NUCLEOTIDE ANALOGUES WITH QUATERNARY CARBON STEREOGENIC CENTERS AND METHODS OF USE
    1.
    发明申请
    NUCLEOTIDE ANALOGUES WITH QUATERNARY CARBON STEREOGENIC CENTERS AND METHODS OF USE 有权
    具有季碳异体中心的核苷类似物及其使用方法

    公开(公告)号:US20110092451A1

    公开(公告)日:2011-04-21

    申请号:US12933291

    申请日:2009-03-18

    申请人: Yvan Guindon

    发明人: Yvan Guindon

    摘要: The present invention comprises compounds useful as antiviral or antitumor agents. The compounds comprise nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moeities with quaternary centers at the 3′ position. The nucleotide analogues can be used to inhibit cancer or viruses. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit viruses or tumors and treat, prevent, or inhibit the foregoing diseases.

    摘要翻译: 本发明包括可用作抗病毒剂或抗肿瘤剂的化合物。 这些化合物包含核苷酸类似物,其包含在3'位上具有四元中心的四氢呋喃基或四氢噻吩基。 核苷酸类似物可用于抑制癌症或病毒。 因此,本发明的化合物可用于治疗,预防和/或抑制与癌症和病毒相关的疾病或病症。 因此,本发明还包括包含该化合物的药物制剂和使用该化合物和制剂抑制病毒或肿瘤并治疗,预防或抑制前述疾病的方法。

    Nucleoside and Nucleotide Analogues with Quaternary Carbon Centers and Methods of Use
    2.
    发明申请
    Nucleoside and Nucleotide Analogues with Quaternary Carbon Centers and Methods of Use 有权
    具有第四纪碳中心的核苷和核苷酸类似物和使用方法

    公开(公告)号:US20100093737A1

    公开(公告)日:2010-04-15

    申请号:US12523193

    申请日:2008-01-17

    申请人: Yvan Guindon

    发明人: Yvan Guindon

    摘要: The present invention comprises compounds useful as antiviral or antitumor agents. The compounds comprise nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moeities with quaternary centers at the 3′ position. The nucleotide analogues can be used to inhibit cancer or viruses. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit viruses or tumors and treat, prevent, or inhibit the foregoing diseases.

    摘要翻译: 本发明包括可用作抗病毒剂或抗肿瘤剂的化合物。 这些化合物包含核苷酸类似物,其包含在3'位上具有四元中心的四氢呋喃基或四氢噻吩基。 核苷酸类似物可以用于抑制癌症或病毒。 因此,本发明的化合物可用于治疗,预防和/或抑制与癌症和病毒相关的疾病或病症。 因此,本发明还包括包含该化合物的药物制剂和使用该化合物和制剂抑制病毒或肿瘤并治疗,预防或抑制前述疾病的方法。

    Mammalian Subtilisin/kexin isozyme SKI-1: a proprotein convertase with a unique cleavage specificity
    9.
    发明授权
    Mammalian Subtilisin/kexin isozyme SKI-1: a proprotein convertase with a unique cleavage specificity 失效
    哺乳动物枯草杆菌蛋白酶/ kexin同功酶SKI-1:具有独特裂解特异性的前蛋白转化酶

    公开(公告)号:US07211424B1

    公开(公告)日:2007-05-01

    申请号:US09830837

    申请日:1999-11-04

    CPC分类号: C12N9/6424

    摘要: Using RT-PCR and degenerate oligonucleotides derived from the active site residues of subtilisin-kexin-like serine proteinases, we have identified a highly conserved and phylogenetically ancestral human, rat and mouse type-I membrane-bound proteinase called subtilisin-kexin-isozyme-1 (SKI-1). Computer data bank searches reveals that human SKI-1 was previously cloned but with no identified function. A SKI-1 processed fragment is secreted in culture media in a soluble form. In vitro studies suggest that SKI-1 is a Ca2+-dependent serine proteinase exhibiting a wide pH optimum for cleavage of proBDNF. Peptides mimicking SKI-1 cleavages sites are also disclosed. SKI-1 prosegment has an ex vivo inhibitory effect on SKI-1 activity. The prosegment is also processed and secreted in culture media. One of its fragments is found tightly associated with the SKI-1 soluble form. Therapeutic applications for SKI-1 inhibitors are disclosed.

    摘要翻译: 使用RT-PCR和衍生自枯草杆菌蛋白酶 - 类克隆丝氨酸蛋白酶的活性位点残基的简并寡核苷酸,我们确定了一种高度保守和系统发育的祖先人类,大鼠和小鼠I型膜结合蛋白酶,称为枯草杆菌蛋白酶 - 1(SKI-1)。 计算机数据库搜索显示人类SKI-1以前被克隆,但没有识别功能。 SKI-1处理的片段以可溶形式分泌在培养基中。 体外研究表明,SKI-1是表现出对于proBDNF的切割具有宽pH最适的Ca 2+ 2 +依赖性丝氨酸蛋白酶。 还公开了模拟SKI-1切割位点的肽。 SKI-1 prosegment具有对SKI-1活性的离体抑制作用。 散文也在文化媒体中被处理和分发。 其中一个片段被发现与SKI-1可溶形式紧密相关。 公开了SKI-1抑制剂的治疗应用。