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    INHIBITION OF NUCLEAR IMPORT BY BACKBONE CYCLIC PEPTIDE ANALOGS
    1.
    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.