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1. 发明申请

US20090253717A1 Inhibitors of p97 有权
标题翻译： p97的抑制剂
公开(公告)号：US20090253717A1
公开(公告)日：2009-10-08
申请号：US12321463
申请日：2009-01-20
申请人： Steven J. Brown , Tsui-Fen Chou , Raymond Deshaies , Amanda C. Jones , Hugh Rosen , Brian M. Stoltz
发明人： Steven J. Brown , Tsui-Fen Chou , Raymond Deshaies , Amanda C. Jones , Hugh Rosen , Brian M. Stoltz
IPC分类号： A61K31/519 , A61P35/00
CPC分类号： A61K31/519
摘要： One aspect of the invention relates to compounds that inhibit the activity of p97, such as by binding covalently to a cysteine residue in the active site. In certain embodiments, the invention relates to the treatment of disease, such as cancer, comprising administering a compound of the invention.
摘要翻译：本发明的一个方面涉及抑制p97活性的化合物，例如通过与活性位点中的半胱氨酸残基共价结合。在某些实施方案中，本发明涉及疾病如癌症的治疗，其包括施用本发明的化合物。

2. 发明授权

US09089572B2 Inhibitors of p97 有权
公开(公告)号：US09089572B2
公开(公告)日：2015-07-28
申请号：US12321463
申请日：2009-01-20
申请人： Steven J. Brown , Tsui-Fen Chou , Raymond Deshaies , Amanda C. Jones , Hugh Rosen , Brian M. Stoltz
发明人： Steven J. Brown , Tsui-Fen Chou , Raymond Deshaies , Amanda C. Jones , Hugh Rosen , Brian M. Stoltz
IPC分类号： A61K31/519
CPC分类号： A61K31/519
摘要： One aspect of the invention relates to compounds that inhibit the activity of p97, such as by binding covalently to a cysteine residue in the active site. In certain embodiments, the invention relates to the treatment of disease, such as cancer, comprising administering a compound of the invention.

3. 发明申请

US20050203063A1 Proteasome pathway inhibitors and related methods 审中-公开
标题翻译：蛋白酶体途径抑制剂及相关方法
公开(公告)号：US20050203063A1
公开(公告)日：2005-09-15
申请号：US10940502
申请日：2004-09-13
申请人： Raymond Deshaies , Randall King , Rati Verma
发明人： Raymond Deshaies , Randall King , Rati Verma
IPC分类号： A61K20060101 , A61K31/195 , A61K31/277 , A61K31/40 , A61K31/44 , A61K31/655 , A61K31/695 , A61K31/785 , A61K31/795
CPC分类号： A61K31/785 , A61K31/795
摘要： The disclosure provides compositions and methods for blocking the proteasome pathway, as well as compounds that block mitotic cell cycle progression. Compounds disclosed include a family of molecules that bind to a multiubiquitin chain attached to a protein and thereby inhibit degradation of that protein by the proteasome pathway. According to another aspect of the disclosure, compounds are provided that inhibit cell cycle progression. Compounds disclosed herein may be formulated for pharmaceutical use and employed in methods for treating cancers or other hyperproliferative disorders.
摘要翻译：本公开提供了用于阻断蛋白酶体途径的组合物和方法，以及阻断有丝分裂细胞周期进程的化合物。所公开的化合物包括结合到与蛋白质连接的多泛素链的分子家族，从而通过蛋白酶体途径抑制该蛋白质的降解。根据本公开的另一方面，提供抑制细胞周期进程的化合物。本文公开的化合物可以配制用于药物用途，并用于治疗癌症或其它过度增殖性疾病的方法中。

