SOLID-PHASE METHOD FOR SYNTHESIS OF PEPTIDE/SPACER/LIPID CONJUGATE, CONJUGATE SYNTHESIZED THEREBY, AND OBJECTIVE LIPOSOME CONTAINING THE CONJUGATE

摘要

PROBLEM TO BE SOLVED: To provide a solid-phase synthesis method for preparing a peptide/spacer/lipid conjugate and to provide matter related thereto.

SOLUTION: The synthesis method comprises the steps of synthesizing in a solid phase a peptydyl resin with protected amino residues; conjugating the peptidyl resin with a spacer and a lipid to form a peptide/spacer/lipid resin having a peptide/spacer/ lipid; cleaving the peptide/spacer/lipid resin to form the peptide/spacer/lipid; removing at least one side-chain-protecting group from at least one amino acid of the peptide/spacer/lipid to form a peptide/spacer/lipid conjugate; and subjecting the peptide/spacer/lipid conjugate to no treatment or to a treatment for cyclizing the peptide moieties of the peptide/spacer/lipid conjugate. The spacer is conjugated with the peptidyl resin or the lipid through one bonding functional group.

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