发明授权
US06849714B1 Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components 失效
通过与血液成分缀合,保护内源性治疗肽免受肽酶活性的影响

Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
摘要:
A method of synthesizing a modified therapeutic peptide capable of forming a peptidase-stabilized therapeutic peptide conjugate, the peptide having between 3 and 50 amino acids, is k. In a first step of the method, a therapeutic peptide having a carboxy terminal amino acid and amino terminal amino acid is synthesized. In a second step, pairs of cysteine residues present in the therapeutic peptide are sequentially and selectively oxidized to form disulfide bridges in the therapeutic peptide. In a third step, a protecting group is attached to remaining cysteine residues that do not form disulfide bridges in the therapeutic peptide. Finally, the peptide is coupled to a reactive group capable of reacting with amino groups, hydroxyl groups or thiol groups on a blood component to form a covalent bond therewith.
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