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    KINASES AS TARGETS FOR ANTI-DIABETIC THERAPY
    1.
    发明申请
    KINASES AS TARGETS FOR ANTI-DIABETIC THERAPY 审中-公开
    作为抗糖尿病治疗的目标

    公开(公告)号：US20130336986A1

    公开(公告)日：2013-12-19

    申请号：US13820226

    申请日：2011-09-05

    申请人： Mathias Falcenberg ,  Axel Ullrich

    发明人： Mathias Falcenberg ,  Axel Ullrich

    IPC分类号： A61K31/713

    CPC分类号： A61K31/713 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/14 ,  C12Y207/11001 ,  C12Y207/11016 ,  C12Y207/1102

    摘要： The present invention is related to compound capable of modulating the activity and/or expression of the protein kinases SCYL1, ADCK1, and GRK5, thereby enhancing the expression and/or release of insulin. The invention is further related to methods of identifying said compounds for the treatment of diseases of the carbohydrate metabolism. The invention is further related to methods of treatment of diseases of the carbohydrate metabolism, particularly diabetes mellitus type 2.

    摘要翻译： 本发明涉及能够调节蛋白激酶SCYL1，ADCK1和GRK5的活性和/或表达的化合物，从而增强胰岛素的表达和/或释放。 本发明还涉及鉴定用于治疗碳水化合物代谢疾病的所述化合物的方法。 本发明还涉及治疗糖代谢疾病，特别是2型糖尿病的方法。

    USE OF INHIBITORS FOR THE TREATMENT OF RTK-HYPERFUNCTION-INDUCED DISORDERS, PARTICULARLY CANCER
    6.
    发明申请
    USE OF INHIBITORS FOR THE TREATMENT OF RTK-HYPERFUNCTION-INDUCED DISORDERS, PARTICULARLY CANCER 有权
    使用抑制剂治疗RTK超敏感性疾病，特别是癌症

    公开(公告)号：US20100184686A1

    公开(公告)日：2010-07-22

    申请号：US12689672

    申请日：2010-01-19

    申请人： Axel Ullrich ,  Johannes Bange ,  Pjotr Knyazev

    发明人： Axel Ullrich ,  Johannes Bange ,  Pjotr Knyazev

    IPC分类号： A61K38/17 ,  C07K14/71 ,  C07H21/04 ,  C07K16/28 ,  A61P35/04 ,  A61P35/00 ,  C12Q1/68 ,  C12Q1/48

    CPC分类号： C07K14/71 ,  A61K38/00 ,  G01N33/574

    摘要： The present invention concerns the use of inhibitors for the treatment and/or prophylaxis of diseases which are the consequence of increased receptor tyrosine kinase activity, particularly cancer. The use is particularly directed towards inhibition or lowering of the overexpression and/or altered activity of receptor tyrosine kinases (RTKs). In particular, this altered activity of receptor tyrosine kinase can be triggered by a mutation of FGFR-4, wherein this mutation is in particular a point mutation in the transmembrane domain of FGFR-4 and leads to an exchange of a hydrophobic amino acid for a hydrophilic amino acid. The invention further concerns the use of an inhibitor directed against FGFR-4, for the treatment and/or prophylaxis of cancer. Furthermore, the invention concerns a mutated FGFR-4, which leads to over-expression and/or altered activity in cells. Finally, the invention concerns a DNA and RNA sequence of a mutated FGFR-4 molecule. Finally, in addition the invention concerns a pharmaceutical composition, containing the inhibitor as described above and further a diagnostic and screening procedure.

    摘要翻译： 本发明涉及抑制剂用于治疗和/或预防由于受体酪氨酸激酶活性增加，特别是癌症引起的疾病的用途。 该用途特别涉及抑制或降低受体酪氨酸激酶（RTK）的过表达和/或改变的活性。 特别地，受体酪氨酸激酶的这种改变的活性可以由FGFR-4的突变引发，其中该突变特别是FGFR-4的跨膜结构域中的点突变，并导致疏水性氨基酸的交换 亲水氨基酸。 本发明还涉及使用针对FGFR-4的抑制剂来治疗和/或预防癌症。 此外，本发明涉及突变的FGFR-4，其导致细胞中过度表达和/或改变的活性。 最后，本发明涉及突变的FGFR-4分子的DNA和RNA序列。 最后，本发明还涉及包含如上所述的抑制剂的药物组合物，并进一步进行诊断和筛选程序。

