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    Histone conjugates and uses thereof
    2.
    发明申请
    Histone conjugates and uses thereof 审中-公开
    组蛋白共轭物及其用途

    公开(公告)号：US20060008464A1

    公开(公告)日：2006-01-12

    申请号：US10508959

    申请日：2003-04-03

    申请人： Chaim Gilon ,  Abraham Loyter ,  Adolf Graessman ,  Ilana Hariton-Gazal ,  Joseph Sperling

    发明人： Chaim Gilon ,  Abraham Loyter ,  Adolf Graessman ,  Ilana Hariton-Gazal ,  Joseph Sperling

    IPC分类号： A61K39/00 ,  C07K14/47

    CPC分类号： A61K47/645 ,  A61K47/62 ,  A61K47/643

    摘要： A conjugate of a histone moiety covalently attached to a macromolecule-of-interest, in which the histone moiety is transportable through the cell membrane and importable into the cell nuclei, is disclosed. Further disclosed are chemical and recombinant methods of preparing such a conjugate, pharmaceutical compositions containing same and uses thereof for delivering therapeutically active macromolecules into cells. A novel method for quantitatively determining a cytoplasmic uptake and/or a nuclear uptake of a moiety into cells is also disclosed.

    摘要翻译： 公开了共价连接到感兴趣的大分子的组蛋白部分的缀合物，其中组蛋白部分可通过细胞膜传输并可导入细胞核。 进一步公开的是制备这种缀合物的化学和重组方法，含有它的药物组合物和用于将治疗活性大分子递送到细胞中的用途。 还公开了用于定量测定部分细胞的细胞质摄取和/或核摄取的新方法。

    Inhibition of nuclear import by backbone cyclic peptide analogs
    5.
    发明授权
    Inhibition of nuclear import by backbone cyclic peptide analogs 失效
    通过骨架环肽类似物抑制核进口

    公开(公告)号：US06664368B1

    公开(公告)日：2003-12-16

    申请号：US09564677

    申请日：2000-05-04

    申请人： Assaf Friedler ,  Abraham Loyter ,  Chaim Gilon ,  Amnon Wolf

    发明人： Assaf Friedler ,  Abraham Loyter ,  Chaim Gilon ,  Amnon Wolf

    IPC分类号： C07K750

    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 12 &mgr;M 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.

    摘要翻译： 公开了功能上模拟大分子的核定位信号（NLS）区域的骨架环肽类似物的设计和合成。 对于HIV-1蛋白Vif的人免疫缺陷病毒1型蛋白MA，Vpr，Tat和NLS样序列的NLS序列，举例说明了本发明的原理。 我们公开了一种称为BCvir的新型高效骨架环肽的发现，其抑制核导入，IC50值为35nM。 将该抑制效力与线性亲本HIV-1 MA NLS肽显示的12μM进行比较。 在感染的非分裂培养的人类T细胞中，BCvir还将艾滋病毒1的产量降低了75％，并且相对抗胰蛋白酶消化。 这些性质使NLS或NLS样序列的骨架环肽类似物作为基于阻断核进入病毒基因组的新型药物的候选物。