4. 发明申请

US20100193270A1 HYBRID ELECTRIC PROPULSION SYSTEM 审中-公开
标题翻译：混合电动推进系统
公开(公告)号：US20100193270A1
公开(公告)日：2010-08-05
申请号：US12665268
申请日：2008-06-23
申请人： Raymond Deshaies , Marcel Chartrand
发明人： Raymond Deshaies , Marcel Chartrand
IPC分类号： B60W10/04 , F16F15/30 , B60W20/00 , H02K7/02
CPC分类号： B60W20/00 , B60K1/02 , B60K6/105 , B60K6/26 , B60K6/38 , B60K6/46 , B60L50/30 , B60L50/61 , B60L53/14 , B60L2270/44 , B60W10/06 , B60W10/08 , B60W10/24 , Y02T10/6204 , Y02T10/6217 , Y02T10/6269 , Y02T10/6282 , Y02T10/6286 , Y02T10/7005 , Y02T10/7027 , Y02T10/7033 , Y02T10/7072 , Y02T10/7077 , Y02T90/14 , Y10T74/2119
摘要： A hybrid electric propulsion system for a vehicle. The system includes an internal combustion engine (12); a flywheel (14) operatively connected to the engine (12), the flywheel (14) having a horizontal rotation axis parallel to a rotation axis of the wheels of the vehicle, the flywheel (14) having a main disk being rotatable in an opposite direction (RFES) with respect to a rotation of the wheels (RT) of the vehicle when the vehicle is travelling forward so as to inhibit a rollover effect of the vehicle when the vehicle is turning; an electric generator (18) operatively connected to the flywheel (14); an electric motor (22) operatively connected to the electric generator (18); and a controller for controlling operation of the engine (12), the flywheel (14), the electric generator (18) and the electric motor (22).
摘要翻译：一种用于车辆的混合动力电动推进系统。该系统包括内燃机（12）; 飞轮（14），其可操作地连接到所述发动机（12），所述飞轮（14）具有平行于所述车辆的车轮的旋转轴线的水平旋转轴线，所述飞轮（14）具有主盘，当车辆向前行进时相对于车辆的车轮（RT）的旋转方向（RFES），以便当车辆转向时阻止车辆的翻车效果; 可操作地连接到飞轮（14）的发电机（18）; 可操作地连接到所述发电机（18）的电动机（22）; 以及用于控制发动机（12），飞轮（14），发电机（18）和电动机（22）的操作的控制器。

5. 发明申请

US20090192084A1 Compositions and method of treating hypoxia-associated diseases 有权
标题翻译：治疗缺氧相关疾病的组合物和方法
公开(公告)号：US20090192084A1
公开(公告)日：2009-07-30
申请号：US12291155
申请日：2008-11-05
申请人： Gabriela Alexandru , Raymond Deshaies , Johannes Graumann
发明人： Gabriela Alexandru , Raymond Deshaies , Johannes Graumann
IPC分类号： A61K38/17 , G01N33/566 , G01N33/53 , G01N33/536 , C12Q1/68 , C12N5/06 , A61K31/711
CPC分类号： G01N33/6872 , A61K31/711 , G01N2333/4703 , G01N2500/02
摘要： Hypoxia, a state of lower than normal tissue oxygen tension, has recently been implicated in a host of human diseases, including cancer, heart disease, and neurological disorders. Novel associations between p97 and other proteins, including UBX-domain-containing proteins (UBX-polypeptides), HIF1α, and a variety of E3 ligases are provided herein. The disclosure provides complexes comprising UBX-domain-containing polypeptides (UBX-polypeptides) and other polypeptides involved in the degradation of ubiquitinated proteins. In addition, the disclosure provides uses for active agents that modulate protein-protein complex formation between an UBX-polypeptide and its complementary-binding substrate. For example, the disclosure provides methods for treating or preventing hypoxia-related disorders or conditions in a patient or a cell by administration of an active agent that modulates the activity of an UBX-polypeptide and/or its complementary binding-substrate. Furthermore, the disclosure provides uses for active agents that modulate HIF1α activity; such agents may be used to modulate processes that are regulated by HIF1α. The disclosure also provides many screening assays to identify test agents that modulate complex formation between an UBX-polypeptide and its complementary-binding substrate or methods for evaluating modes of action and/or effects of active agents that have already been identified as modulators of an UBX-polypeptide and/or its complementary-binding substrate.
摘要翻译：缺氧是一种低于正常组织氧气紧张度的状态，最近已经涉及许多人类疾病，包括癌症，心脏病和神经障碍。本文提供了p97和其他蛋白质（包括含UBX结构域的蛋白质（UBX-多肽），HIF1α和各种E3连接酶）之间的新型关联。本公开提供了包含含有UBX结构域的多肽（UBX-多肽）和参与泛素化蛋白质降解的其它多肽的复合物。此外，本公开提供了调节UBX-多肽与其互补结合底物之间的蛋白质 - 蛋白质复合物形成的活性剂的用途。例如，本公开提供了通过施用调节UBX-多肽和/或其互补结合底物的活性的活性剂来治疗或预防患者或细胞中的缺氧相关病症或病症的方法。此外，本公开提供了调节HIF1α活性的活性剂的用途; 这些药剂可用于调节由HIF1alpha调节的过程。本公开还提供了许多筛选测定法，以鉴定调节UBX-多肽及其互补结合底物之间的复合物形成的测试剂或用于评估已被鉴定为UBX调节剂的活性剂的作用模式和/或效果的方法 - 多肽和/或其互补结合底物。

