发明申请
- 专利标题: Modified therapeutic peptides with extended half-lives in vivo
- 专利标题(中): 体内延长半衰期的修饰治疗肽
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申请号: US11982033申请日: 2007-10-31
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公开(公告)号: US20090175821A1公开(公告)日: 2009-07-09
- 发明人: Dominique P. Bridon , Alan M. Ezrin , Peter G. Milner , Darren L. Holmes , Karen Thibaudeau
- 申请人: Dominique P. Bridon , Alan M. Ezrin , Peter G. Milner , Darren L. Holmes , Karen Thibaudeau
- 主分类号: A61K38/38
- IPC分类号: A61K38/38 ; C07K19/00 ; A61K38/21 ; A61K38/28 ; A61K38/22 ; A61K38/18
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 reactive 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.
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