TEST SYSTEMS, METHODS AND USES INVOLVING AS160 PROTEIN
    1.
    发明申请
    TEST SYSTEMS, METHODS AND USES INVOLVING AS160 PROTEIN 审中-公开
    涉及AS160蛋白质的测试系统,方法和用途

    公开(公告)号:US20120108464A1

    公开(公告)日:2012-05-03

    申请号:US13142869

    申请日:2010-01-27

    摘要: The present invention relates to a method of identifying a substance altering glucose uptake and/or GLUT4 translocation to the plasma membrane of a cell comprising contacting a test system comprising AKT substrate 160 kDa-protein (AS160-protein) with a test substance, and identifying a test substance as a substance altering glucose uptake of a cell by detecting a signal indicative for altered glucose uptake of a cell; a test system comprising a gene coding for the AKT substrate 160 kDa-protein (AS160-protein) and an inducible promoter providing for controllable expression of the gene; the use of the test system for the identification of a substance improving glucose uptake and/or GLUT4 translocation to the plasma membrane of a cell; and the use of AS 160-protein in a model for type 2 diabetes.

    摘要翻译: 本发明涉及一种鉴定改变葡萄糖摄取和/或GLUT4易位于细胞质膜的物质的方法,所述方法包括将包含AKT底物160kDa蛋白(AS160-蛋白)的测试系统与测试物质接触,并鉴定 作为通过检测指示细胞葡萄糖摄取变化的信号改变细胞葡萄糖摄取的物质的测试物质; 包括编码AKT底物160kDa蛋白(AS160-蛋白)的基因和提供该基因的可控表达的诱导型启动子的测试系统; 使用测试系统来鉴定改善葡萄糖摄取和/或GLUT4易位于细胞质膜的物质; 以及在2型糖尿病模型中使用AS 160蛋白。

    NOVEL AS160-LIKE PROTEIN, TEST SYSTEMS, METHODS AND USES INVOLVING IT FOR THE IDENTIFICATION OF DIABETES TYPE 2 THERAPEUTICS
    2.
    发明申请
    NOVEL AS160-LIKE PROTEIN, TEST SYSTEMS, METHODS AND USES INVOLVING IT FOR THE IDENTIFICATION OF DIABETES TYPE 2 THERAPEUTICS 审中-公开
    新型AS160型蛋白质,测试系统,涉及其用于鉴定糖尿病2型治疗药物的方法和用途

    公开(公告)号:US20100256014A1

    公开(公告)日:2010-10-07

    申请号:US12667772

    申请日:2008-07-23

    摘要: The present invention relates to novel AKT substrate 160 kDa-like protein (AS160-like protein), to a method of identifying a substance altering glucose uptake and/or GLUT4 translocation to the plasma membrane of a cell comprising contacting a test system comprising AKT substrate 160 kDa-like protein (AS160-like protein) with a test substance, and identifying a test substance as a substance altering glucose uptake of a cell by detecting a signal indicative for altered glucose uptake of a cell; a test system comprising a gene coding for the AKT substrate 160 kDa-like protein (AS 160-like protein) and an inducible promoter providing for controllable expression of the gene; the use of the test system for the identification of a substance improving glucose uptake and/or GLUT4 translocation to the plasma membrane of a cell; and the use of AS160-like protein in a model for type 2 diabetes.

    摘要翻译: 本发明涉及新型AKT底物160kDa样蛋白(AS160样蛋白),用于鉴定改变葡萄糖摄取和/或GLUT4移位至细胞质膜的物质的方法,包括使包含AKT底物的测试系统 具有测试物质的160kDa样蛋白(AS160样蛋白),并通过检测指示细胞葡萄糖摄取变化的信号,将测试物质鉴定为改变细胞葡萄糖摄取的物质; 包括编码AKT底物160kDa样蛋白(AS160样蛋白)的基因和提供该基因的可控表达的诱导型启动子的测试系统; 使用测试系统来鉴定改善葡萄糖摄取和/或GLUT4易位于细胞质膜的物质; 以及在2型糖尿病模型中使用AS160样蛋白。

    Azolopyridin-2-one derivatives as lipase and phospholipase inhibitors
    7.
    发明授权
    Azolopyridin-2-one derivatives as lipase and phospholipase inhibitors 有权
    偶氮吡啶-2-酮衍生物作为脂肪酶和磷脂酶抑制剂

    公开(公告)号:US07846943B2

    公开(公告)日:2010-12-07

    申请号:US11950932

    申请日:2007-12-05

    CPC分类号: C07D498/04

    摘要: The present invention provides compounds which have an inhibitory effect on hormone-sensitive lipase or endothelial lipase. The compounds of the invention are azolopyridin-2-one derivatives of the general formula I wherein the substituents are as defined herein. The compounds of formula I wherein R2 is hydrogen are distinguished by favorable effects on disorders of lipid metabolism. They beneficially influence the HDL to LDL ratio and increase in particular the HDL level and are suitable for the prevention and treatment of dyslipidemias and metabolic syndrome and their diverse sequelae such as atherosclerosis, coronary heart disease, heart failure, obesity and diabetes. The compounds of formula I wherein R1 and R2 together form a ring system are distinguished by favorable effects on metabolic disorders. They beneficially influence lipid and sugar metabolism; in particular they lower the triglyceride level and are suitable for the prevention and treatment of type II diabetes and arteriosclerosis and the diverse sequelae thereof.

    摘要翻译: 本发明提供对激素敏感性脂肪酶或内皮脂肪酶具有抑制作用的化合物。 本发明的化合物是通式I的偶氮吡啶-2-酮衍生物,其中取代基如本文所定义。 其中R2是氢的式I化合物的特征在于对脂质代谢紊乱的有利影响。 它们有利地影响HDL与LDL的比例,特别是HDL水平的升高,适用于预防和治疗血脂异常和代谢综合征及其各种后遗症如动脉粥样硬化,冠心病,心力衰竭,肥胖和糖尿病。 其中R1和R2一起形成环系的式I化合物的特征在于对代谢紊乱的有利影响。 它们有利地影响脂质和糖代谢; 特别是它们降低甘油三酯水平,并且适合于预防和治疗II型糖尿病和动脉硬化及其各种后遗症。