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    Modulation of protein functionalities
    25.
    发明申请
    Modulation of protein functionalities 审中-公开
    蛋白质功能的调节

    公开(公告)号：US20080220497A1

    公开(公告)日：2008-09-11

    申请号：US11178834

    申请日：2005-07-11

    申请人： Daniel L. Flynn ,  Peter A. Petillo

    发明人： Daniel L. Flynn ,  Peter A. Petillo

    IPC分类号： C12N9/12 ,  C07K14/00 ,  C12N9/16 ,  C12N9/48 ,  C12N9/10

    CPC分类号： C07K14/4702 ,  C12N9/1205

    摘要： New methods for the rational identification of molecules capable of interacting with specific naturally occurring proteins are provided, in order to yield new pharmacologically important compounds and treatment modalities. Broadly, the method comprises the steps of identifying a switch control ligand forming a part of a particular protein of interest, and also identifying a complemental switch control pocket forming a part of the protein and which interacts with said switch control ligand. The ligand interacts in vivo with the pocket to regulate the conformation and biological activity of the protein such that the protein assumes a first conformation and a first biological activity upon the ligand-pocket interaction, and assumes a second, different conformation and biological activity in the absence of the ligand-pocket interaction. Next, respective samples of said protein in the first and second conformations are provided, and these are screened against one or more candidate molecules by contacting the molecules and the samples. Thereupon, small molecules which bind with the protein at the region of the pocket maybe identified. Novel protein-modulator adducts and methods of altering protein activity are also provided.

    摘要翻译： 提供了用于合理鉴定能够与特定天然存在的蛋白质相互作用的分子的新方法，以产生新的药理学上重要的化合物和治疗方式。 广泛地，该方法包括鉴定形成特定目的蛋白质的一部分的开关控制配体，以及鉴定形成蛋白质的一部分并与所述开关对照配体相互作用的互补开关控制袋。 配体在体内与口袋相互作用以调节蛋白质的构象和生物学活性，使得蛋白质在配体 - 口袋相互作用上呈现第一构象和第一生物活性，并且在第二种不同构象和生物学活性中 缺乏配体 - 口袋相互作用。 接下来，提供第一和第二构象中的所述蛋白质的各个样品，并且通过使分子和样品接触将它们与一种或多种候选分子进行筛选。 因此，可以鉴定在口​​袋区域与蛋白质结合的小分子。 还提供了新的蛋白质调节剂加合物和改变蛋白质活性的方法。