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    NICOTINIC ACID RECEPTOR LIGANDS
    1.
    发明申请
    NICOTINIC ACID RECEPTOR LIGANDS 审中-公开

    公开(公告)号：US20110071198A1

    公开(公告)日：2011-03-24

    申请号：US12736966

    申请日：2009-05-27

    申请人： Robert J. Lefkowitz ,  Scott M. Dewire ,  Erin J. Whalen ,  Jonathan D. Violin ,  Robert W. Walters

    发明人： Robert J. Lefkowitz ,  Scott M. Dewire ,  Erin J. Whalen ,  Jonathan D. Violin ,  Robert W. Walters

    IPC分类号： A61K31/455 ,  G01N33/53 ,  A61P9/10 ,  A61P3/06

    CPC分类号： G01N33/566 ,  C07K14/705 ,  G01N2333/726 ,  G01N2800/044

    摘要： The present invention relates, in general, to nicotinic acid receptor ligands and, in particular, to ligands that have a relative efficacy for activating a G-protein-coupled receptor function (e.g., signaling) that is greater than their relative efficacy for stimulating β-arrestin function (e.g., recruitment and/or signaling). The invention further relates to the use of such “biased ligands” to decrease triglycerides levels and to potentially increase high density lipoprotein (HDL) levels in patients and potentially lower low density lipoprotein (LDL) and/or very low density lipoprotein (VLDL) levels. In addition, the invention relates to methods of identifying such “biased ligands”.

    摘要翻译： 本发明一般涉及烟酸受体配体，特别是涉及具有激活G蛋白偶联受体功能（例如，信号传导）的相对功效的配体，其大于它们对刺激作用的相对功效 ; -arrestin功能（例如招聘和/或信令）。 本发明还涉及这种“有偏配体”降低甘油三酯水平并潜在地增加患者中高密度脂蛋白（HDL）水平以及潜在地降低低密度脂蛋白（LDL）和/或极低密度脂蛋白（VLDL）水平的用途 。 此外，本发明涉及鉴定这种“有偏配体”的方法。

    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
    8.
    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。