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公开(公告)号：US08895245B2
公开(公告)日：2014-11-25
申请号：US13230703
申请日：2011-09-12
申请人： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
发明人： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
IPC分类号： C12Q1/68 , C07D493/04 , A61K31/7076 , C07D473/34 , C12Q1/48 , G01N33/50 , G01N33/574 , A61P35/00 , C07H21/00 , C07H21/04
CPC分类号： A61K31/7076 , C07D473/34 , C07D493/04 , C12Q1/48 , C12Q1/6876 , G01N33/5011 , G01N33/57426 , G01N2333/91011
摘要： The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
摘要翻译： 本发明涉及抑制人组蛋白甲基转移酶EZH2的野生型和某些突变体形式，其是催化组蛋白H3（H3-K27）上赖氨酸27的单通三甲基化的PRC2复合物的催化亚单位。 在一个实施方案中，抑制对于EZH2的突变体形式是选择性的，使得与某些癌症相关的H3-K27的三甲基化被抑制。 该方法可用于治疗包括滤泡性淋巴瘤和弥漫性大B细胞淋巴瘤（DLBCL）的癌症。 还提供了用于鉴定EZH2的突变形式的小分子选择性抑制剂的方法以及用于测定受试者中对EZH2抑制剂的反应性的方法。
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公开(公告)号：US20120071418A1
公开(公告)日：2012-03-22
申请号：US13230703
申请日：2011-09-12
申请人： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
发明人： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
IPC分类号： A61K38/00 , C12Q1/68 , G01N33/574 , G01N33/566 , A61P35/00 , C07H19/19 , A61K31/7076 , G01N33/567 , C12N5/02
CPC分类号： A61K31/7076 , C07D473/34 , C07D493/04 , C12Q1/48 , C12Q1/6876 , G01N33/5011 , G01N33/57426 , G01N2333/91011
摘要： The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
摘要翻译： 本发明涉及抑制人组蛋白甲基转移酶EZH2的野生型和某些突变体形式，其是催化组蛋白H3（H3-K27）上赖氨酸27的单通三甲基化的PRC2复合物的催化亚单位。 在一个实施方案中，抑制对于EZH2的突变体形式是选择性的，使得与某些癌症相关的H3-K27的三甲基化被抑制。 该方法可用于治疗包括滤泡性淋巴瘤和弥漫性大B细胞淋巴瘤（DLBCL）的癌症。 还提供了用于鉴定EZH2的突变形式的小分子选择性抑制剂的方法以及用于测定受试者中对EZH2抑制剂的反应性的方法。
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3.发明授权Antibodies to aggrecan-degrading metalloprotease and diagnostic methods using same 有权抗凝集素降解金属蛋白酶的抗体及其使用的诊断方法公开(公告)号：US07049412B1
公开(公告)日：2006-05-23
申请号：US09634287
申请日：2000-08-09
申请人： Elizabeth C. Arner , Timothy C. Burn , Robert A. Copeland , Carl P. Decicco , Ruiqin Liu , Ronald Magolda , Michael Pratta , Kimberly A. Solomon , Micky D. Tortorella , James M. Trzaskos , Fude Yang
发明人： Elizabeth C. Arner , Timothy C. Burn , Robert A. Copeland , Carl P. Decicco , Ruiqin Liu , Ronald Magolda , Michael Pratta , Kimberly A. Solomon , Micky D. Tortorella , James M. Trzaskos , Fude Yang
IPC分类号： C07K16/00
CPC分类号： C12N9/6489 , A61K38/00 , C07K16/40 , C12Q1/37 , G01N33/6887 , G01N2333/96486 , G01N2500/00 , G01N2800/102
摘要： The invention is directed to the family of aggrecan degrading metallo proteases (ADMPs) that exhibit the ability to cleave the aggrecan core protein between amino acid residues Glu373-Ala374. The invention encompasses the nucleic acids encoding such enzymes, processes for production of recombinant ADMPs, compositions containing such enzymes, and the use of these enzymes in various assays and for the development of novel inhibitors for use as therapies for diseases involving aggrecanase-mediated degradation of cartilage or other aggrecanase-associated diseases.
