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1. 发明授权

US06689887B2 Inhibition of human telomerase by a G-quadruplex-interaction compound 失效
标题翻译：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
申请人： Sean M. Kerwin , Oleg Y. Fedoroff , Miguel Salazar , Laurence H. Hurley
发明人： Sean M. Kerwin , Oleg Y. Fedoroff , Miguel Salazar , Laurence H. Hurley
IPC分类号： C07D51500
CPC分类号： C07D471/06 , C07D277/64 , C12Q1/68 , C12Q1/6886 , C12Q2600/136 , C12Q2600/154
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。

2. 发明授权

US06623930B2 Inhibition of human telomerase by a G-quadruplex-interaction compound 失效
标题翻译：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
申请人： Sean M. Kerwin , Oleg Y. Fedoroff , Miguel Salazar , Laurence H. Hurley
发明人： Sean M. Kerwin , Oleg Y. Fedoroff , Miguel Salazar , Laurence H. Hurley
IPC分类号： C12Q168
CPC分类号： C07D471/06 , C07D277/64 , C12Q1/68 , C12Q1/6886 , C12Q2600/136 , C12Q2600/154
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。

3. 发明授权

US6156763A Inhibition of human telomerase by a g-quadruplex-interaction compound 失效
标题翻译：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
申请人： Sean M. Kerwin , Oleg Y. Fedoroff , Miguel Salazar , Laurence H. Hurley
发明人： Sean M. Kerwin , Oleg Y. Fedoroff , Miguel Salazar , Laurence H. Hurley
IPC分类号： C07D277/64 , C07D471/06 , C12Q1/68 , A61K31/44 , C07D221/22
CPC分类号： C07D471/06 , C07D277/64 , C12Q1/68 , C12Q1/6886 , C12Q2600/136 , C12Q2600/154
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。

4. 发明授权

US6054442A Methods and compositions for modulation and inhibition of telomerase in vitro 失效
标题翻译：用于调节和抑制端粒酶的方法和组合物
公开(公告)号：US6054442A
公开(公告)日：2000-04-25
申请号：US675119
申请日：1996-07-03
申请人： Shih-Fong Chen , Ira Maine , Sean M. Kerwin , Terace M. Fletcher , Miguel Salazar , Blain Mamiya , Bradford E. Windle , Makoto Wajima
发明人： Shih-Fong Chen , Ira Maine , Sean M. Kerwin , Terace M. Fletcher , Miguel Salazar , Blain Mamiya , Bradford E. Windle , Makoto Wajima
IPC分类号： A61K31/70 , C07H19/14
CPC分类号： A61K31/7076 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/708 , C07H19/14
摘要： It was found that normal human stem cells produce a regulated non-processive telomerase activity, while cancer cells produce a processive telomerase activity. Nucleotide analogs, such as 7-deaza-2'-deoxyquanosine-5'-triphosphate (7-deaza-dGTP) were found to be substrates for processive telomerase and incorporated into telomeric sequence. The incorporation of this nucleotide subsequently affected the processivity of telomerase, converting processive telomerase to non-processive telomerase. The incorporation of this nucleotide analogs was also found to inhibit formation of G-quartets by telomeric sequence. Other methods for converting cancer processive telomerase to the more benign non-processive telomerase include partially cleaving the telomerase RNA. The nucleoside analogs were found to be capable of a variety of activities including mediating allosteric-like inhibition of telomerase, premature termination and shortening of telomeric DNA, destabilization of telomeric structure and function and eventually cell death. Understanding the mechanisms of telomerase modulation by the 7-deaza-nucleotides has allowed the design of new telomerase inhibitors, modulators and agents for affecting telomere structure and function. These discoveries have application in the treatment of cancer.
摘要翻译：发现正常的人类干细胞产生调节的非进程性端粒酶活性，而癌细胞产生进行性的端粒酶活性。发现核苷酸类似物，如7-脱氮-2'-脱氧鸟苷-5'-三磷酸（7-脱氮-dGTP）是进行性端粒酶的底物并掺入端粒序列。该核苷酸的并入随后影响端粒酶的进程，将进程性端粒酶转化为非进程性端粒酶。还发现该核苷酸类似物的掺入通过端粒序列抑制G四重奏的形成。将癌症进程性端粒酶转化为更良性非进程性端粒酶的其他方法包括部分切割端粒酶RNA。发现核苷类似物具有多种活性，包括介导端粒酶的变构类似的抑制，早期终止和端粒DNA的缩短，端粒结构和功能的不稳定以及最终的细胞死亡。了解7-脱氮核苷酸端粒酶调节机制使得设计了新的端粒酶抑制剂，调节剂和药剂来影响端粒结构和功能。这些发现可用于治疗癌症。

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