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    Use of one-dimensional nuclear magnetic resonance to identify ligands to target biomolecules
    4.
    发明授权
    Use of one-dimensional nuclear magnetic resonance to identify ligands to target biomolecules 失效
    使用一维核磁共振来鉴定靶向生物分子的配体

    公开(公告)号：US6043024A

    公开(公告)日：2000-03-28

    申请号：US844124

    申请日：1997-04-18

    申请人： Stephen W. Fesik ,  Philip J. Hajduk ,  Edward T. Olejniczak

    发明人： Stephen W. Fesik ,  Philip J. Hajduk ,  Edward T. Olejniczak

    IPC分类号： G01R33/32 ,  A61K45/00 ,  C07K14/705 ,  C12N9/00 ,  C12Q1/68 ,  G01N24/08 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/68 ,  G01R33/44

    CPC分类号： G01R33/44 ,  G01N24/08 ,  G01N33/6803 ,  G01N2500/20 ,  Y10S435/81

    摘要： The present invention provides a process for identifying compounds which bind to a specific target molecule. The process comprises the steps of: a) generating a first T.sub.2 - or diffusion-filtered proton spectrum of one or a mixture of chemical compounds; b) exposing one or a mixture of chemical compounds to the target molecule; c) generating a second T.sub.2 - or diffusion-filtered proton spectrum of one or a mixture of chemical compounds that has been exposed the target molecule in step (b); and d) comparing said first and second T.sub.2 - or diffusion-filtered proton spectra to determine differences between said first and said second spectra, the differences identifying the presence of one or more compounds that are ligands which have bound to the target molecule.

    摘要翻译： 本发明提供了鉴定结合特定靶分子的化合物的方法。 该方法包括以下步骤：a）产生化合物之一或混合物的第一个T2或扩散过滤的质子光谱; b）将一种或一种化合物混合物暴露于靶分子; c）产生在步骤（b）中已经暴露于目标分子的化合物之一或其混合物的第二个T2或扩散过滤的质子光谱; 以及d）比较所述第一和第二T2或扩散过滤的质子光谱以确定所述第一和第二光谱之间的差异，所述差异鉴定了作为与靶分子结合的配体的一种或多种化合物的存在。

    Use of nuclear magnetic resonance to identify ligands to target biomolecules
    5.
    发明授权
    Use of nuclear magnetic resonance to identify ligands to target biomolecules 失效
    使用核磁共振来鉴定靶向生物分子的配体

    公开(公告)号：US5698401A

    公开(公告)日：1997-12-16

    申请号：US555691

    申请日：1995-11-14

    申请人： Stephen W. Fesik ,  Philip J. Hajduk

    发明人： Stephen W. Fesik ,  Philip J. Hajduk

    IPC分类号： G01R33/465 ,  C12Q1/00 ,  G01N20060101 ,  G01N24/08 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/542 ,  G01N33/566 ,  G01N33/58 ,  G01N33/68

    CPC分类号： G01N33/502 ,  G01N33/5008 ,  G01N33/542 ,  G01N33/6803 ,  G01N24/08 ,  G01N2500/20 ,  Y10T436/24

    摘要： The present invention provides a process for identifying compounds which bind to a specific target molecule. The process includes the steps of a) generating a first two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of a .sup.15 N-labeled target molecule; b) exposing the labeled target molecule to one or a mixture of chemical compounds; c) generating a second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of the labeled target molecule that has been exposed to one or a mixture of compounds in step (b); and d) comparing said first and second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectra to determine differences between said first and said second spectra, the differences identifying the presence of one or more compounds that are ligands which have bound to the target molecule.

    摘要翻译： 本发明提供了鉴定结合特定靶分子的化合物的方法。 该方法包括以下步骤：a）产生15N标记的靶分子的第一个二维15N / 1H NMR相关谱; b）将标记的靶分子暴露于化合物的一种或混合物; c）产生已经暴露于步骤（b）中的一种或其混合物的标记的目标分子的第二二维15N / 1H NMR相关谱; 和d）比较所述第一和第二二维15N / 1H NMR相关光谱以确定所述第一和第二光谱之间的差异，鉴别存在一种或多种与靶分子结合的配体的化合物的差异。

    Use of nuclear magnetic resonance to design ligands to target biomolecules
    8.
    发明授权
    Use of nuclear magnetic resonance to design ligands to target biomolecules 失效
    使用核磁共振来设计配体以靶向生物分子

    公开(公告)号：US5891643A

    公开(公告)日：1999-04-06

    申请号：US558633

    申请日：1995-11-14

    申请人： Stephen W. Fesik ,  Philip J. Hajduk ,  Edward T. Olejniczak

    发明人： Stephen W. Fesik ,  Philip J. Hajduk ,  Edward T. Olejniczak

    IPC分类号： G01N33/53 ,  G01N33/68 ,  G01N33/94 ,  G01R33/46 ,  G01N24/12

    CPC分类号： G01N33/6803 ,  G01N33/53 ,  G01N33/94 ,  G01R33/4633 ,  G01N2500/00 ,  Y10T436/24

    摘要： The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional .sup.15 N/.sup.1 H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional .sup.15 N/.sup.1 H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.

    摘要翻译： 本发明提供了设计结合特定靶分子的化合物的方法。 该方法包括以下步骤：a）使用二维15N / 1H NMR相关光谱法鉴定靶分子的第一配体; b）使用二维15N / 1H NMR相关光谱法鉴定靶分子的第二配体; c）通过将第一和第二配体与靶分子结合形成三元复合物; d）确定三元复合物的三维结构，从而确定靶分子上第一和第二配体的空间取向; 和e）连接第一和第二配体以形成药物，其中维持步骤（d）的空间取向。

    Use of nuclear magnetic resonance to identify ligands to target biomolecules
    9.
    发明授权
    Use of nuclear magnetic resonance to identify ligands to target biomolecules 失效
    使用核磁共振来鉴定靶向生物分子的配体

    公开(公告)号：US5804390A

    公开(公告)日：1998-09-08

    申请号：US804777

    申请日：1997-02-24

    申请人： Stephen W. Fesik ,  Philip J. Hajduk

    发明人： Stephen W. Fesik ,  Philip J. Hajduk

    IPC分类号： G01R33/465 ,  C12Q1/00 ,  G01N20060101 ,  G01N24/08 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/542 ,  G01N33/566 ,  G01N33/58 ,  G01N33/68

    CPC分类号： G01N33/502 ,  G01N33/5008 ,  G01N33/542 ,  G01N33/6803 ,  G01N24/08 ,  G01N2500/20 ,  Y10T436/24

    摘要： The present invention provides a process for identifying compounds which bind to a specific target molecule. The process includes the steps of a) generating a first two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of a .sup.15 N-labeled target molecule; b) exposing the labeled target molecule to one or a mixture of chemical compounds; c) generating a second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of the labeled target molecule that has been exposed to one or a mixture of compounds in step (b); and d) comparing said first and second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectra to determine differences between said first and said second spectra, the differences identifying the presence of one or more compounds that are ligands which have bound to the target molecule.

    摘要翻译： 本发明提供了鉴定结合特定靶分子的化合物的方法。 该方法包括以下步骤：a）产生15N标记的靶分子的第一个二维15N / 1H NMR相关谱; b）将标记的靶分子暴露于化合物的一种或混合物; c）产生已经暴露于步骤（b）中的一种或其混合物的标记的目标分子的第二二维15N / 1H NMR相关谱; 和d）比较所述第一和第二二维15N / 1H NMR相关光谱以确定所述第一和第二光谱之间的差异，鉴别存在一种或多种与靶分子结合的配体的化合物的差异。