摘要翻译： 本发明涉及聚集蛋白聚糖降解性金属蛋白酶（ADMP）的家族，其表现出在聚集蛋白聚糖核心蛋白之间切割氨基酸残基Glu 373之间的能力。 本发明包括编码这些酶的核酸，重组ADMP的生产方法，含有这些酶的组合物，以及这些酶在各种测定中的用途以及用于开发用于治疗涉及聚蛋白聚糖蛋白聚糖酶介导的降解的疾病的新型抑制剂 软骨或其他聚集蛋白聚糖相关疾病。
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4.发明授权Beta secretase exosite binding peptides and methods for identifying beta secretase modulators 有权β分泌酶外切位点结合肽和用于鉴定β分泌酶调节剂的方法公开(公告)号：US07314726B2
公开(公告)日：2008-01-01
申请号：US10685898
申请日：2003-10-15
申请人： Michael G. Kornacker , Robert A. Copeland , Joseph Hendrick , Zhihong Lai , Claudio Mapelli , Mark Richard Witmer , Jovita Marcinkeviciene , William Metzler , Ving Lee , Douglas James Riexinger
发明人： Michael G. Kornacker , Robert A. Copeland , Joseph Hendrick , Zhihong Lai , Claudio Mapelli , Mark Richard Witmer , Jovita Marcinkeviciene , William Metzler , Ving Lee , Douglas James Riexinger
IPC分类号： G01N33/53
CPC分类号： C07K7/08 , C07K1/04 , C07K1/042 , C07K7/06 , C07K14/005 , C07K14/4702 , C07K14/4711 , C12N2740/16122
摘要： The present invention provides peptides that specifically bind to BACE at a newly discovered exosite. The invention also provides methods for identifying peptides that bind to a BACE exosite. The invention further provides methods for identifying compounds that bind to a BACE exosite and modulate BACE activity. In another aspect, the invention provides methods for treating or preventing neurodegenerative disorders such as Alzheimer's disease by administering compounds that bind to a BACE exosite and modulate BACE activity.
摘要翻译： 本发明提供了在新发现的外部位点特异性结合BACE的肽。 本发明还提供了鉴定与BACE外部位点结合的肽的方法。 本发明还提供用于鉴定结合BACE外部位点并调节BACE活性的化合物的方法。 另一方面，本发明提供了通过施用与BACE外部位点结合并调节BACE活性的化合物来治疗或预防神经变性疾病如阿尔茨海默病的方法。
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5.发明授权公开(公告)号：US06844318B2
公开(公告)日：2005-01-18
申请号：US09808832
申请日：2001-03-15
申请人： Robert A. Copeland , Charles F. Albright , Andrew P. Combs , Randine L. Dowling , Nilsa R. Graciani , Wei Han , C. Anne Higley , Pearl S. Huang , Eddy W. Yue , Susan V. DiMeo
发明人： Robert A. Copeland , Charles F. Albright , Andrew P. Combs , Randine L. Dowling , Nilsa R. Graciani , Wei Han , C. Anne Higley , Pearl S. Huang , Eddy W. Yue , Susan V. DiMeo
IPC分类号： A61K31/704 , A61K38/00 , A61K47/48 , A61P35/00 , A61P35/02 , C07K5/02 , C07K5/04 , C07K5/117 , C07K7/06 , A61K38/07 , A61K38/08 , A61K38/14
摘要： This invention is directed to antineoplastic agents conjugated to enzyme-cleavable peptides comprising the amino acid recognition sequence of a membrane-bound and/or cell-secreted peptidase, and to the use of such conjugated compounds as chemotherapeutic agents in the targeted treatment of cancers.
