发明公开
- 专利标题: LIBRAIRIES OF BACKBONE-CYCLIZED PEPTIDOMIMETICS
- 专利标题(中): 图书馆主干环化肽
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申请号: EP96928663.0申请日: 1996-08-28
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公开(公告)号: EP0923601A2公开(公告)日: 1999-06-23
- 发明人: HORNIK, Vered , GILON, Chaim
- 申请人: PEPTOR LTD , YISSUM RESEARCH DEVELOPMENT COMPANY of the Hebrew University of Jerusalem
- 申请人地址: Weizmann Industrial Park 76326 Rehovot IL
- 专利权人: PEPTOR LTD,YISSUM RESEARCH DEVELOPMENT COMPANY of the Hebrew University of Jerusalem
- 当前专利权人: PEPTOR LTD,YISSUM RESEARCH DEVELOPMENT COMPANY of the Hebrew University of Jerusalem
- 当前专利权人地址: Weizmann Industrial Park 76326 Rehovot IL
- 代理机构: Baldock, Sharon Claire, et al
- 优先权: IL19950115096 19950829; US19950569042 19951207
- 国际公布: WO1997009344 19970313
- 主分类号: G01N33
- IPC分类号: G01N33 ; C07K1 ; C07K5 ; C07K7 ; C07K14 ; C07K17 ; G01R31 ; A61K38
摘要:
Libraries of novel backbone-cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units used in the synthesis of these backbone-cyclized peptide analogs are Nα (φ-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these Nα (φ-functionalized) amino acids are incorporated into a library of peptide sequences, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by libraries of backbone-cyclized bradykinin analogs, somatostatin analogs, BPI analogs and Substance P analogs having biological activity. Further embodiments of the invention are Interleukin-6 receptor derived peptides having ring structures involving backbone cyclization.
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