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    Mechanism based screen for retinoid X receptor agonists and antagonists
    1.
    发明授权
    Mechanism based screen for retinoid X receptor agonists and antagonists 失效
    类维生素X受体激动剂和拮抗剂的机制筛选

    公开(公告)号：US5700682A

    公开(公告)日：1997-12-23

    申请号：US465783

    申请日：1995-06-06

    申请人： Paul Mak ,  Sotirios K. Karathanasis

    发明人： Paul Mak ,  Sotirios K. Karathanasis

    IPC分类号： C07K14/705 ,  C07K14/775 ,  C12N1/21 ,  C12N15/09 ,  C12Q1/02 ,  C12Q1/68 ,  C12R1/19 ,  G01N33/566

    CPC分类号： G01N33/566 ,  C07K14/70567 ,  C07K14/775 ,  C12Q1/6897 ,  G01N2333/395 ,  G01N2333/70567 ,  G01N2500/00

    摘要： A method is described for screening retinoid X receptor agonists or antagonists using a retinoid X receptor expressed by a yeast expression system to screen a compound having a retinoid X receptor agonist or antagonist activity. Another screen is described for detecting a compound having retinoid X receptor agonist or antagonist activity by: (1) providing a yeast strain which expresses the retinoic acid receptor and activates a reporter plasmid containing apolipoprotein AI gene site A or a mutated variant thereof; (2) incubating the compound in suitable media and a colorless chromogenic substrate; and (3) examining the media for development of color. Mutated variants of apolipoprotein AI gene site A which respond selectively to the retinoid X receptor or respond to receptors other than RXR.alpha. are also described.

    摘要翻译： 描述了使用由酵母表达系统表达的类视黄醇X受体筛选视黄醇X受体激动剂或拮抗剂以筛选具有类视黄醇X受体激动剂或拮抗剂活性的化合物的方法。 描述了另一个用于通过以下方式检测具有类视黄醇X受体激动剂或拮抗剂活性的化合物：（1）提供表达视黄酸受体并激活含有载脂蛋白AI基因位点A或其突变变体的报道质粒的酵母菌株; （2）将化合物在合适的培养基和无色的显色底物中孵育; 和（3）检查媒体的颜色发展。 还描述了对视黄酸X受体或对RXRα以外的受体有反应的载脂蛋白AI基因位点A的突变变体。

    Mechanism-based screen for retinoid X receptor agonists and antagonists
    2.
    发明授权
    Mechanism-based screen for retinoid X receptor agonists and antagonists 失效
    类维生素X受体激动剂和拮抗剂的机制筛选

    公开(公告)号：US5700650A

    公开(公告)日：1997-12-23

    申请号：US469122

    申请日：1995-06-06

    申请人： Paul Mak ,  Sotirios K. Karathanasis

    发明人： Paul Mak ,  Sotirios K. Karathanasis

    IPC分类号： C07K14/705 ,  C07K14/775 ,  C12N1/21 ,  C12N15/09 ,  C12Q1/02 ,  C12Q1/68 ,  C12R1/19 ,  G01N33/566

    CPC分类号： G01N33/566 ,  C07K14/70567 ,  C07K14/775 ,  C12Q1/6897 ,  G01N2333/395 ,  G01N2333/70567 ,  G01N2500/00

    摘要： A method is described for screening retinoid X receptor agonists or antagonists using a retinoid X receptor expressed by a yeast expression system to screen a compound having a retinoid X receptor agonist or antagonist activity. Another screen is described for detecting a compound having retinoid X receptor agonist or antagonist activity by: (1) providing a yeast strain which expresses the retinoic acid receptor and activates a reporter plasmid containing apolipoprotein AI gene site A or a mutated variant thereof; (2) incubating the compound in suitable media and a colorless chromogenic substrate; and (3) examining the media for development of color. Mutated variants of apolipoprotein AI gene site A which respond selectively to the retinoid X receptor or respond to receptors other than RXR.alpha. are also described.

    摘要翻译： 描述了使用由酵母表达系统表达的类视黄醇X受体筛选视黄醇X受体激动剂或拮抗剂以筛选具有类视黄醇X受体激动剂或拮抗剂活性的化合物的方法。 描述了另一个用于通过以下方式检测具有类视黄醇X受体激动剂或拮抗剂活性的化合物：（1）提供表达视黄酸受体并激活含有载脂蛋白AI基因位点A或其突变变体的报道质粒的酵母菌株; （2）将化合物在合适的培养基和无色的显色底物中孵育; 和（3）检查媒体的颜色发展。 还描述了对视黄酸X受体或对RXRα以外的受体有反应的载脂蛋白AI基因位点A的突变变体。

    Recombinant nucleic acid containing a response element
    3.
    发明授权
    Recombinant nucleic acid containing a response element 失效
    含有响应元件的重组核酸

    公开(公告)号：US5691196A

    公开(公告)日：1997-11-25

    申请号：US999071

    申请日：1992-12-31

    申请人： Paul Mak ,  Sotirios K. Karathanasis

    发明人： Paul Mak ,  Sotirios K. Karathanasis

    IPC分类号： C07K14/705 ,  C07K14/775 ,  C12N1/21 ,  C12N15/09 ,  C12Q1/02 ,  C12Q1/68 ,  C12R1/19 ,  G01N33/566 ,  C12N15/63 ,  C12N15/11

    CPC分类号： G01N33/566 ,  C07K14/70567 ,  C07K14/775 ,  C12Q1/6897 ,  G01N2333/395 ,  G01N2333/70567 ,  G01N2500/00

    摘要： The present invention describes a novel method for screening retinoid X receptor agonists or antagonists, comprising: using a retinoid X receptor expressed by a yeast expression system to screen a compound having a retinoid X receptor agonist or antagonist activity as well as a screen for detecting a compound having retinoid X receptor agonist or antagonist activity, which comprises the steps of (1) providing a yeast strain which expresses the retinoic acid receptor and activates a reporter plasmid containing apolipoprotein AI gene site A or a mutated variant thereof; (2) incubating the compound in suitable media and a colorless chromogenic substrate; and (3) examining the media for development of color.

