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    Antagonists of G-protein-coupled receptor
    3.
    发明授权
    Antagonists of G-protein-coupled receptor 失效
    G蛋白偶联受体的拮抗剂

    公开(公告)号：US5955575A

    公开(公告)日：1999-09-21

    申请号：US995927

    申请日：1997-12-22

    申请人： Krishna G. Peri ,  Sylvain Chemtob ,  Michel Potier

    发明人： Krishna G. Peri ,  Sylvain Chemtob ,  Michel Potier

    IPC分类号： A61K38/00 ,  C07K14/47 ,  C07K14/705 ,  A61K38/04 ,  A61K38/16

    CPC分类号： C07K14/70571 ,  C07K14/4722 ,  A61K38/00 ,  C07K2319/00

    摘要： The present invention relates to a new class of G-protein-coupled receptor antagonists which bind to the intracellular molecular interface between the receptor and the G-protein, thus hampering signal transduction. The present invention describes peptide sequences derived from the prostaglandin receptor F.sub.2.alpha. and the G-protein, G.alpha.q protein, produced by molecular biology techniques or chemical synthesis, as selective inhibitors of signal transduction involved in the stimulation of this receptor. Such peptides or molecules derived from their primary, secondary and tertiary structures may be used as effective tocolytics for the prevention of premature labor or be utilized for the treatment of dysmenorrhea.

    摘要翻译： 本发明涉及结合受体和G蛋白之间的细胞内分子界面的新一类G蛋白偶联受体拮抗剂，从而阻碍了信号转导。 本发明描述了衍生自前列腺素受体F2α和通过分子生物学技术或化学合成产生的G-protein，Gαq蛋白的肽序列作为参与刺激该受体的信号转导的选择性抑制剂。 衍生自其初级，次级和三级结构的这些肽或分子可以用作预防早产或用于治疗痛经的有效tocolytics。

    Cytokine receptor modulators and uses thereof
    5.
    发明申请
    Cytokine receptor modulators and uses thereof 审中-公开
    细胞因子受体调节剂及其用途

    公开(公告)号：US20090048161A1

    公开(公告)日：2009-02-19

    申请号：US11919941

    申请日：2006-05-05

    申请人： Sylvain Chemtob ,  Christiane Quiniou ,  Martin Beauchamp

    发明人： Sylvain Chemtob ,  Christiane Quiniou ,  Martin Beauchamp

    IPC分类号： A61K38/00 ,  C07K7/00 ,  C07K14/00 ,  C12N15/00 ,  G01N33/566 ,  C12Q1/28 ,  A61P27/00 ,  C12Q1/42 ,  C12N1/20 ,  C12N5/06 ,  C12N1/19

    CPC分类号： G01N33/6863 ,  C07K7/06 ,  C07K7/08 ,  C07K14/72 ,  G01N33/6869

    摘要： The present invention relates to cytokine receptor-binding compounds, such as non-competitive VEGF receptor, IL-1 receptor, IL-4 receptor, or IGF-1 receptor-binding peptides and petidomimetic antagonists, and therapeutic uses of such compounds. The compounds of the present invention may be used in the treatment of cytokine-associated diseases such as proliferative disorders (for example, colon, breast, prostate, and lung cancer), abnormal neovascularization and angiogenesis, age-related macular degeneration, and proliferative and/or inflammatory skin disorders such as psoriasis.

    摘要翻译： 本发明涉及细胞因子受体结合化合物，例如非竞争性VEGF受体，IL-1受体，IL-4受体或IGF-1受体结合肽和小鼠模拟拮抗剂，以及这些化合物的治疗用途。 本发明的化合物可用于治疗细胞因子相关疾病，例如增殖性疾病（例如结肠癌，乳腺癌，前列腺癌和肺癌），异常新生血管形成和血管发生，年龄相关性黄斑变性和增殖性和 /或炎症性皮肤病如牛皮癣。

    Cytokine receptor modulators and method of modulating cytokine receptor activity
    6.
    发明授权
    Cytokine receptor modulators and method of modulating cytokine receptor activity 失效
    细胞因子受体调节剂和调节细胞因子受体活性的方法

    公开(公告)号：US07432341B2

    公开(公告)日：2008-10-07

    申请号：US10693657

    申请日：2003-10-24

    申请人： Sylvain Chemtob ,  Christiane Quiniou ,  Martin Beauchamp

    发明人： Sylvain Chemtob ,  Christiane Quiniou ,  Martin Beauchamp

    IPC分类号： A61K38/00 ,  A61K38/04 ,  C07K7/00

    CPC分类号： G01N33/6863 ,  A61K38/1709 ,  G01N2500/00

    摘要： The present invention relates to a method for identifying a non-competitive peptide, which inhibits the activity of a cytokine receptor. This method includes the steps of selecting a candidate peptide containing from about 7 to about 20 amino acids derived from a flexible region of a cytokine receptor, and determining the ability of the peptide to inhibit or promote the oligomerization and/or activation of the receptor by measuring an activity of the receptor in the absence or the presence of the candidate peptide, wherein the non-competitive peptide is selected when the activity of the receptor is measurably lower in the presence of the peptide as compared to in the absence of the peptide so identified. This invention also provides agonists of cytokine receptor activity. Pharmaceutical compositions that comprise the identified peptides are disclosed. Also disclosed are methods for treating patients with a disease or condition associated with abnormal cytokine receptor mediated function or activity such as inflammatory, autoimmune and vascular diseases.

