Modified tyrosine amino acids, peptides containing them, and their use for detecting hydrolase enzyme activity

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.;

主权项

1. A method for detecting hydrolase enzyme activity in a sample, said method comprising the step of:
contacting said sample with one or more modified tyrosine amino acids according to formula IVwherein Y is chosen from —POy2− with y equal to 2 or 3 and esters thereof; and wherein X1 and/or X2 is selected from —N3, —NO2, —Br, or H, wherein either X1 or X2 is not H;or contacting said sample with one or more synthetic peptides comprising between 2 and 100 amino acids, characterized therein that said peptide has incorporated therein at least one of said modified tyrosine amino acids
detecting the product of the hydrolase enzyme activity on said amino acids or peptides, and optionally detecting the inhibition of hydrolase enzyme activity on said amino acids or peptides.