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1. 发明申请

WO2004005550A3 METHOD OF SCREENING FOR ANTIDIABETIC AGENTS 审中-公开
标题翻译：抗生素代谢筛选方法
公开(公告)号：WO2004005550A3
公开(公告)日：2004-04-15
申请号：PCT/JP0308523
申请日：2003-07-04
申请人： FUJISAWA PHARMACEUTICAL CO , FUJIMURA TAKAO , SAKUMA HIROYUKI , KIMURA CHIAKI , OE TOMOYA , ARAMORI ICHIRO
发明人： FUJIMURA TAKAO , SAKUMA HIROYUKI , KIMURA CHIAKI , OE TOMOYA , ARAMORI ICHIRO
IPC分类号： A61P3/08 , G01N33/50 , G01N33/68 , G01N33/92
CPC分类号： G01N33/5044 , G01N33/5008 , G01N33/5023 , G01N33/6872 , G01N33/92 , G01N2333/70567 , G01N2800/042
摘要： A method of screening for an antidiabetic agent that lowers blood glucose level without inducing obesity and/or insulin resistance, is provided. The method comprises measuring the expression level of a nuclear peroxisome proliferator-activated receptor g (PPARg)-induced adipogenic gene in mature adipocytes in the presence of a test compound or a PPARg full agonist and selecting a compound that results in an expression level significantly lower than that measured using the PPARg full agonist. The method may further comprise the same steps except for using differentiating adipocytes to select a compound that results in an expression level comparable to or higher than that measured using the PPARg full agonist. A kit used for the above screening method, a compound obtainable by the screening method, a pharmaceutical composition containing such a compound, and a method lowering the blood glucose level without causing obesity and/or insulin resistance using the compound, are also provided.
摘要翻译：提供了筛选降低血糖水平而不诱导肥胖和/或胰岛素抵抗的抗糖尿病药的方法。该方法包括在受试化合物或PPARg全激动剂的存在下测量成熟脂肪细胞中核过氧化物酶体增殖物激活受体g（PPARg）诱导的脂肪形成基因的表达水平，并选择导致表达水平显着降低的化合物比使用PPARg全激动剂测量的。该方法可以进一步包括相同的步骤，除了使用分化脂肪细胞来选择导致与使用PPARg全激动剂测量的表达水平相当或更高的表达水平的化合物。还提供了用于上述筛选方法的试剂盒，通过筛选方法获得的化合物，含有这种化合物的药物组合物，以及使用该化合物降低血糖水平而不引起肥胖和/或胰岛素抵抗的方法。

2. 发明申请

WO2004005550A2 METHOD OF SCREENING FOR ANTIDIABETIC AGENTS 审中-公开
标题翻译：筛选抗糖尿病药物的方法
公开(公告)号：WO2004005550A2
公开(公告)日：2004-01-15
申请号：PCT/JP2003/008523
申请日：2003-07-04
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , FUJIMURA, Takao , SAKUMA, Hiroyuki , KIMURA, Chiaki , OE, Tomoya , ARAMORI, Ichiro
发明人： FUJIMURA, Takao , SAKUMA, Hiroyuki , KIMURA, Chiaki , OE, Tomoya , ARAMORI, Ichiro
IPC分类号： C12Q1/68
CPC分类号： G01N33/5044 , G01N33/5008 , G01N33/5023 , G01N33/6872 , G01N33/92 , G01N2333/70567 , G01N2800/042
摘要： A method of screening for an antidiabetic agent that lowers blood glucose level without inducing obesity and/or insulin resistance, is provided. The method comprises measuring the expression level of a nuclear peroxisome proliferator-activated receptor g (PPARg)-induced adipogenic gene in mature adipocytes in the presence of a test compound or a PPARg full agonist and selecting a compound that results in an expression level significantly lower than that measured using the PPARg full agonist. The method may further comprise the same steps except for using differentiating adipocytes to select a compound that results in an expression level comparable to or higher than that measured using the PPARg full agonist. A kit used for the above screening method, a compound obtainable by the screening method, a pharmaceutical composition containing such a compound, and a method lowering the blood glucose level without causing obesity and/or insulin resistance using the compound, are also provided.
摘要翻译：提供了筛选降低血糖水平而不诱导肥胖症和/或胰岛素抵抗的抗糖尿病药的方法。该方法包括在测试化合物或PPARg全激动剂存在下测量成熟脂肪细胞中核过氧化物酶体增殖物激活受体g（PPARg）诱导的脂肪形成基因的表达水平，并选择导致表达水平显着降低比使用PPARg完全激动剂测得的值更高。除了使用分化脂肪细胞来选择导致与使用PPARg完全激动剂测量的表达水平相当或更高的表达水平的化合物之外，该方法可以进一步包括相同的步骤。还提供了用于上述筛选方法的试剂盒，通过筛选方法获得的化合物，含有该化合物的药物组合物以及使用该化合物降低血糖水平而不引起肥胖症和/或胰岛素抵抗的方法。 / p>

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