PROTECTION OF ENDOGENOUS THERAPEUTIC PEPTIDES FROM PEPTIDASE ACTIVITY THROUGH CONJUGATION TO BLOOD COMPONENTS

摘要

A method for protecting a peptide from peptidase activity in vivo, the peptidebeing composed of between 2 and 50amino acids and having a C-terminus and an N-terminus and a C-terminus aminoacid and an N-terminus amino acid is described.In the first step of the method, the peptide is modified by attaching areactive group to the C-terminus amino acid, to the N-terminusamino acid, or to an amino acid located between the N-terminus and the C-terminus, such that the modified peptide is capable offorming a covalent bond in vivo with a reactive functionality on a bloodcomponent. In the next step, a covalent bond is formedbetween the reactive group and a reactive functionality on a blood componentto form a peptide-blood component conjugate, therebyprotecting said peptide from peptidase activity. The final step of the methodinvolves the analyzing of the stability of thepeptide--blood component conjugate to assess the protection of the peptidefrom peptidase activity.