Methods for regulating transcription by targeting quadruplex DNA
    3.
    发明授权
    Methods for regulating transcription by targeting quadruplex DNA 失效
    通过靶向四联体DNA调节转录的方法

    公开(公告)号:US07405041B2

    公开(公告)日:2008-07-29

    申请号:US10645471

    申请日:2003-08-20

    IPC分类号: C12Q1/68

    CPC分类号: C07D513/22 Y10S977/924

    摘要: Among the different intrastrand quadruplex structures that can arise from duplex DNA, it has been discovered that the nucleotide sequences (GGA)4 (SEQ ID NO: 1) and (GGA)3GG (SEQ ID NO: 2) form biologically significant quadruplex structures. Thus, provided herein are methods for identifying molecules that modulate the biological activity of quadruplex DNA comprising the nucleotide sequence (GGA)4 (SEQ ID NO: 1) or the nucleotide sequence (GGA)3GG (SEQ ID NO: 2), and specifically, methods for identifying molecules that bind such quadruplexes. Also provided herein are methods for modulating the biological activity of a biologically significant native quadruplex DNA with a molecule identified by the methods described herein.

    摘要翻译: 在双链DNA可能产生的不同的intrastrand四链体结构中,已经发现核苷酸序列(GGA)4(SEQ ID NO:1)和(GGA)3

    Inhibition of human telomerase by a G-quadruplex-interaction compound
    6.
    发明授权
    Inhibition of human telomerase by a G-quadruplex-interaction compound 失效
    通过G-四链体相互作用化合物抑制人端粒酶

    公开(公告)号:US06689887B2

    公开(公告)日:2004-02-10

    申请号:US09730893

    申请日:2000-12-05

    IPC分类号: C07D51500

    摘要: Certain non-nucleoside compounds that will selectively inhibit telomerase by targeting the nucleic add structures, such as G-quadruplexes, that may be associated with human telomeres or telomerase have been identified. Inhibition of human telomerase by two perylenetetracarboxylic acid diimides and a carbocyanine has been demonstrated. 1H-NMR studies have evidenced the stabilization of a G-quadruplex by the perylenetetracarboxylic acid diimide compounds and provided evidence that these and structurally related compounds inhibit the telomerase enzyme by a mechanism consistent with interaction with G-quadruplex structures.

    摘要翻译: 已经鉴定了通过靶向可能与人端粒或端粒酶相关的核酸添加结构(例如G-四链体)选择性抑制端粒酶的某些非核苷化合物。 已经证明了两种苝四羧酸二酰亚胺和羰花青对人端粒酶的抑制作用。 1 H-NMR研究证明了由苝四羧酸二酰亚胺化合物稳定G-四链体,并提供证据表明这些和结构相关的化合物通过与G-四链体结构的相互作用一致的机制来抑制端粒酶。

    Methods for treating bone deficit conditions with benzothiazole
    7.
    发明授权
    Methods for treating bone deficit conditions with benzothiazole 失效
    用苯并噻唑治疗骨缺损病症的方法

    公开(公告)号:US5922753A

    公开(公告)日:1999-07-13

    申请号:US808742

    申请日:1997-02-28

    CPC分类号: A61K31/428 A61K31/4184

    摘要: Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or "linker" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 .ANG., are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.

    摘要翻译: 包含通过含有一个或多个原子的接头共价连接的两个芳族体系的化合物或定义为包含共价键本身的“连接体”,以使芳族体系在距离为1.5-15安培的范围内空间有效地处理与 骨缺损。 化合物可以单独施用于脊椎动物,或者与促进骨生长或抑制骨吸收的其它试剂组合施用。 可以通过评估其在影响与骨形态发生蛋白相关的启动子相关的报告基因的转录和/或刺激模型动物系统中颅骨生长的能力的能力来筛选其给药前的活性。