6. 发明授权

US07867724B2 Compositions and method of treating hypoxia-associated diseases 有权
标题翻译：治疗缺氧相关疾病的组合物和方法
公开(公告)号：US07867724B2
公开(公告)日：2011-01-11
申请号：US12291155
申请日：2008-11-05
申请人： Gabriela Alexandru , Raymond Deshaies , Johannes Graumann
发明人： Gabriela Alexandru , Raymond Deshaies , Johannes Graumann
IPC分类号： G01N33/53 , G01N33/543
CPC分类号： G01N33/6872 , A61K31/711 , G01N2333/4703 , G01N2500/02
摘要： Hypoxia, a state of lower than normal tissue oxygen tension, has recently been implicated in a host of human diseases, including cancer, heart disease, and neurological disorders. Novel associations between p97 and other proteins, including UBX-domain-containing proteins (UBX-polypeptides), HIF1α, and a variety of E3 ligases are provided herein. The disclosure provides complexes comprising UBX-domain-containing polypeptides (UBX-polypeptides) and other polypeptides involved in the degradation of ubiquitinated proteins. In addition, the disclosure provides uses for active agents that modulate protein-protein complex formation between an UBX-polypeptide and its complementary-binding substrate. For example, the disclosure provides methods for treating or preventing hypoxia-related disorders or conditions in a patient or a cell by administration of an active agent that modulates the activity of an UBX-polypeptide and/or its complementary binding-substrate. Furthermore, the disclosure provides uses for active agents that modulate HIF1α activity; such agents may be used to modulate processes that are regulated by HIF1α. The disclosure also provides many screening assays to identify test agents that modulate complex formation between an UBX-polypeptide and its complementary-binding substrate or methods for evaluating modes of action and/or effects of active agents that have already been identified as modulators of an UBX-polypeptide and/or its complementary-binding substrate.
摘要翻译：缺氧是一种低于正常组织氧气紧张度的状态，最近已经涉及许多人类疾病，包括癌症，心脏病和神经障碍。本文提供了p97和其他蛋白质（包括含UBX结构域的蛋白质（UBX-多肽），HIF1α和各种E3连接酶）之间的新型关联。本公开提供了包含含有UBX结构域的多肽（UBX-多肽）和参与泛素化蛋白质降解的其它多肽的复合物。此外，本公开提供了调节UBX-多肽与其互补结合底物之间的蛋白质 - 蛋白质复合物形成的活性剂的用途。例如，本公开提供了通过施用调节UBX-多肽和/或其互补结合底物的活性的活性剂来治疗或预防患者或细胞中的缺氧相关病症或病症的方法。此外，本公开提供了调节HIF1α活性的活性剂的用途; 这些药剂可用于调节由HIF1α调节的过程。本公开还提供了许多筛选测定法，以鉴定调节UBX-多肽及其互补结合底物之间的复合物形成的测试剂或用于评估已被鉴定为UBX调节剂的活性剂的作用模式和/或效果的方法 - 多肽和/或其互补结合底物。

