phosphorylated ZAP-70, b) contacting the protein preparation with ligand aminopyrido-pyrimidine ligand 24 immobilized on a solid support and with a given compound under conditions allowing the formation of an aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex, and c) detecting the aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex formed in step b). In a third aspect, the invention provides a method for the identification of an ZAP-70 interacting compound, comprising the steps of: a) providing two aliquots of a protein preparation containing phosphorylated ZAP-70, b) contacting one aliquot with aminopyrido-pyrimidine ligand 24 immobilized on a solid support under conditions allowing the formation of an aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex, c) contacting the other aliquot with aminopyrido-pyrimidine ligand 24 immobilized on a solid support and with a given compound under conditions allowing the formation of an aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex, and d) determining the amount of aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex formed in steps b) and c). In a forth aspect, the invention relates to a method for the identification of an ZAP-70 interacting compound, comprising the steps of: a) providing two aliquots comprising each at least one cell containing phosphorylated ZAP-70, b) incubating one aliquot with a given compound, c) harvesting the cells of each aliquot, d) lysing the cells in order to obtain protein preparations, e) contacting the protein preparations with aminopyrido-pyrimidine ligand 24 immobilized on a solid support under conditions allowing the formation of an aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex, and f) determining the amount of aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex formed in each aliquot in step e).