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    LIBRAIRIES OF BACKBONE-CYCLIZED PEPTIDOMIMETICS
    6.
    发明公开
    LIBRAIRIES OF BACKBONE-CYCLIZED PEPTIDOMIMETICS 失效
    图书馆主干环化肽

    公开(公告)号：EP0923601A2

    公开(公告)日：1999-06-23

    申请号：EP96928663.0

    申请日：1996-08-28

    申请人： PEPTOR LTD ,  YISSUM RESEARCH DEVELOPMENT COMPANY of the Hebrew University of Jerusalem

    发明人： HORNIK, Vered ,  GILON, Chaim

    IPC分类号： G01N33 ,  C07K1 ,  C07K5 ,  C07K7 ,  C07K14 ,  C07K17 ,  G01R31 ,  A61K38

    CPC分类号： C07K7/22 ,  A61K38/00 ,  C07K1/047 ,  C07K7/56 ,  C07K14/001 ,  C07K14/6555 ,  G01R31/318541 ,  Y02P20/55

    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.

    INHIBITION OF NUCLEAR IMPORT BY BACKBONE CYCLIC PEPTIDE ANALOGS
    8.
    发明公开
    INHIBITION OF NUCLEAR IMPORT BY BACKBONE CYCLIC PEPTIDE ANALOGS 审中-公开
    核心传输的抑制的密钥链模拟环肽

    公开(公告)号：EP1034182A1

    公开(公告)日：2000-09-13

    申请号：EP98955888.7

    申请日：1998-11-26

    申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM ,  PEPTOR LTD

    发明人： FRIEDLER, Assaf ,  LOYTER, Abraham ,  GILON, Chaim ,  WOLF, AMNON

    IPC分类号： C07K1/02 ,  C07K1/04 ,  C07K5/12

    CPC分类号： C07K14/005 ,  C12N2740/16322

    摘要： The design and the synthesis of backbone cyclic peptide analogs which functionally mimic the nuclear localization signal (NLS) region of macromolecules is disclosed. The principles of the invention are exemplified for the NLS sequences of the human immunodeficiency virus type 1 proteins MA, Vpr, Tat and NLS-like sequences of HIV-1 protein Vif. We disclose the discovery of a novel, highly potent backbone cyclic peptide, designated BCvir, which inhibits nuclear import with an IC50 value of 35 nM. This inhibitory potency is to be compared to 12νM exhibited by the linear parent HIV-1 MA NLS peptide. BCvir also reduced HIV-1 production by 75 % in infected non-dividing cultured human T-cells and was relatively resistant to tryptic digestion. These properties render backbone cyclic peptide analogs of NLS or NLS-like sequences as candidates for novel drugs based on blocking nuclear import of viral genomes.