会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 13. 发明授权
    • Inhibition of nuclear import by backbone cyclic peptide analogs
    • 通过骨架环肽类似物抑制核进口
    • US06664368B1
    • 2003-12-16
    • US09564677
    • 2000-05-04
    • Assaf FriedlerAbraham LoyterChaim GilonAmnon Wolf
    • Assaf FriedlerAbraham LoyterChaim GilonAmnon Wolf
    • C07K750
    • C07K14/005C12N2740/16322
    • 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.
    • 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。