PURPOSE: To obtain a novel peptide complex effective for the treatment of thrombosis as a thrombolytic agent enabling the drug delivery exclusive to thrombotic part by bonding a peptide having a specific amino acid sequence to a thrombolytic biopolymer.
CONSTITUTION: A peptide chain is synthesized by solid-phase synthesis using an Fmoc-cysteine resin (Fmoc is 9-fluorenylmethylcarbonyl group) as a carrier, swelling the resin with dimethylformamide, etc., removing Fmoc group and successively bonding amino acids having α-amino acid protected with Fmoc group according to the amino acid sequence of the peptide. The synthesized peptide chain is separated from the resin and all the protection groups are removed from the chain to obtain a peptide having the sequence of formula I and formula II and containing ≥3 amino acid residues. The objective peptide complex composed of a peptide chemically bonded to a biopolymer can be prepared by linking the above peptide to a thrombolytic biopolymer (e.g. urokinase) by carbodiimide condensation process.
TAJIMA MAYUMI
KUMAGAI HIROMICHI
KOYAMA YOSHIYUKI