MODIFIED TRIDEGINS, PRODUCTION AND USE THEREOF AS TRANSGLUTAMINASE INHIBITORS

摘要

The invention relates to modified tridegins, polypeptides derived from SEQ ID No. 1, in which the modification is replacement of a cysteine residue and/or one of the following amino acids-Lys2, Lys7, His10, Gly12, Leu24, Tyr31, Phe34, Arg39, Ile45, Met48, Asp50, Pro55, Phe58, Asn60, Pro65, Arg66, by another amino acid and/or N- or C-terminal deletion, whereby the remaining polypeptide comprises at least the amino acid sequence DDIYQRXVXFPXLPL (SEQ ID NO.89) and/or a covalent bonding to polyethylene glycol. Said polypeptides are novel inhibitors of transglutaminases, in particular of Factor XIIIa, of the terminal enzymes in the blood coagulation cascade. The invention further relates to methods for production of said inhibitors and the use thereof as transglutaminase inhibitors.