7. 发明授权

US07291494B2 Regulation of target protein activity through modifier proteins 有权
标题翻译：通过修饰蛋白调节靶蛋白活性
公开(公告)号：US07291494B2
公开(公告)日：2007-11-06
申请号：US10047253
申请日：2002-01-14
申请人： Gregory Cope , Rati Verma , Lakshminarayanan Aravind , Eugene V. Koonin , Raymond Deshaies , Xavier Ambroggio
发明人： Gregory Cope , Rati Verma , Lakshminarayanan Aravind , Eugene V. Koonin , Raymond Deshaies , Xavier Ambroggio
IPC分类号： C12N9/48 , C12N9/00 , C12Q1/00 , C12Q1/68 , C23Q1/37 , C07H21/04 , A01N25/00
CPC分类号： C12N9/16 , A61K38/00 , C07K14/705 , C12N9/48 , C12N9/6489 , C12Q1/37 , G01N2500/02
摘要： The present invention is based on the discovery that a polypeptide containing the JAB subunit or the JAM domain has peptidase activity, e.g., isopeptidase activity. The present invention provides polypeptides and crystalline polypeptides containing the JAM domain and methods of using such polypeptides to screen for agents capable of affecting the peptidase activity of the polypeptides. The present invention also provides methods of using the JAM domain for rational drug design or identifying agents capable of affecting the peptidase activity of the JAM domain.
摘要翻译：本发明基于以下发现：含有JAB亚基或JAM结构域的多肽具有肽酶活性，例如肽酶活性。本发明提供含有JAM结构域的多肽和结晶多肽以及使用这些多肽筛选能够影响多肽的肽酶活性的试剂的方法。本发明还提供了使用JAM结构域进行合理药物设计或鉴定能够影响JAM结构域的肽酶活性的试剂的方法。

8. 发明授权

US06846663B2 Regulation of target protein activity through modifier proteins 有权
标题翻译：通过修饰蛋白调节靶蛋白活性
公开(公告)号：US06846663B2
公开(公告)日：2005-01-25
申请号：US10046961
申请日：2002-01-14
申请人： Svetlana A. Lyapina , Rati Verma , Raymond Deshaies , Greg Cope
发明人： Svetlana A. Lyapina , Rati Verma , Raymond Deshaies , Greg Cope
IPC分类号： A61K38/00 , C07K14/705 , C12N9/16 , C12N9/48 , C12N9/50 , C12N9/64 , C12Q1/37 , C12N9/76
CPC分类号： C12N9/16 , A61K38/00 , C07K14/705 , C12N9/48 , C12N9/6489 , C12Q1/37 , G01N2500/02
摘要： The present invention is based on the discovery that a polypeptide containing the JAB subunit or the JAM domain has peptidase activity, e.g., isopeptidase activity. The present invention provides polypeptides and crystalline polypeptides containing the JAM domain and methods of using such polypeptides to screen for agents capable of affecting the peptidase activity of the polypeptides. The present invention also provides methods of using the JAM domain for rational drug design or identifying agents capable of affecting the peptidase activity of the JAM domain.
摘要翻译：本发明基于以下发现：含有JAB亚基或JAM结构域的多肽具有肽酶活性，例如肽酶活性。本发明提供含有JAM结构域的多肽和结晶多肽以及使用这些多肽筛选能够影响多肽的肽酶活性的试剂的方法。本发明还提供了使用JAM结构域进行合理药物设计或鉴定能够影响JAM结构域的肽酶活性的试剂的方法。

