Utilization of histamine receptor h3 gene participating in body weight or food intake control
    3.
    发明授权
    Utilization of histamine receptor h3 gene participating in body weight or food intake control 失效
    利用组胺受体h3基因参与体重或食物摄取控制

    公开(公告)号:US07767881B2

    公开(公告)日:2010-08-03

    申请号:US10482464

    申请日:2002-06-28

    摘要: To clarify histamine receptor H3 protein function in vivo, the present inventors constructed a nonhuman higher animal in which the expression of a histamine receptor H3 gene was artificially inhibited. As a result, the present inventors found that this nonhuman higher animal showed increased body weight, food intake, blood insulin level, or blood leptin level compared with a control. Thus, the present inventors found that abnormalities in the histamine receptor H3 protein relate to diseases characterized by changes in body weight or food intake, and this has made it possible to screen drugs for treatment or prevention of these diseases, and to examine these diseases.

    摘要翻译: 为了在体内阐明组胺受体H3蛋白功能,本发明人构建了人体高效动物,其中组胺受体H3基因的表达被人为抑制。 结果,本发明人发现,与对照相比,该非人类高等动物的体重,食物摄取量,血液胰岛素水平或血液瘦素水平增加。 因此,本发明人发现组胺受体H3蛋白质的异常与以体重或食物摄取为特征的疾病有关,能够筛选用于治疗或预防这些疾病的药物,并检查这些疾病。

    METHOD OF ASSUMING DRUG SENSITIVITY TO CDK4 INHIBITOR
    4.
    发明申请
    METHOD OF ASSUMING DRUG SENSITIVITY TO CDK4 INHIBITOR 审中-公开
    对CDK4抑制剂的药物敏感性的方法

    公开(公告)号:US20090081645A1

    公开(公告)日:2009-03-26

    申请号:US11659258

    申请日:2005-08-02

    IPC分类号: C12Q1/68 C12N15/11 C07K16/18

    CPC分类号: C12Q1/485

    摘要: It is intended to provide a gene for assuming drug sensitivity, which is to be used for assuming the drug sensitivity to a CDK4 inhibitor based on the expression amount in a test tissue or a test cell, selected from the group consisting of p16 gene, p18 gene and p27 gene. It is also intended to provide a method of assuming the drug sensitivity to a CDK4 inhibitor by using the expression amount of the above gene in a test tissue or a test cell as an indication.

    摘要翻译: 旨在提供用于假定药物敏感性的基因,其用于基于在选自p16基因,p18的测试组织或测试细胞中的表达量来假定对CDK4抑制剂的药物敏感性 基因和p27基因。 还旨在提供一种通过使用在测试组织或测试细胞中的上述基因的表达量作为指示来确定对CDK4抑制剂的药物敏感性的方法。

    Constitutively active histamine H3 receptor mutants and uses thereof
    5.
    发明授权
    Constitutively active histamine H3 receptor mutants and uses thereof 失效
    组胺活性组胺H3受体突变体及其用途

    公开(公告)号:US07279293B2

    公开(公告)日:2007-10-09

    申请号:US10512240

    申请日:2003-04-23

    摘要: Internal domain 3 of seven transmembrane G protein-coupled receptors is important for G protein binding or receptor activity, and is well conserved. In H3 receptors, which are a type of G protein-coupled receptor, this region is also conserved in the same way. Therefore, as a result of using PCR to introduce point mutations into sequences encoding the region in H3 receptor cDNA, H3 receptor mutants comprising extremely strong constitutive activity could be successfully produced. The present inventors further found that by using constitutively active H3 receptor mutants, drug candidate compounds such as H3 receptor inverse agonists can be screened more easily and efficiently.

    摘要翻译: 七个跨膜G蛋白偶联受体的内部结构域3对于G蛋白结合或受体活性是重要的,并且是保守的。 在作为G蛋白偶联受体类型的H3受体中,该区域也以相同的方式保守。 因此,作为使用PCR将点突变引入编码H3受体cDNA中的区域的序列的结果,可以成功制备包含极强组成活性的H3受体突变体。 本发明人进一步发现,通过使用组成型活性H3受体突变体,可以更容易且有效地筛选候选药物如H3受体反向激动剂。

    Histamine receptor h3 ordinary activity mutant and utilization thereof
    10.
    发明申请
    Histamine receptor h3 ordinary activity mutant and utilization thereof 失效
    组胺受体h3普通活性突变体及其利用

    公开(公告)号:US20050234223A1

    公开(公告)日:2005-10-20

    申请号:US10512240

    申请日:2003-04-23

    摘要: Internal domain 3 of seven transmembrane G protein-coupled receptors is important for G protein binding or receptor activity, and is well conserved. In H3 receptors, which are a type of G protein-coupled receptor, this region is also conserved in the same way. Therefore, as a result of using PCR to introduce point mutations into sequences encoding the region in H3 receptor cDNA, H3 receptor mutants comprising extremely strong constitutive activity could be successfully produced. The present inventors further found that by using constitutively active H3 receptor mutants, drug candidate compounds such as H3 receptor inverse agonists can be screened more easily and efficiently.

    摘要翻译: 七个跨膜G蛋白偶联受体的内部结构域3对于G蛋白结合或受体活性是重要的,并且是保守的。 在作为G蛋白偶联受体类型的H3受体中,该区域也以相同的方式保守。 因此,作为使用PCR将点突变引入编码H3受体cDNA中的区域的序列的结果,可以成功制备包含极强组成活性的H3受体突变体。 本发明人进一步发现,通过使用组成型活性H3受体突变体,可以更容易且有效地筛选候选药物如H3受体反向激动剂。