摘要翻译： 本发明涉及与包含膜结合和/或细胞分泌的肽酶的氨基酸识别序列的酶切割肽缀合的抗肿瘤剂，以及在靶向治疗癌症中使用这些缀合化合物作为化学治疗剂。
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6.发明授权Assays and peptide substrate for determining aggrecan degrading metallo protease activity 失效用于测定聚集蛋白聚糖降解金属蛋白酶活性的测定和肽底物公开(公告)号：US07223834B2
公开(公告)日：2007-05-29
申请号：US09975813
申请日：2001-10-12
申请人： Jeffrey A. Miller , Elizabeth C. Arner , Robert A. Copeland , Gary L. Davis , Ruiqin Liu , Michael A. Pratta , Micky D. Tortorella
发明人： Jeffrey A. Miller , Elizabeth C. Arner , Robert A. Copeland , Gary L. Davis , Ruiqin Liu , Michael A. Pratta , Micky D. Tortorella
CPC分类号： C12N9/6489 , A61K38/00 , C07K16/40 , C12Q1/37 , G01N33/6887 , G01N2333/96486 , G01N2500/00 , G01N2800/102
摘要： This invention is directed to assays to determine the presence or absence of proteins that exhibit aggrecanase or ADMP activity. This invention also relates to peptides that acts as a substrates for ADMPs, their use in various assays to determine the presence or absence of ADMP activity, and their use as inhibitors of ADMP activity.
摘要翻译： 本发明涉及确定存在或不存在表现出聚集蛋白聚糖蛋白聚糖酶或ADMP活性的蛋白质的测定法。 本发明还涉及作为ADMP底物的肽，其用于各种测定以确定ADMP活性的存在或不存在，以及它们作为ADMP活性抑制剂的用途。
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7.发明授权Assays and peptide substrate for determining aggrecan degrading metallo protease activity 失效用于测定聚集蛋白聚糖降解金属蛋白酶活性的测定和肽底物公开(公告)号：US06326162B1
公开(公告)日：2001-12-04
申请号：US09122127
申请日：1998-07-24
申请人： Jeffrey A. Miller , Elizabeth C. Arner , Robert A. Copeland , Gary L. Davis , Ruiqin Liu , Michael Pratta , Micky D. Tortorella
发明人： Jeffrey A. Miller , Elizabeth C. Arner , Robert A. Copeland , Gary L. Davis , Ruiqin Liu , Michael Pratta , Micky D. Tortorella
IPC分类号： C12Q137
CPC分类号： C12N9/6489 , A61K38/00 , C07K16/40 , C12Q1/37 , G01N33/6887 , G01N2333/96486 , G01N2500/00 , G01N2800/102
摘要： This invention is directed to assays to determine the presence or absence of proteins that exhibit aggrecanase or ADMP activity. This invention also relates to peptides that acts as a substrates for ADMPs, their use in various assays to determine the presence or absence of ADMP activity, and their use as inhibitors of ADMP activity.
摘要翻译： 本发明涉及确定存在或不存在表现出聚集蛋白聚糖蛋白聚糖酶或ADMP活性的蛋白质的测定法。 本发明还涉及作为ADMP底物的肽，其用于各种测定以确定ADMP活性的存在或不存在，以及它们作为ADMP活性抑制剂的用途。
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公开(公告)号：US06753176B2
公开(公告)日：2004-06-22
申请号：US10247685
申请日：2002-09-19
申请人： Elizabeth C. Arner , Timothy C. Burn , Robert A. Copeland , Carl P. Decicco , Ruiqin Liu , Ronald Magolda , Michael Pratta , Kimberly A. Solomon , Micky D. Tortorella , James M. Trzaskos , Fude Yang
发明人： Elizabeth C. Arner , Timothy C. Burn , Robert A. Copeland , Carl P. Decicco , Ruiqin Liu , Ronald Magolda , Michael Pratta , Kimberly A. Solomon , Micky D. Tortorella , James M. Trzaskos , Fude Yang
IPC分类号： C12N964
CPC分类号： C12N9/6489 , A61K38/00 , C07K16/40 , C12Q1/37 , G01N33/6887 , G01N2333/96486 , G01N2500/00 , G01N2800/102
摘要： The invention is directed to the family of aggrecan degrading metallo proteases (ADMPs) that exhibit the ability to cleave the aggrecan core protein between amino acid residues Glu373-Ala374. The invention encompasses the nucleic acids encoding such enzymes, processes for production of recombinant ADMPs, compositions containing such enzymes, and the use of these enzymes in various assays and for the development of novel inhibitors for use as therapies for diseases involving aggrecanase-mediated degradation of cartilage or other aggrecanase-associated diseases.
