MODIFIED TYROSINE AMINO ACIDS, PEPTIDES CONTAINING THEM, AND THEIR USE FOR DETECTING HYDROLASE ENZYME ACTIVITY
申请人:PAMGENE B.V.
公开号:US20140155286A1
公开(公告)日:2014-06-05
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 —PO
y
2−
with y equal to 2 or 3 and esters thereof, —SO
z
−
with z equal to 2 or 3 and esters thereof, a carbohydrate or carbohydrate derivatives; and; wherein X
1
and/or X
2
is selected from —N
3
, —NO
2
, —CI, or —CN, —SCN, a C
1
to C
8
alkyl, or H, wherein either X
1
or X
2
is not H.
本发明涉及一种方法和工具,可允许动力学监测水解酶酶活性。本发明还旨在提供合成的多肽和多肽残基的修饰,使它们可以用于监测水解酶酶活性,优选磷酸酶活性的测定中。还声明了公式(IV)中的修饰酪氨酸氨基酸衍生物,其中Y选择自-POy2-,其中y等于2或3及其酯,-SOz-,其中z等于2或3及其酯,一种碳水化合物或碳水化合物衍生物; 而X1和/或X2选择自-N3,-NO2,-CI或-CN,-SCN,C1至C8烷基或H,其中X1或X2中的任意一个不是H。