management of transglutaminase - catalysed by transglutaminase proteinmodifizierung selective irreversible inhibitors

摘要

Method for specific protein modification catalyzed by transglutaminase (TG) which is controlled by at least one selective, irreversible TG inhibitor (A). Independent claims are also included for the following: (1) (A) of formula (I); and (2) method for preparing sidechain-modified peptides, as (A), by replacing, in a peptide known to be a TG substrate, a Glu residue by a modified Glu that has a methyl ketone in the gamma -position. X : diazo, Me2S+, RCOO or RS; Xaa1 and Xaa2 : amino protecting group, amino acid (or derivative) or peptide of 2-8, preferably 6-8, amino acids (or derivatives); proviso : the compound acetyl-prolinyl-glutaminyl-prolinyl-(6-diazo-5-oxoleucinyl)leucinyl-prolinyl-phenylalaninyl-NH2 is excluded and R is not defined [Image].