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    • 2. 发明申请
    • METHOD OF MODULATION OF INTERACTION BETWEEN RECEPTOR AND LIGAND
    • 受体和配体之间相互作用的调节方法
    • WO2004056865A3
    • 2005-02-24
    • PCT/DK0300901
    • 2003-12-18
    • ENKAM PHARMACEUTICALS ASBEREZIN VLADIMIRALBRECHTSEN MORTENBOCK ELISABETH
    • BEREZIN VLADIMIRALBRECHTSEN MORTENBOCK ELISABETH
    • A61K38/00C07K7/06C07K7/08C07K16/22G01N33/566G01N33/74C07K7/00
    • C07K7/06A61K38/00C07K7/08C07K16/22G01N33/566G01N33/74G01N2333/50
    • The present invention relates to a method for modulating the interaction between at least two proteins, wherein at least one of the two proteins is a functional cell-surface receptor and the other protein is the receptor ligand. The invention features a binding site of said functional cell-surface receptor on the receptor ligand and discloses a series of amino acid sequences, which are part of the structure of said binding site and/or involved in the interaction between the receptor and the ligand. Moreover, the present invention features methods for molecular design and screening of a candidate compound capable of modulating the interaction between the functional cell-surface receptor and receptor ligand through the described binding site, and provides a screening assay for identification of such a compound. The invention further describes an antibody capable of binding to the above binding site and/or to an epitope comprising an amino acid sequence essential for executing the receptor ligand interaction through said binding site. The invention also concerns a variety of uses of the disclosed methods, peptide sequences and antibodies. The invention in preferred embodiments concerns the binding site of the fibroblast growth factor receptor (FGFR) on FGFR ligands, compounds capable of modulating the receptor ligand interaction through said binding site, and antibody capable of recognition of said binding site.
    • 本发明涉及调节至少两种蛋白质之间的相互作用的方法,其中两种蛋白质中的至少一种是功能性细胞表面受体,而另一种蛋白质是受体配体。 本发明的特征在于所述功能性细胞表面受体在受体配体上的结合位点,并公开了一系列氨基酸序列,其是所述结合位点结构的一部分和/或参与受体和配体之间的相互作用。 此外,本发明的特征在于分子设计和筛选能够通过所述结合位点调节功能性细胞表面受体和受体配体之间的相互作用的候选化合物的方法,并提供了鉴定这种化合物的筛选试验。 本发明还描述了能够结合上述结合位点和/或包含通过所述结合位点执行受体配体相互作用所必需的氨基酸序列的表位的抗体。 本发明还涉及所公开的方法,肽序列和抗体的各种用途。 本发明在优选实施方案中涉及成纤维细胞生长因子受体(FGFR)对FGFR配体的结合位点,能够通过所述结合位点调节受体配体相互作用的化合物和能够识别所述结合位点的抗体。