    摘要翻译： 本发明涉及一种鉴定抑制细胞因子受体活性的非竞争性肽的方法。 该方法包括以下步骤：选择含有衍生自细胞因子受体的柔性区的约7至约20个氨基酸的候选肽，以及通过以下步骤确定肽抑制或促进受体的寡聚和/或活化的能力： 在不存在或存在候选肽的情况下测量受体的活性，其中当肽的存在下与不存在肽时相比，当受体的活性可测量较低时，选择非竞争性肽 确定。 本发明还提供了细胞因子受体活性的激动剂。 公开了包含鉴定的肽的药物组合物。 还公开了用于治疗患有与异常细胞因子受体介导的功能或活性（例如炎症，自身免疫和血管疾病）相关的疾病或病症的患者的方法。

    CYTOKINE RECEPTOR MODULATORS, METHOD OF IDENTIFYING SAME, AND METHOD OF MODULATING CYTOKINE RECEPTORS ACTIVITY WITH SAME
    9.
    发明申请
    CYTOKINE RECEPTOR MODULATORS, METHOD OF IDENTIFYING SAME, AND METHOD OF MODULATING CYTOKINE RECEPTORS ACTIVITY WITH SAME 审中-公开
    细胞因子受体调节剂，鉴别方法和调节细胞因子受体活性的方法

    公开(公告)号：US20110014128A1

    公开(公告)日：2011-01-20

    申请号：US12836809

    申请日：2010-07-15

    申请人： Sylvain Chemtob ,  Christiane Quiniou ,  Martin Beauchamp

    发明人： Sylvain Chemtob ,  Christiane Quiniou ,  Martin Beauchamp

    IPC分类号： A61K49/00 ,  G01N33/566 ,  C07K2/00 ,  A61K38/03 ,  A61P35/00 ,  A61P37/02 ,  A61P29/00 ,  A61P37/08 ,  A61P11/06 ,  A61P7/02 ,  A61P9/00

    CPC分类号： G01N33/6863 ,  A61K38/1709 ,  G01N2500/00

    摘要： The present invention relates to a method for identifying a non-competitive peptide, which inhibits the activity of a cytokine receptor. This method includes the steps of selecting a candidate peptide containing from about 7 to about 20 amino acids derived from a flexible region of a cytokine receptor, and determining the ability of the peptide to inhibit or promote the oligomerization and/or activation of the receptor by measuring an activity of the receptor in the absence or the presence of the candidate peptide, wherein the non-competitive peptide is selected when the activity of the receptor is measurably lower in the presence of the peptide as compared to in the absence of the peptide so identified. This invention also provides agonists of cytokine receptor activity. Pharmaceutical compositions that comprise the identified peptides are disclosed. Also disclosed are methods for treating patients with a disease or condition associated with abnormal cytokine receptor mediated function or activity such as inflammatory, autoimmune and vascular diseases.

    摘要翻译： 本发明涉及一种鉴定抑制细胞因子受体活性的非竞争性肽的方法。 该方法包括以下步骤：选择含有源自细胞因子受体的柔性区域的约7至约20个氨基酸的候选肽，以及通过以下步骤确定肽抑制或促进受体的寡聚和/或活化的能力： 在不存在或存在候选肽的情况下测量受体的活性，其中当肽的存在下与不存在肽时相比，当受体的活性可测量较低时，选择非竞争性肽 确定。 本发明还提供了细胞因子受体活性的激动剂。 公开了包含鉴定的肽的药物组合物。 还公开了用于治疗患有与异常细胞因子受体介导的功能或活性（例如炎症，自身免疫和血管疾病）相关的疾病或病症的患者的方法。

    Peptide antagonists of prostaglandin F2α receptor
    10.
    发明授权
    Peptide antagonists of prostaglandin F2α receptor 失效
    前列腺素F2α受体的肽拮抗剂

    公开(公告)号：US06984719B1

    公开(公告)日：2006-01-10

    申请号：US09787334

    申请日：1999-09-15

    申请人： Sylvain Chemtob ,  Krishna G. Peri

    发明人： Sylvain Chemtob ,  Krishna G. Peri

    IPC分类号： A61K38/04 ,  A61K38/00 ,  C07K16/00 ,  C07K14/00 ,  A01N37/18

    CPC分类号： C07K14/72 ,  A61K38/00

    摘要： The present invention relates to a new class of G protein-coupled receptor agonist or antagonist, which specifically binds to the receptor protein structural elements, thus altering signal transmission and subsequent physiological effects. Described herein are peptide sequences derived from the G protein-coupled receptor protein, produced by chemical methods as selective inhibitors of signal transduction associated with stimulation of the receptor by its ligand. Such peptides or molecules derived from their primary, secondary or tertiary structures may be used as effective tocolytics for the prevention of premature labor or be used for the treatment of dysmenorrhea.

    摘要翻译： 本发明涉及一类新的G蛋白偶联受体激动剂或拮抗剂，其特异性结合受体蛋白质结构元件，从而改变信号传导和随后的生理效应。 本文描述了衍生自G蛋白偶联受体蛋白质的肽序列，其通过化学方法作为与其配体刺激受体相关的信号转导的选择性抑制剂产生。 衍生自其初级，次级或三级结构的这些肽或分子可以用作预防早产或用于治疗痛经的有效tocolytics。