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    Small molecule printing
    1.
    发明授权
    Small molecule printing 失效
    小分子印刷

    公开(公告)号：US06824987B1

    公开(公告)日：2004-11-30

    申请号：US09567910

    申请日：2000-05-10

    申请人： Stuart L. Schreiber ,  Gavin MacBeath ,  Angela N. Koehler ,  Paul Hergenrother ,  Kristopher M. Depew

    发明人： Stuart L. Schreiber ,  Gavin MacBeath ,  Angela N. Koehler ,  Paul Hergenrother ,  Kristopher M. Depew

    IPC分类号： G01N3353

    CPC分类号： G01N31/00 ,  B01J19/0046 ,  B01J2219/00387 ,  B01J2219/00454 ,  B01J2219/00459 ,  B01J2219/005 ,  B01J2219/00533 ,  B01J2219/00605 ,  B01J2219/0061 ,  B01J2219/00612 ,  B01J2219/00626 ,  B01J2219/00637 ,  B01J2219/0072 ,  C07B2200/11 ,  C07C311/49 ,  C40B30/04 ,  C40B40/04 ,  C40B50/14 ,  C40B60/14 ,  G01N33/54353 ,  Y10S436/809

    摘要： The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction. In general, these inventive arrays are generated by: (1) providing a solid support, wherein said solid support is functionalized with a selected chemical moiety capable of interacting with a desired chemical compound to form an attachment; (2) providing one or more solutions of one or more types of compounds to be attached to the solid support; and (3) delivering said one or more types of compounds to the solid support, whereby an array is formed and the array of compounds has a density of at least 1000 spots per cm2. In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest comprising: (1) providing an array of compounds, wherein the array has a density of at least 1000 spots per cm2; (2) contacting the array with one of more types of biological macromolecules of interest; and (3) determining the interaction of specific small molecule-biological macromolecule partners.

    摘要翻译： 本发明提供了有助于鉴定能够与感兴趣的生物大分子相互作用的化合物的组合物和方法。 在一个方面，提供了包含连接到固体支持物上的一种或多种类型化学化合物的阵列的组合物，其中化合物阵列的密度为至少1000个斑点/ cm 2。 在特别优选的实施方案中，这些化合物通过共价相互作用连接到固体支持物上。 通常，这些本发明的阵列通过以下方式产生：（1）提供固体支持物，其中所述固体支持物用能够与所需化学化合物相互作用以形成附着物的选定化学部分官能化; （2）提供待连接到固体支持物上的一种或多种类型化合物的一种或多种溶液; 和（3）将所述一种或多种类型的化合物递送到固体支持物，由此形成阵列，并且所述化合物阵列的密度至少为1000个点/ cm 2。 另一方面，本发明提供了利用这些阵列来识别感兴趣的生物大分子的小分子配偶体的方法，包括：（1）提供化合物阵列，其中阵列的密度至少为1000个点/ cm 2 ; （2）使阵列与感兴趣的多种生物大分子之一接触; 和（3）确定特定小分子 - 生物大分子伴侣的相互作用。

    Small molecule printing
    2.
    发明申请
    Small molecule printing 审中-公开
    小分子印刷

    公开(公告)号：US20050095639A1

    公开(公告)日：2005-05-05

    申请号：US10998867

    申请日：2004-11-29

    申请人： Stuart L. Schreiber ,  Gavin MacBeath ,  Angela Koehler ,  Paul Hergenrother ,  Kristopher Depew

    发明人： Stuart L. Schreiber ,  Gavin MacBeath ,  Angela Koehler ,  Paul Hergenrother ,  Kristopher Depew

    IPC分类号： B01J19/00 ,  C07B61/00 ,  C07C311/49 ,  C40B30/04 ,  C40B40/04 ,  C40B50/14 ,  C40B60/14 ,  G01N33/543 ,  C12Q1/68 ,  G01N33/53

    CPC分类号： G01N31/00 ,  B01J19/0046 ,  B01J2219/00387 ,  B01J2219/00454 ,  B01J2219/00459 ,  B01J2219/005 ,  B01J2219/00533 ,  B01J2219/00605 ,  B01J2219/0061 ,  B01J2219/00612 ,  B01J2219/00626 ,  B01J2219/00637 ,  B01J2219/0072 ,  C07B2200/11 ,  C07C311/49 ,  C40B30/04 ,  C40B40/04 ,  C40B50/14 ,  C40B60/14 ,  G01N33/54353 ,  Y10S436/809

    摘要： The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction. In general, these inventive arrays are generated by: (1) providing a solid support, wherein said solid support is functionalized with a selected chemical moiety capable of interacting with a desired chemical compound to form an attachment; (2) providing one or more solutions of one or more types of compounds to be attached to the solid support; and (3) delivering said one or more types of compounds to the solid support, whereby an array is formed and the array of compounds has a density of at least 1000 spots per cm2. In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest comprising: (1) providing an array of compounds, wherein the array has a density of at least 1000 spots per cm2; (2) contacting the array with one of more types of biological macromolecules of interest; and (3) determining the interaction of specific small molecule-biological macromolecule partners.

