Nuclear hormone receptor fluorescence polarization assay
    1.
    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

    IPC分类号: G01N3352

    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 drug screens
    2.
    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

    IPC分类号: G01N33/53

    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。

    Detection method for monitoring &bgr; tubulin isotype specific modification
    6.
    发明授权
    Detection method for monitoring &bgr; tubulin isotype specific modification 失效
    检测β微管蛋白同种型特异性修饰的检测方法

    公开(公告)号:US06306615B1

    公开(公告)日:2001-10-23

    申请号:US09377554

    申请日:1999-08-19

    IPC分类号: C12Q100

    CPC分类号: G01N33/68 C07K16/18

    摘要: This invention relates to monoclonal antibodies that recognize modified &bgr;-tubulin isotypes, methods of using such antibodies to detect modified &bgr;-tubulin isotypes, methods of using such antibodies to monitor &bgr;-tubulin modifying agents administered to a patient, methods of using such antibodies to isolate modified &bgr;-tubulin, and methods of detecting the anti-modified &bgr;-tubulin antibodies.

    摘要翻译: 本发明涉及识别修饰的β-微管蛋白同种型的单克隆抗体,使用这种抗体以检测修饰的β-微管蛋白同种型的方法,使用此类抗体监测给予患者的β-微管蛋白调节剂的方法,使用这种抗体的方法 分离修饰的β-微管蛋白,以及检测抗修饰β-微管蛋白抗体的方法。