Aqueous Solution Containing Partial Ras Polypeptide and Method for Screening Inhibitor of Ras Function
    12.
    发明申请
    Aqueous Solution Containing Partial Ras Polypeptide and Method for Screening Inhibitor of Ras Function 审中-公开
    含有部分Ras多肽的水溶液和筛选Ras功能抑制剂的方法

    公开(公告)号:US20140024123A1

    公开(公告)日:2014-01-23

    申请号:US13984027

    申请日:2012-01-31

    IPC分类号: C07K14/47 C07C337/02

    摘要: Provided is a screening method for a more effective Ras inhibitor. Further provided are amino acid residues at a site important for an interaction with a Ras inhibitor in a Ras polypeptide. By confirming a difference between structural information on the Ras polypeptide by NMR and structural information between a complex of the Ras polypeptide and a seed compound by NMR, a more effective lead compound than the seed compound can be selected. As a result of analysis based on the structural information on the Ras polypeptide by NMR, the amino acid residues capable of interacting with a Ras inhibitor candidate (a) are K5, E37, D38, S39, L56, E63, Y64, A66, M67, Q70, Y71, R73, and T74 with reference to an amino acid sequence set forth in SEQ ID NO: 1.

    摘要翻译: 提供了一种更有效的Ras抑制剂的筛选方法。 还提供了在Ras多肽中与Ras抑制剂相互作用重要的位点处的氨基酸残基。 通过NMR证实Ras多肽的结构信息与Ras多肽与种子化合物的复合物之间的结构信息之间的差异,可以选择比种子化合物更有效的铅化合物。 作为基于通过NMR的Ras多肽的结构信息的分析的结果,能够与Ras抑制剂候选物(a)相互作用的氨基酸残基是K5,E37,D38,S39,L56,E63,Y64,A66,M67 ,Q70,Y71,R73和T74,参照SEQ ID NO:1所示的氨基酸序列。