    摘要翻译： 本发明提供了有助于鉴定能够与感兴趣的生物大分子相互作用的化合物的组合物和方法。 在一个方面，提供了一种组合物，其包含连接到固体支持物上的一种或多种类型化学化合物的阵列，其中化合物阵列的密度为至少1000个点/ cm 2。 在特别优选的实施方案中，这些化合物通过共价相互作用连接到固体支持物上。 通常，这些本发明的阵列通过以下方式产生：（1）提供固体支持物，其中所述固体支持物用能够与所需化学化合物相互作用以形成附着物的选定化学部分官能化; （2）提供待连接到固体支持物上的一种或多种类型化合物的一种或多种溶液; 和（3）将所述一种或多种类型的化合物递送到固体支持物，由此形成阵列，并且化合物阵列具有至少1000个点/ cm 2的密度。 另一方面，本发明提供利用这些阵列鉴定感兴趣的生物大分子的小分子伴侣的方法，包括：（1）提供化合物阵列，其中阵列的密度至少为1000个点/ 2 ; （2）使阵列与感兴趣的多种生物大分子之一接触; 和（3）确定特定小分子 - 生物大分子伴侣的相互作用。

    Frizzled 2 as a target for therapeutic antibodies in the treatment of cancer
    8.
    发明授权
    Frizzled 2 as a target for therapeutic antibodies in the treatment of cancer 有权
    卷曲2作为治疗抗癌治疗癌症的靶标

    公开(公告)号：US09260519B2

    公开(公告)日：2016-02-16

    申请号：US14127017

    申请日：2012-06-15

    申请人： Taranjit S. Gujral ,  Gavin MacBeath

    发明人： Taranjit S. Gujral ,  Gavin MacBeath

    IPC分类号： A61K39/395 ,  C07K16/28 ,  C07K16/30 ,  A61K39/00

    CPC分类号： C12Q1/6883 ,  A61K2039/505 ,  C07K16/28 ,  C07K16/2863 ,  C07K16/30 ,  C07K16/303 ,  C07K2317/24 ,  C07K2317/34 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/77 ,  C07K2317/92 ,  C12Q2600/106 ,  C12Q2600/158

    摘要： Disclosed herein are methods of treating cancer in a subject, and methods for inhibiting growth, migration and/or invasion of a cancer cell in the subject, comprising administering to the subject a therapeutically effective amount of an antibody or antigen binding fragment thereof that downmodulates Fzd2. The antibody may specifically bind Fzd2, and may promote internalization of the Fzd2 receptor by the cancer cells and/or prevent ligand binding to Fzd2. Specific antibodies, and also specific portions of the Fzd2 molecule for antibody binding are disclosed. In one embodiment the antibody specifically binds to the epitope HGAEQICVGQNHSEDGAPAL (SEQ ID NO: 1). Specific cancers (e.g. late stage hepatocellular carcinoma), intended for treatment are provided, and include cancers that exhibit overexpression of Fzd2, and/or Wnt5a.

    摘要翻译： 本文公开了治疗受试者的癌症的方法以及用于抑制受试者中癌细胞的生长，迁移和/或侵袭的方法，包括向受试者施用治疗有效量的下调Fzd2的抗体或其抗原结合片段 。 抗体可以特异性结合Fzd2，并且可以促进癌细胞对Fzd2受体的内化和/或阻止配体结合Fzd2。 公开了特异性抗体以及用于抗体结合的Fzd2分子的特定部分。 在一个实施方案中，抗体特异性结合表位HGAEQICVGQNHSEDGAPAL（SEQ ID NO：1）。 提供旨在治疗的特异性癌症（例如晚期肝细胞癌），包括表现出过度表达Fzd2和/或Wnt5a的癌症。

    FRIZZLED 2 AS A TARGET FOR THERAPEUTIC ANTIBODIES IN THE TREATMENT OF CANCER
    10.
    发明申请
    FRIZZLED 2 AS A TARGET FOR THERAPEUTIC ANTIBODIES IN THE TREATMENT OF CANCER 有权
    作为治疗癌症的治疗药物的目标2

    公开(公告)号：US20140242070A1

    公开(公告)日：2014-08-28

    申请号：US14127017

    申请日：2012-06-15

    申请人： Taranjit S. Gujral ,  Gavin MacBeath

    发明人： Taranjit S. Gujral ,  Gavin MacBeath

    IPC分类号： C07K16/28

    CPC分类号： C12Q1/6883 ,  A61K2039/505 ,  C07K16/28 ,  C07K16/2863 ,  C07K16/30 ,  C07K16/303 ,  C07K2317/24 ,  C07K2317/34 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/77 ,  C07K2317/92 ,  C12Q2600/106 ,  C12Q2600/158

    摘要： Disclosed herein are methods of treating cancer in a subject, and methods for inhibiting growth, migration and/or invasion of a cancer cell in the subject, comprising administering to the subject a therapeutically effective amount of an antibody or antigen binding fragment thereof that downmodulates Fzd2. The antibody may specifically bind Fzd2, and may promote internalization of the Fzd2 receptor by the cancer cells and/or prevent ligand binding to Fzd2. Specific antibodies, and also specific portions of the Fzd2 molecule for antibody binding are disclosed. In one embodiment the antibody specifically binds to the epitope HGAEQICVGQNHSEDGAPAL (SEQ ID NO: 1). Specific cancers (e.g. late stage hepatocellular carcinoma), intended for treatment are provided, and include cancers that exhibit overexpression of Fzd2, and/or Wnt5a.

    摘要翻译： 本文公开了治疗受试者的癌症的方法以及用于抑制受试者中癌细胞的生长，迁移和/或侵袭的方法，包括向受试者施用治疗有效量的下调Fzd2的抗体或其抗原结合片段 。 抗体可以特异性结合Fzd2，并且可以促进癌细胞对Fzd2受体的内化和/或阻止配体结合Fzd2。 公开了特异性抗体以及用于抗体结合的Fzd2分子的特定部分。 在一个实施方案中，抗体特异性结合表位HGAEQICVGQNHSEDGAPAL（SEQ ID NO：1）。 提供旨在治疗的特异性癌症（例如晚期肝细胞癌），包括表现出过度表达Fzd2和/或Wnt5a的癌症。