VERFAHREN ZUR AMIDIERUNG VON POLYPEPTIDEN MIT C- TERMINALEN BASISCHEN AMINOSÄUREN UNTER VERWENDUNG SPEZIFISCHER ENDOPROTEASEN

摘要

Method for preparing C-terminally amidated di- or poly-basic peptides (I). Method for preparing C-terminally amidated di- or poly-basic peptides of formula (I) comprises reacting peptide (II) and amine (III) in presence of an enzyme (E) with trypsin activity, optionally followed by purification of (I) by methods used in protein chemistry. (AS)n-Xm-NH2 (I) (AS)n-Xp (II) (X)q-NH2 (III) AS : amino acid, or its analog or derivative; X : basic amino acid or its analog or derivative; n : 3-2000; m : 2-15; p and q : integers and p+q = m . An independent claim is also included for new peptides of formula His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-(Glu) 3-Ala-Val-Arg- Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gl y-Ala-Pro-Pro-Ser-Z-NH2 where Z = LysLys (Seq. (2)); LysArg (Seq. (3)); (Lys)5Arg (Seq. (4)) or ArgLys (Seq. (5)). - ACTIVITY : Antidiabetic; Anorectic; Anticoagulant; Thrombolytic. No details of tests for these activities are given. - MECHANISM OF ACTION : GLP-1 agonist; Extendin agonist; Hirudin agonist.