    Expanded porphyrin compositions for tumor inhibition
    8.
    发明授权
    Expanded porphyrin compositions for tumor inhibition 失效
    膨胀卟啉组合物用于肿瘤抑制

    公开(公告)号:US07001588B2

    公开(公告)日:2006-02-21

    申请号:US10661241

    申请日:2003-09-12

    摘要: Expanded porphyrin comprising substitutions for at least two NH groups by S, Se or Te are non-photoactive and are selective for binding G-quadruplexes characteristic of the c-MYC control region. Accordingly, these expanded porphyrins are useful to modulate the expression of genes controlled by the formation of c-MYC type G-quadruplexes, such as c-MYC itself.

    摘要翻译: 包含由S,Se或Te取代至少两个NH基团的扩增卟啉是非光活性的,并且对于结合c-MYC对照区特征的G-四链体体是有选择性的。 因此,这些扩增的卟啉可用于调节由形成c-MYC型G-四链体(例如c-MYC本身)控制的基因的表达。

    Inhibition of human telomerase by a G-quadruplex-interaction compound
    9.
    发明授权
    Inhibition of human telomerase by a G-quadruplex-interaction compound 失效
    通过G-四链体相互作用化合物抑制人端粒酶

    公开(公告)号:US06623930B2

    公开(公告)日:2003-09-23

    申请号:US09940173

    申请日:2001-08-27

    IPC分类号: C12Q168

    摘要: Certain non-nucleoside compounds that will selectively inhibit telomerase by targeting the nucleic add structures, such as G-quadruplexes, that may be associated with human telomeres or telomerase have been identified. Inhibition of human telomerase by two perylenetetracarboxylic acid diimides and a carbocyanine has been demonstrated. 1H-NMR studies have evidenced the stabilization of a G-quadruplex by the perylenetetracarboxylic acid diimide compounds and provided evidence that these and structurally related compounds inhibit the telomerase enzyme by a mechanism consistent with interaction with G-quadruplex structures.

    摘要翻译: 已经鉴定了通过靶向可能与人端粒或端粒酶相关的核酸添加结构(例如G-四链体)选择性抑制端粒酶的某些非核苷化合物。 已经证明了两种苝四羧酸二酰亚胺和羰花青对人端粒酶的抑制作用。 1 H-NMR研究证明了由苝四羧酸二酰亚胺化合物稳定G-四链体,并提供证据表明这些和结构相关的化合物通过与G-四链体结构的相互作用一致的机制来抑制端粒酶。

    Inhibition of human telomerase by a g-quadruplex-interaction compound
    10.
    发明授权
    Inhibition of human telomerase by a g-quadruplex-interaction compound 失效
    通过g-四链体相互作用化合物抑制人端粒酶

    公开(公告)号:US6156763A

    公开(公告)日:2000-12-05

    申请号:US244675

    申请日:1999-02-04

    摘要: Certain non-nucleoside compounds that will selectively inhibit telomerase by targeting the nucleic add structures, such as G-quadruplexes, that may be associated with human telomeres or telomerase have been identified. Inhibition of human telomerase by two perylenetetracarboxylic acid diimides and a carbocyanine has been demonstrated. .sup.1 H-NMR studies have evidenced the stabilization of a G-quadruplex by the perylenetetracarboxylic acid diimide compounds and provided evidence that these and structurally related compounds inhibit the telomerase enzyme by a mechanism consistent with interaction with G-quadruplex structures.

    摘要翻译: 已经鉴定了通过靶向可能与人端粒或端粒酶相关的核酸添加结构(例如G-四链体)选择性抑制端粒酶的某些非核苷化合物。 已经证明了两种苝四羧酸二酰亚胺和羰花青对人端粒酶的抑制作用。 1 H-NMR研究证明了由苝四羧酸二酰亚胺化合物稳定G-quadruplex,并提供证据表明这些和结构相关的化合物通过与G-四链体结构的相互作用一致的机制来抑制端粒酶。