    Use of inhibitors for the treatment of RTK-hyperfunction-induced disorders, particularly cancer
    7.
    发明授权
    Use of inhibitors for the treatment of RTK-hyperfunction-induced disorders, particularly cancer 有权
    使用抑制剂治疗RTK-超功能障碍，特别是癌症

    公开(公告)号：US07297774B2

    公开(公告)日：2007-11-20

    申请号：US10863880

    申请日：2004-06-08

    申请人： Axel Ullrich ,  Johannes Bange ,  Pjotr Knyazev

    发明人： Axel Ullrich ,  Johannes Bange ,  Pjotr Knyazev

    IPC分类号： C07K14/00 ,  C12N15/11 ,  C12P21/06

    CPC分类号： C07K14/71 ,  A61K38/00 ,  G01N33/574

    摘要： The present invention concerns the use of inhibitors for the treatment and/or prophylaxis of diseases which are the consequence of increased receptor tyrosine kinase activity, particularly cancer. The use is particularly directed towards inhibition or lowering of the overexpression and/or altered activity of receptor tyrosine kinases (RTKs). In particular, this altered activity of receptor tyrosine kinase can be triggered by a mutation of FGFR-4, wherein this mutation is in particular a point mutation in the transmembrane domain of FGFR-4 and leads to an exchange of a hydrophobic amino acid for a hydrophilic amino acid. The invention further concerns the use of an inhibitor directed against FGFR-4, for the treatment and/or prophylaxis of cancer. Furthermore, the invention concerns a mutated FGFR-4, which leads to overexpression and/or altered activity in cells. Finally, the invention concerns a DNA and RNA sequence of a mutated FGFR-4 molecule. Finally, in addition the invention concerns a pharmaceutical composition, containing the inhibitor as described above and further a diagnostic and screening procedure.

    摘要翻译： 本发明涉及抑制剂用于治疗和/或预防由于受体酪氨酸激酶活性增加，特别是癌症引起的疾病的用途。 该用途特别涉及抑制或降低受体酪氨酸激酶（RTK）的过表达和/或改变的活性。 特别地，受体酪氨酸激酶的这种改变的活性可以由FGFR-4的突变引发，其中该突变特别是FGFR-4的跨膜结构域中的点突变，并导致疏水性氨基酸的交换 亲水氨基酸。 本发明还涉及使用针对FGFR-4的抑制剂来治疗和/或预防癌症。 此外，本发明涉及突变的FGFR-4，其导致细胞中的过表达和/或改变的活性。 最后，本发明涉及突变的FGFR-4分子的DNA和RNA序列。 最后，本发明还涉及包含如上所述的抑制剂的药物组合物，并进一步进行诊断和筛选程序。

    Methods for diagnosis and treatment of MDK1 signal transduction disorders
    9.
    发明申请
    Methods for diagnosis and treatment of MDK1 signal transduction disorders 审中-公开
    MDK1信号转导障碍的诊断和治疗方法

    公开(公告)号：US20060099708A1

    公开(公告)日：2006-05-11

    申请号：US11303935

    申请日：2005-12-19

    申请人： Thomas Ciossek ,  Axel Ullrich ,  Birgit Millauer

    发明人： Thomas Ciossek ,  Axel Ullrich ,  Birgit Millauer

    IPC分类号： C12N5/06 ,  C07K16/40

    CPC分类号： C07K16/40 ,  A61K38/00 ,  C07K14/71

    摘要： The present invention relates to MDK1 polypeptides, nucleic acids encoding such polypeptides, cells, tissues and animals containing such nucleic acids, antibodies to such polypeptides, assays utilizing such polypeptides, and methods relating to all of the foregoing. Methods for treatment, diagnosis, and screening are provided for diseases or conditions characterized by an abnormality in a signal transduction disorder. The signal transduction pathway involves an interaction between a MDK1 receptor tyrosine kinase and a receptor for the kinase. The MDK1 receptor tyrosine kinase may be truncated and lack a kinase domain and may be selected from the group consisting of MDK1.T1, MDK1.T2, MDK1.Δ1 and MDK1.Δ2.

    摘要翻译： 本发明涉及MDK1多肽，编码这种多肽的核酸，含有此类核酸的细胞，组织和动物，对这些多肽的抗体，利用这些多肽的测定法，以及与上述所有相关的方法。 提供治疗，诊断和筛查的方法用于以信号转导障碍异常为特征的疾病或病症。 信号转导途径涉及MDK1受体酪氨酸激酶与激酶受体之间的相互作用。 MDK1受体酪氨酸激酶可能被截短并缺少激酶结构域，并且可以选自MDK1.T1，MDK1T2，MDK1Delta1和MDK1Delta2。