    摘要翻译： 本发明描述了一种用于筛选视黄醇X受体激动剂或拮抗剂的新方法，其包括：使用由酵母表达系统表达的类视黄醇X受体筛选具有类视黄醇X受体激动剂或拮抗剂活性的化合物以及用于检测 具有类视黄醇X受体激动剂或拮抗剂活性的化合物，其包括以下步骤：（1）提供表达视黄酸受体并活化含有载脂蛋白AI基因位点A或其突变变体的报告质粒的酵母菌株; （2）将化合物在合适的培养基和无色的显色底物中孵育; 和（3）检查媒体的颜色发展。

    Mechanism-based screen for retinoid X receptor agonists and antagonists
    4.
    发明授权
    Mechanism-based screen for retinoid X receptor agonists and antagonists 失效
    类维生素X受体激动剂和拮抗剂的机制筛选

    公开(公告)号：US5714595A

    公开(公告)日：1998-02-03

    申请号：US469120

    申请日：1995-06-06

    申请人： Paul Mak ,  Sotirios K. Karathanasis

    发明人： Paul Mak ,  Sotirios K. Karathanasis

    IPC分类号： C07K14/705 ,  C07K14/775 ,  C12N1/21 ,  C12N15/09 ,  C12Q1/02 ,  C12Q1/68 ,  C12R1/19 ,  G01N33/566 ,  C07H21/04

    CPC分类号： G01N33/566 ,  C07K14/70567 ,  C07K14/775 ,  C12Q1/6897 ,  G01N2333/395 ,  G01N2333/70567 ,  G01N2500/00

    摘要： A method is described for screening retinoid X receptor agonists or antagonists using a retinoid X receptor expressed by a yeast expression system to screen a compound having a retinoid X receptor agonist or antagonist activity. Another screen is described for detecting a compound having retinoid X receptor agonist or antagonist activity by: (1) providing a yeast strain which expresses the retinoic acid receptor and activates a reporter plasmid containing apolipoprotein AI gene site A or a mutated variant thereof; (2) incubating the compound in suitable media and a colorless chromogenic substrate; and (3) examining the media for development of color. Mutated variants of apolipoprotein AI gene site A which respond selectively to the retinoid X receptor or respond to receptors other than RXR.alpha. are also described.

    摘要翻译： 描述了使用由酵母表达系统表达的类视黄醇X受体筛选视黄醇X受体激动剂或拮抗剂以筛选具有类视黄醇X受体激动剂或拮抗剂活性的化合物的方法。 描述了另一个用于通过以下方式检测具有类视黄醇X受体激动剂或拮抗剂活性的化合物：（1）提供表达视黄酸受体并激活含有载脂蛋白AI基因位点A或其突变变体的报道质粒的酵母菌株; （2）将化合物在合适的培养基和无色的显色底物中孵育; 和（3）检查媒体的颜色发展。 还描述了对视黄酸X受体或对RXRα以外的受体有反应的载脂蛋白AI基因位点A的突变变体。

    Methods of screening for compounds with ability to alter apolipoprotein AI gene expression
    9.
    发明授权
    Methods of screening for compounds with ability to alter apolipoprotein AI gene expression 失效
    筛选具有改变载脂蛋白AI基因表达能力的化合物的方法

    公开(公告)号：US5721096A

    公开(公告)日：1998-02-24

    申请号：US255471

    申请日：1994-06-08

    申请人： Sotirios K. Karathanasis ,  John A.A. Ladias ,  Jeffrey N. Rottman ,  Russell L. Widom

    发明人： Sotirios K. Karathanasis ,  John A.A. Ladias ,  Jeffrey N. Rottman ,  Russell L. Widom

    IPC分类号： C12Q1/68 ,  G01N33/53

    CPC分类号： C12Q1/6897

    摘要： Activation of the apolipoprotein AI (apoAI) gene in mammalian liver cells has been studied, as described herein, and shown to depend on synergistic interactions between nuclear proteins which bind to three distinct sites within a hepatocyte-specific transcriptional enhancer located between nucleotides -222 to -110 5' of the human apoAI gene (relative to the transcription start site). Two proteins, the apoAI regulatory protein-1 and the retinoic acid receptor RXR.alpha., have been shown to regulate expression of the apoAI gene.

    摘要翻译： 如本文所述已经研究了哺乳动物肝细胞中载脂蛋白AI（apoAI）基因的活化，并且显示出依赖于核苷酸之间的协同相互作用的核蛋白之间的协同相互作用，所述核蛋白结合位于核苷酸-222至 -110 5'的人apoAI基因（相对​​于转录起始位点）。 已经显示两种蛋白质，即载脂蛋白A调节蛋白-1和视黄酸受体RXRα调节apoAI基因的表达。