9. 发明授权

US06165731A Assay for the ubiquitination-promoting activity of human proteins 失效
标题翻译：测定人类蛋白质泛素化促进活性
公开(公告)号：US06165731A
公开(公告)日：2000-12-26
申请号：US235572
申请日：1999-01-22
申请人： Raymond Deshaies , Svetlana Lyapina , Craig C. Correll
发明人： Raymond Deshaies , Svetlana Lyapina , Craig C. Correll
IPC分类号： C07K16/14 , C07K16/18 , C12Q1/25 , G01N33/53 , A61K39/395 , C07K16/00 , C12P13/18 , G01N33/573
CPC分类号： C07K16/18 , C07K16/14 , C12Q1/25 , G01N2333/9015 , G01N2500/00
摘要： A method is provided for identifying an compound that affects an activity of a polypeptide subunit of a SCF complex. The method includes contacting a sample comprising a chimeric SCF complex assembled from subunits derived from Saccharomyces cerevisiae or human and another species and a CDC34p polypeptide with the compound under conditions that allow the components to interact, and adding to these components an E1 enzyme, ubiquitin and ATP, and a SCF substrate. The ubiquitination of the SCF substrate is measured. A chimeric in vitro assay system is provided for measuring CDC53p or CUL1p activity, comprising a CDC4p, CDC34p, and a SKP1p polypeptide, and either a CDC53p or CUL1p polypeptide. In this assay the CDC4p, CDC34p, and SKP1p polypeptide are either a yeast polypeptide or a polypeptide from another species, and at least one of the CDC4p, CDC34p, and SKP1p polypeptides is a yeast polypeptide and at least one of the CDC4p, CDC34p, and SKP1p polypeptides is a polypeptide from another species. A method is further provided for identifying a compound that affects the ability of a CDC4p, a SKP1p, a CDC34p, and a CDC53p or a CUL1p to ubiquitinate a substrate. The method includes contacting a sample comprising a CDC4p, a SKP1p, a CDC34p, and a CDC53p or CUL1p, with the compound under conditions sufficient to allow the components to interact, and adding to these components an E1 enzyme, ubiquitin and ATP, and a substrate for ubiquitination. The ability of the CDC4p, the SKP1p, the CDC34p, and the CDC53p or CUL1p, to ubiquitinate the substrate is measured. A method is also provided of identifying a polypeptide having a function of a CDC4 subunit of SCF. A method is further provided for identifying a polypeptide as a substrate for a ubiquitination reaction.
摘要翻译：提供了用于鉴定影响SCF复合物的多肽亚基的活性的化合物的方法。该方法包括在允许组分相互作用的条件下将包含由来自酿酒酵母（Saccharomyces cerevisiae）或人与另一物种的亚基组装的样品与CDC34p多肽与所述化合物接触，并将E1酶，泛素和 ATP和SCF底物。测量SCF底物的泛素化。提供嵌合体外测定系统用于测量CDC53p或CUL1p活性，其包含CDC4p，CDC34p和SKP1p多肽，以及CDC53p或CUL1p多肽。在该测定中，CDC4p，CDC34p和SKP1p多肽是酵母多肽或来自另一物种的多肽，并且CDC4p，CDC34p和SKP1p多肽中的至少一个是酵母多肽，并且CDC4p，CDC34p，和SKP1p多肽是来自另一物种的多肽。还提供了一种鉴定影响CDC4p，SKP1p，CDC34p和CDC53p或CUL1p泛素化底物的能力的化合物的方法。该方法包括使包含CDC4p，SKP1p，CDC34p和CDC53p或CUL1p的样品与足以允许组分相互作用的条件下与化合物接触，并将E1酶，泛素和ATP以及底物用于泛素化。测量CDC4p，SKP1p，CDC34p和CDC53p或CUL1p的泛素化底物的能力。还提供了鉴定具有SCF的CDC4亚基的功能的多肽的方法。还提供了一种鉴定多肽作为泛素化反应底物的方法。

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