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41 条记录 (耗时 0.023 秒)

    Method of detecting inhibitors of agonist-specific desensitization
    2.
    发明授权
    Method of detecting inhibitors of agonist-specific desensitization 失效
    检测激动剂特异性脱敏抑制剂的方法

    公开(公告)号：US06605424B1

    公开(公告)日：2003-08-12

    申请号：US09568983

    申请日：2000-05-11

    申请人： Robert J. Lefkowitz ,  Martin J. Lohse ,  Jeffrey L. Benovic ,  Marc G. Caron

    发明人： Robert J. Lefkowitz ,  Martin J. Lohse ,  Jeffrey L. Benovic ,  Marc G. Caron

    IPC分类号： C12Q300

    CPC分类号： A61K31/715 ,  A61K31/21 ,  A61K31/66 ,  A61K31/675 ,  A61K38/1787 ,  G01N33/566 ,  G01N33/573

    摘要： The present invention relates to a method of inhibiting desensitization of a cell to the effects of a compound. The method comprises contacting the cell with an agent capable of inhibiting phosphorylation, by a protein kinase, of a receptor for the compound present on the surface of the cell. The present invention also relates to a method of screening a compound for its ability to inhibit desensitization. The method comprises: i) contacting a receptor specific kinase-containing sample with the compound under conditions such that interaction between receptor specific kinase present in the sample and the compound can occur, and ii) determining the ability of the receptor specific kinase to phosphorylate the receptor for which it is specific.

    摘要翻译： 本发明涉及抑制细胞对化合物作用的脱敏的方法。 该方法包括使细胞与能够通过蛋白激酶抑制存在于细胞表面的化合物的受体的磷酸化的试剂接触。 本发明还涉及一种筛选化合物抑制脱敏能力的方法。 该方法包括：i）使受体特异性激酶样品与化合物在使得存在于样品中的受体特异性激酶与化合物之间发生相互作用的条件下接触，以及ii）确定受体特异性激酶使受体磷酸化的能力 它是具体的。

    Expression of G protein coupled receptors in yeast
    6.
    发明授权
    Expression of G protein coupled receptors in yeast 失效
    酵母中G蛋白偶联受体的表达

    公开(公告)号：US06168927A

    公开(公告)日：2001-01-02

    申请号：US09056920

    申请日：1998-04-08

    申请人： Klim King ,  Henrik G. Dohlman ,  Marc G. Caron ,  Robert J. Lefkowitz

    发明人： Klim King ,  Henrik G. Dohlman ,  Marc G. Caron ,  Robert J. Lefkowitz

    IPC分类号： G01N3353

    CPC分类号： G01N33/566 ,  C07K14/39 ,  C07K14/4722 ,  C07K14/70571 ,  C07K2319/00 ,  C07K2319/02 ,  C07K2319/32 ,  C07K2319/61 ,  C07K2319/705 ,  C12N15/81 ,  C12Q1/6897 ,  G01N2333/726 ,  G01N2500/00

    摘要： Disclosed is a transformed yeast cell containing a first heterologous DNA sequence which codes for a mammalian G protein coupled receptor and a second heterologous DNA sequence which codes for a mammalian G protein &agr; subunit (mammalian G&agr;). The first and second heterologous DNA sequences are capable of expression in the cell, but the cell is incapable of expressing an endogenous G protein &agr;-subunit (yeast G&agr;) The cells are useful for screening compounds which affect the rate of dissociation of G&agr; from G&bgr;&ggr; in a cell. Also disclosed is a novel DNA expression vector useful for making cells as described above. The vector contains a first segment comprising at least a fragment of the extreme amino-terminal coding sequence of a yeast G protein coupled receptor. A second segment is positioned downstream from the first segment (and in correct reading frame therewith), with the second segment comprising a DNA sequence encoding a heterologous G protein coupled receptor.

    摘要翻译： 公开了含有编码哺乳动物G蛋白偶联受体的第一异源DNA序列和编码哺乳动物G蛋白α亚基（哺乳动物Galpha）的第二异源DNA序列的转化酵母细胞。 第一和第二异源DNA序列能够在细胞中表达，但是细胞不能表达内源性G蛋白α亚基（酵母Galpha）。细胞可用于筛选影响Galeta从Gbetagamma分离速率的化合物 在一个单元格 还公开了用于如上所述制备细胞的新型DNA表达载体。 载体含有至少包含酵母G蛋白偶联受体的极端氨基末端编码序列的片段的第一片段。 第二片段位于第一片段的下游（并且在其正确的阅读框架中），其中第二片段包含编码异源G蛋白偶联受体的DNA序列。

    Adrenergic receptor as a proto-oncogene
    7.
    发明授权
    Adrenergic receptor as a proto-oncogene 失效
    肾上腺素受体作为原癌基因

