MODIFIED TYROSINE AMINO ACIDS, PEPTIDES CONTAINING THEM, AND THEIR USE FOR DETECTING HYDROLASE ENZYME ACTIVITY
    3.
    发明申请
    MODIFIED TYROSINE AMINO ACIDS, PEPTIDES CONTAINING THEM, AND THEIR USE FOR DETECTING HYDROLASE ENZYME ACTIVITY 有权
    改性的酪氨酸氨基酸,含有它们的肽及其用于检测水解酶活性的用途

    公开(公告)号:US20140155286A1

    公开(公告)日:2014-06-05

    申请号:US14118920

    申请日:2012-05-18

    申请人: PAMGENE B.V.

    IPC分类号: G01N33/573 C07F9/08

    摘要: The present invention relates to a method and tools which allow the kinetic monitoring of hydrolase enzyme activity. The present invention also aims to provide synthetic peptides and peptide residues modified such that they can be used in assays for monitoring hydrolase enzyme activity, and preferably phosphatase activity. Also claimed are modified tyrosine amino acid derivatives of formula (IV), wherein Y is chosen from —POy2− with y equal to 2 or 3 and esters thereof, —SOz− with z equal to 2 or 3 and esters thereof, a carbohydrate or carbohydrate derivatives; and; wherein X1 and/or X2 is selected from —N3, —NO2, —CI, or —CN, —SCN, a C1 to C8 alkyl, or H, wherein either X1 or X2 is not H.

    摘要翻译: 本发明涉及允许动态监测水解酶活性的方法和工具。 本发明还旨在提供经修饰的合成肽和肽残基,使得它们可用于监测水解酶活性的测定,优选用于磷酸酶活性。 还要求保护的是式(IV)的修饰的酪氨酸氨基酸衍生物,其中Y选自-Yyy2-,其中y等于2或3,其酯,-SO z-,其中z等于2或3及其酯,碳水化合物或 碳水化合物衍生物; 和; 其中X 1和/或X 2选自-N 3,-NO 2,-C 1或-CN,-SCN,C 1至C 8烷基或H,其中X 1或X 2不为H.