摘要翻译： 本发明涉及聚集蛋白聚糖降解金属蛋白酶（ADMP）家族，其表现出在氨基酸残基Glu <373> -Ala <374>之间切割聚蛋白聚糖核心蛋白的能力。 本发明包括编码这些酶的核酸，重组ADMP的生产方法，含有这些酶的组合物，以及这些酶在各种测定中的用途以及用于开发用于治疗涉及聚蛋白聚糖蛋白聚糖酶介导的降解的疾病的新型抑制剂 软骨或其他聚集蛋白聚糖相关疾病。
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公开(公告)号：US06521436B1
公开(公告)日：2003-02-18
申请号：US09634286
申请日：2000-08-09
申请人： Elizabeth C. Arner , Timothy C. Burn , Robert A. Copeland , Carl P. Decicco , Ruiqin Liu , Ronald Magolda , Michael Pratta , Kimberly A. Solomon , Micky D. Tortorella , James M. Trzaskos , Fude Yang
发明人： Elizabeth C. Arner , Timothy C. Burn , Robert A. Copeland , Carl P. Decicco , Ruiqin Liu , Ronald Magolda , Michael Pratta , Kimberly A. Solomon , Micky D. Tortorella , James M. Trzaskos , Fude Yang
IPC分类号： C12N964
CPC分类号： C12N9/6489 , A61K38/00 , C07K16/40 , C12Q1/37 , G01N33/6887 , G01N2333/96486 , G01N2500/00 , G01N2800/102
摘要： The invention is directed to the family of aggrecan degrading metallo proteases (ADMPs) that exhibit the ability to cleave the aggrecan core protein between amino acid residues Glu373-Ala374. The invention encompasses the nucleic acids encoding such enzymes, processes for production of recombinant ADMPs, compositions containing such enzymes, and the use of these enzymes in various assays and for the development of novel inhibitors for use as therapies for diseases involving aggrecanase-mediated degradation of cartilage or other aggrecanase-associated diseases.
摘要翻译： 本发明涉及聚集蛋白聚糖降解金属蛋白酶（ADMP）家族，其表现出在氨基酸残基Glu373-Ala374之间切割聚蛋白聚糖核心蛋白的能力。 本发明包括编码这种酶的核酸，重组ADMP的生产方法，含有这些酶的组合物，以及这些酶在各种测定中的用途以及用于开发用于治疗涉及聚蛋白聚糖蛋白聚糖酶介导的降解的疾病的新型抑制剂 软骨或其他聚集蛋白聚糖相关疾病。
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公开(公告)号：US06451575B1
公开(公告)日：2002-09-17
申请号：US09122126
申请日：1998-07-24
申请人： Elizabeth C. Arner , Timothy C. Burn , Robert A. Copeland , Carl P. Decicco , Ruiqin Liu , Ronald Magolda , Michael Pratta , Kimberly A. Solomon , Micky D. Tortorella , James M. Trzaskos , Fude Yang
发明人： Elizabeth C. Arner , Timothy C. Burn , Robert A. Copeland , Carl P. Decicco , Ruiqin Liu , Ronald Magolda , Michael Pratta , Kimberly A. Solomon , Micky D. Tortorella , James M. Trzaskos , Fude Yang
IPC分类号： C12N964
CPC分类号： C12N9/6489 , A61K38/00 , C07K16/40 , C12Q1/37 , G01N33/6887 , G01N2333/96486 , G01N2500/00 , G01N2800/102
摘要： The invention is directed to the family of aggrecan degrading metallo proteases (ADMPs) that exhibit the ability to cleave the aggrecan core protein between amino acid residues Glu373-Ala374. The invention encompasses the nucleic acids encoding such enzymes, processes for production of recombinant ADMPs, compositions containing such enzymes, and the use of these enzymes in various assays and for the development of novel inhibitors for use as therapies for diseases involving aggrecanase-mediated degradation of cartilage or other aggrecanase-associated diseases.
摘要翻译： 本发明涉及聚集蛋白聚糖降解金属蛋白酶（ADMP）家族，其表现出在氨基酸残基Glu373-Ala374之间切割聚蛋白聚糖核心蛋白的能力。 本发明包括编码这些酶的核酸，重组ADMP的生产方法，含有这些酶的组合物，以及这些酶在各种测定中的用途以及用于开发用于治疗涉及聚蛋白聚糖蛋白聚糖酶介导的降解的疾病的新型抑制剂 软骨或其他聚集蛋白聚糖相关疾病。
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