SACCHARIDE-MODIFIED PEPTIDE DERIVATIVE CAPABLE OF TRANSFERRING GENE SPECIFICALLY INTO HEPATOCYTE, ITS PRODUCTION AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

摘要

PROBLEM TO BE SOLVED: To obtain the subject new derivative capable of transferring a gene specifically into hepatocytes and useful as e.g. a gene therapeutic agent for hepatic disorders in combination with a DNA, by modifying an amphiphilicα-helix peptide having gene-transferring capability with galactose group(s). SOLUTION: This new saccharide-modified peptide derivative is such one as to be expressed by e.g. formula I [P is an amphiphilicα-helix peptide group; Q is a direct bond-forming group or a bond-forming group expressed by the formula: NH(CH2 CH2 )f CH2 CO (f) is 1-10}; K is a lysine residue; A is a direct bond-forming group, bond-forming group expressed by the formula; NH(CH2 CH2 O)h CH2 CO (h) is 1-10} or the formula NH(CH2 )j CO [(j) is 1-6;] (m) is 0-3; (n) is 1-3; Z is a group having galactose group (s)] and to be capable of transferring a gene and to consist ofα-helix peptide modified with galactose group(s) and to be useful as e.g. a therapeutic agent for hepatic disorders. This derivative is obtained by reductive amination of e.g. a peptide expressed by formula II with lactose to introduce at least one galactose group into the peptide.