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    In Vitro screening for ligands of the estrogen receptor
    1.
    发明授权
    In Vitro screening for ligands of the estrogen receptor 失效
    体外筛选雌激素受体配体

    公开(公告)号：US07166438B2

    公开(公告)日：2007-01-23

    申请号：US09989952

    申请日：2001-11-20

    申请人： Vladimir Patchev ,  Youriy Mitev ,  Siegmund Wolf ,  Gernot Langer

    发明人： Vladimir Patchev ,  Youriy Mitev ,  Siegmund Wolf ,  Gernot Langer

    IPC分类号： G01N33/53

    CPC分类号： G01N33/743 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2500/10 ,  G01N2500/20

    摘要： A method for in vitro screening a group of test substances for a ligand using two assay systems, i.e. a cellular or tissue assay system and an enzymatic assay system, is described. First, those test substances are selected which have transcriptional ER-mediated activity measured by an ER-driven reporter gene in the cellular or tissue assay system with an EC50(ER)(half-maximally effective ligand concentration) lower than or equal to 10 nmol/l. Then in an enzymatic assay system the selected test substances having the required transcriptional ER-mediated activity are tested by measuring a physical-chemical interaction (recruitment) of SRC-1 and the ER in the presence of the test substances. The selected ligand activates the ER and induces interaction with the co-present SRC-1 with an E50(ER+SRC) higher than or equal to 100 nmol/l. The ligands found by the inventive screening method are useful for treatment and prevention of neuro-degeneration in the cerebral cortex, especially of age-related cognitive disorders, affective disorders, Alzheimer's diseases and cerebral ischemia/stroke.

    摘要翻译： 描述了使用两个测定系统（即细胞或组织测定系统和酶测定系统）体外筛选配体的一组测试物质的方法。 首先，选择在细胞或组织测定系统中通过ER驱动的报告基因测量的具有转录ER介导活性的测试物质，其具有EC 50（ER）（半最大有效配体浓度 ）低于或等于10nmol / l。 然后在酶分析系统中，通过测量在存在测试物质的情况下测量SRC-1和ER的物理 - 化学相互作用（招募）来测试所选择的具有所需转录ER介导活性的测试物质。 选择的配体激活ER并诱导与共同存在的SRC-1与高于或等于100nmol / l的E 50（ER + SRC）的相互作用。 通过本发明筛选方法发现的配体可用于治疗和预防大脑皮质中的神经变性，特别是与年龄相关的认知障碍，情感障碍，阿尔茨海默病和脑缺血/卒中。