Protection of exendin-4 peptides through conjugation
    7.
    发明申请
    Protection of exendin-4 peptides through conjugation 审中-公开
    通过缀合保护毒蜥外泌肽-4肽

    公开(公告)号:US20090093408A1

    公开(公告)日:2009-04-09

    申请号:US12221554

    申请日:2008-08-01

    摘要: A method for protecting a peptide from peptidase activity in vivo, the peptide being composed of between 2 and 50 amino acids and having a C-terminus and an N-terminus and a C-terminus amino acid and an N-terminus amino acid is described. In the first step of the method, the peptide is modified by attaching a react group to the C-terminus amino acid, to the N-terminus amino acid, or to an amino acid located between the N-terminus and the C-terminus, such that the modified peptide is capable of forming a covalent bond in vivo with a reactive functionality on a blood component. In the next step, a covalent bond is formed between the reactive group and a reactive functionality on a blood component to form a peptide-blood component conjugate, thereby protecting said peptide from peptidase activity. The final step of the method involves the analyzing of the stability of the peptide-blood component conjugate to assess the protection of the peptide from peptidase activity.

    摘要翻译: 描述了一种在体内保护肽免受肽酶活性的方法,所述肽由2-50个氨基酸组成且具有C末端和N末端以及C末端氨基酸和N-末端氨基酸 。 在该方法的第一步中,通过将反应基团连接到C末端氨基酸,N末端氨基酸或位于N末端和C末端之间的氨基酸来修饰肽, 使得修饰的肽能够在体内与血液成分上的反应性官能团形成共价键。 在下一步骤中,在反应性基团和血液成分上的反应性官能团之间形成共价键以形成肽 - 血液成分缀合物,从而保护所述肽免受肽酶活性。 该方法的最后步骤包括分析肽 - 血液成分缀合物的稳定性,以评估肽对肽酶活性的保护。