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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。
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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
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。
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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
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。
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公开(公告)号：US07279317B2
公开(公告)日：2007-10-09
申请号：US10340578
申请日：2003-01-09
CPC分类号： C12N9/6489 , A61K38/00 , C07K14/705 , C12N9/16 , C12N9/48 , C12Q1/37 , G01N2500/02
摘要： Methods for identifying agents that can increase or decrease the isopeptidase activity of a COP9 signalsome (CSN) are provided, as are agent identified using such screening assays. In addition, methods of ameliorating a pathologic condition such as a cancer or an autoimmune disease in a subject by modulating the CSN isopeptidase activity are provided, as are medicaments useful for treating a subject having such a condition.
摘要翻译： 提供了用于鉴定可以增加或降低COP9信号素（CSN）的肽酶活性的试剂的方法，以及使用这种筛选试验鉴定的试剂。 此外，提供了通过调节CSN类肽酶活性来改善受试者的病理状况如癌症或自身免疫性疾病的方法，以及可用于治疗患有这种病症的受试者的药物。
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