    公开(公告)号：US5573908A

    公开(公告)日：1996-11-12

    申请号：US170684

    申请日：1993-12-20

    申请人： Lee F. Allen ,  Robert J. Lefkowitz ,  Marc G. Caron ,  Susanna Cotecchia

    发明人： Lee F. Allen ,  Robert J. Lefkowitz ,  Marc G. Caron ,  Susanna Cotecchia

    IPC分类号： C07K14/705 ,  G01N33/50 ,  G01N33/94 ,  C12Q1/68 ,  C12N5/10

    CPC分类号： G01N33/5011 ,  C07K14/70571 ,  G01N33/9433 ,  G01N2500/10

    摘要： A recombinant cell comprising a host cell containing a recombinant DNA sequence is disclosed. The recombinant DNA sequence comprises vector DNA and DNA which encodes a mammalian adrenergic receptor. The host cell is one capable of undergoing proliferation in response to activation of the adrenergic receptor. In one specific embodiment of the foregoing, the adrenergic receptor includes a mutation in the third cytoplasmic loop thereof which renders the adrenergic receptor constitutively active, and the host cell undergoes proliferation in response to the constitutively active adrenergic receptor. Also disclosed are in vitro assays employing the foregoing which are useful for screening test compounds for antitumor and antiatherogenic activity, along with a diagnostic assay for detecting the oncogenic activation of cells in a patient. The diagnostic assay comprises collecting sample cells which express adrenergic receptors from the patient, and then detecting the presence or absence of a mutation in the adrenergic receptor which renders the receptor constitutively active. The presence of such a mutation indicates the oncogenic activation of the cells.

    摘要翻译： 公开了包含含有重组DNA序列的宿主细胞的重组细胞。 重组DNA序列包含编​​码哺乳动物肾上腺素能受体的载体DNA和DNA。 宿主细胞是能够响应于肾上腺素能受体活化而经历增殖的宿主细胞。 在上述的一个具体实施方案中，肾上腺素能受体包括其第三细胞质环中的突变，其使肾上腺素能受体组成型活性，并且宿主细胞响应于组成型活性肾上腺素能受体而经历增殖。 还公开了使用前述的体外测定法，其用于筛选测试化合物的抗肿瘤和抗动脉粥样硬化活性，以及​​用于检测患者细胞的致癌活化的诊断测定法。 诊断测定包括收集从患者中表达肾上腺素能受体的样品细胞，然后检测肾上腺素能受体中存在或不存在使得受体组成型活性的突变。 这种突变的存在表明细胞的致癌活化。

    Expression of G protein coupled receptors in yeast
    8.
    发明授权
    Expression of G protein coupled receptors in yeast 失效
    酵母中G蛋白偶联受体的表达

    公开(公告)号：US07413876B2

    公开(公告)日：2008-08-19

    申请号：US10997069

    申请日：2004-11-23

    申请人： Klim King ,  Henrick G. Dohlman ,  Marc G. Caron ,  Robert J. Lefkowitz

    发明人： Klim King ,  Henrick G. Dohlman ,  Marc G. Caron ,  Robert J. Lefkowitz

    IPC分类号： C12N1/19 ,  C07K14/705

    CPC分类号： G01N33/566 ,  C07K14/39 ,  C07K14/4722 ,  C07K14/70571 ,  C07K2319/00 ,  C07K2319/02 ,  C07K2319/32 ,  C07K2319/61 ,  C07K2319/705 ,  C12N15/81 ,  C12Q1/6897 ,  G01N2333/726 ,  G01N2500/00

    摘要： Disclosed is a transformed yeast cell containing a first heterologous DNA sequence which codes for a mammalian G protein-coupled receptor and a second heterologous DNA sequence which codes for a mammalian G protein α subunit (mammalian Gα). The first and second heterologous DNA sequences are capable of expression in the cell, but the cell is incapable of expressing an endogenous G protein α-subunit (yeast Gα). The cells are useful for screening compounds which affect the rate of dissociation of Gα from Gβγ in a cell. Also disclosed is a novel DNA expression vector useful for making cells as described above. The vector contains a first segment comprising at least a fragment of the extreme amino-terminal coding sequence of a yeast G protein-coupled receptor. A second segment is positioned downstream from the first segment (and in correct reading frame therewith), with the second segment comprising a DNA sequence encoding a heterologous G protein-coupled receptor.

    摘要翻译： 公开了含有编码哺乳动物G蛋白偶联受体的第一异源DNA序列和编码哺乳动物G蛋白α亚基（哺乳动物细胞）的第二异源DNA序列的转化酵母细胞。 第一和第二异源DNA序列能够在细胞中表达，但是细胞不能表达内源性G蛋白α亚基（酵母Gαα）。 这些细胞可用于筛选化合物，这些化合物影响来自细胞中的β-氨基酸的解离速率。 还公开了用于如上所述制备细胞的新型DNA表达载体。 载体含有至少包含酵母G蛋白偶联受体的极端氨基末端编码序列的片段的第一片段。 第二片段位于第一片段的下游（并且在其正确的阅读框架中），第二片段包含编码异源G蛋白偶联受体的DNA序列。