利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

3 条记录 (耗时 0.013 秒)

    Nuclear hormone receptor drug screens
    1.
    发明授权
    Nuclear hormone receptor drug screens 有权
    核激素受体药物筛选

    公开(公告)号：US07101681B1

    公开(公告)日：2006-09-05

    申请号：US09163713

    申请日：1998-09-30

    申请人： Kevin Lustig ,  Patrick Baeuerle ,  Holger Beckmann ,  Jin-Long Chen ,  Bei Shan

    发明人： Kevin Lustig ,  Patrick Baeuerle ,  Holger Beckmann ,  Jin-Long Chen ,  Bei Shan

    IPC分类号： G01N33/53

    CPC分类号： G01N33/74 ,  G01N33/542 ,  G01N2333/575 ,  G01N2333/70567

    摘要： Methods for identifying modulators of nuclear hormone receptor function comprise the steps of (a) forming a mixture comprising a nuclear hormone receptor, a peptide sensor and a candidate agent, but not a natural coactivator protein of the receptor, wherein the sensor provides direct, in vitro binding to the receptor under assay conditions; (b) measuring an agent-biased binding of the sensor to the receptor; and (c) comparing the agent-biased binding with a corresponding unbiased binding of the sensor to the receptor. In particular embodiments, the sensor comprises an amphipathic alpha helix nuclear hormone interacting domain comprising a recited nuclear hormone transcriptional coactivator motif sequence, the sensor is present at sub-micromolar concentration, the binding reaction occurs in solution, the sensor comprises a fluorescent label and the measuring step comprises detecting fluorescence polarization of the label. Reagents include labeled sensor peptides and reaction mixtures consisting essentially of nuclear hormone receptor, a peptide and a candidate agent.

    摘要翻译： 用于鉴定核激素受体功能调节剂的方法包括以下步骤：（a）形成包含核激素受体，肽传感器和候选试剂但不是受体的天然共激活蛋白的混合物，其中所述传感器直接提供 在测定条件下与受体的体外结合; （b）测量传感器与受体的药剂偏置结合; 和（c）将代理偏好的结合与传感器与受体的相应的无偏见的结合进行比较。 在具体实施方案中，传感器包括包含所述核激素转录辅激动子序列的两亲性α螺旋核激素相互作用结构域，所述传感器以亚微摩尔浓度存在，所述结合反应发生在溶液中，所述传感器包含荧光标记和 测量步骤包括检测标签的荧光偏振。 试剂包括标记的传感器肽和基本上由核激素受体，肽和候选试剂组成的反应混合物。

    Nuclear hormone receptor fluorescence polarization assay
    2.
    发明授权
    Nuclear hormone receptor fluorescence polarization assay 失效
    核激素受体荧光偏振测定

    公开(公告)号：US06555326B1

    公开(公告)日：2003-04-29

    申请号：US08975614

    申请日：1997-11-21

    申请人： Kevin Lustig ,  Patrick Baeuerle ,  Holger Beckmann ,  Jin-Long Chen ,  Bei Shan

    发明人： Kevin Lustig ,  Patrick Baeuerle ,  Holger Beckmann ,  Jin-Long Chen ,  Bei Shan

    IPC分类号： G01N3352

    CPC分类号： G01N33/542 ,  G01N33/74 ,  G01N2333/575 ,  G01N2333/70567

    摘要： Methods for identifying modulators of nuclear hormone receptor function comprise the steps of (a) forming a mixture comprising a nuclear hormone receptor, a peptide sensor and a candidate agent, but not a natural coactivator protein of the receptor, wherein the sensor provides direct, in vitro binding to the receptor under assay conditions; (b) measuring an agent-biased binding of the sensor to the receptor; and (c) comparing the agent-biased binding with a corresponding unbiased binding of the sensor to the receptor. In particular embodiments, the sensor comprises an amphipathic alpha helix nuclear hormone interacting domain comprising a recited nuclear hormone transcriptional coactivator motif sequence, the sensor is present at sub-micromolar concentration, the binding reaction occurs in solution, the sensor comprises a fluorescent label and the measuring step comprises detecting fluorescence polarization of the label. Reagents include labeled sensor peptides and reaction mixtures consisting essentially of nuclear hormone receptor, a peptide and a candidate agent.

    摘要翻译： 用于鉴定核激素受体功能调节剂的方法包括以下步骤：（a）形成包含核激素受体，肽传感器和候选试剂但不是受体的天然共激活蛋白的混合物，其中所述传感器直接提供 在测定条件下与受体的体外结合; （b）测量传感器与受体的药剂偏置结合; 和（c）将代理偏好的结合与传感器与受体的相应的无偏见的结合进行比较。 在具体实施方案中，传感器包括包含所述核激素转录辅激动子序列的两亲性α螺旋核激素相互作用结构域，所述传感器以亚微摩尔浓度存在，所述结合反应发生在溶液中，所述传感器包含荧光标记和 测量步骤包括检测标签的荧光偏振。 试剂包括标记的传感器肽和基本上由核激素受体，肽和候选试剂组成的反应混合物。