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1.发明申请Methods to identify compounds useful for the treatment of proliferative and differentiative disorders 有权鉴定可用于治疗增殖性和分化性疾病的化合物的方法公开(公告)号：US20090297528A1
公开(公告)日：2009-12-03
申请号：US12315862
申请日：2008-12-05
IPC分类号： A61K39/395 , C12Q1/00 , G01N33/53 , C12Q1/68 , A61K38/02 , A61K31/7088
CPC分类号： G01N33/5023 , A61K31/7088 , A61K38/02 , A61K38/1709 , A61K39/3955 , G01N33/573 , G01N33/574 , G01N2333/4703 , G01N2333/9015 , G01N2500/00 , G01N2500/04
摘要： The present invention relates to the discovery, identification and characterization of nucleotide sequences that encode novel substrate-targeting subunits of ubiquitin ligases. The invention encompasses nucleotides encoding novel substrate-targeting subunits of ubiquitin ligases: FBP1, FBP2, FBP3, FBP4, FBP5, FBP6, FBP7, FBP8, FBP9, FBP10, FBP11, FBP12, FBP13, FBP14, FBP15, FBP16, FBP17, FBP18, FBP19, FBP20, FBP21, FBP22, FBP23, FBP24, and FBP25, transgenic mice, knock-out mice, host-cell expression systems and proteins encoded by the nucleotides of the novel substrate-targeting subunits. The present invention relates to screening assays that use novel and known substrate-targeting subunits of ubiquitin ligases to identify potential therapeutic agents such as small molecules, compounds or derivatives and analogues of the novel and known ubiquitin ligases which modulate activity of the novel and known ubiquitin ligases for the treatment of proliferative and differentiative disorders, such as cancer, major opportunistic infections, immune disorders, certain cardiovascular diseases, and inflammatory disorders. The invention further encompasses therapeutic protocols and pharmaceutical compositions designed to target ubiquitin ligases and their substrates for the treatment of proliferative and differentiative disorders.
摘要翻译： 本发明涉及编码泛素连接酶的新的底物靶向亚基的核苷酸序列的发现，鉴定和表征。 本发明包括编码泛素连接酶的新型底物靶向亚基的核苷酸：FBP1，FBP2，FBP3，FBP4，FBP5，FBP6，FBP7，FBP8，FBP9，FBP10，FBP11，FBP12，FBP13，FBP14，FBP15，FBP16，FBP17，FBP18， FBP19，FBP20，FBP21，FBP22，FBP23，FBP24和FBP25，转基因小鼠，敲除小鼠，宿主细胞表达系统和由新型底物靶向亚基的核苷酸编码的蛋白质。 本发明涉及使用泛素连接酶的新型和已知的底物靶向亚基的筛选测定法来鉴定潜在的治疗剂，例如调节新型和已知的泛素的活性的新型和已知的泛素连接酶的小分子，化合物或衍生物和类似物 用于治疗增殖性和分化性疾病如癌症，主要机会性感染，免疫疾病，某些心血管疾病和炎症性疾病的连接酶。 本发明还包括旨在靶向泛素连接酶及其底物以治疗增殖性和分化性疾病的治疗方案和药物组合物。
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2.发明申请公开(公告)号：US20060088846A1
公开(公告)日：2006-04-27
申请号：US11106014
申请日：2005-04-13
CPC分类号： G01N33/5023 , A61K31/7088 , A61K38/02 , A61K38/1709 , A61K39/3955 , G01N33/573 , G01N33/574 , G01N2333/4703 , G01N2333/9015 , G01N2500/00 , G01N2500/04
摘要： The present invention relates to the discovery, identification and characterization of nucleotide sequences that encode novel substrate-targeting subunits of ubiquitin ligases. The invention encompasses nucleotides encoding novel substrate-targeting subunits of ubiquitin ligases: FBP1, FBP2, FBP3, FBP4, FBP5, FBP6, FBP7, FBP8, FBP9, FBP10, FBP11, FBP12, FBP13, FBP14, FBP15, FBP16, FBP17, FBP18, FBP19, FBP20, FBP21, FBP22, FBP23, FBP24, and FBP25, transgenic mice, knock-out mice, host-cell expression systems and proteins encoded by the nucleotides of the novel substrate-targeting subunits. The present invention relates to screening assays that use novel and known substrate-targeting subunits of ubiquitin ligases to identify potential therapeutic agents such as small molecules, compounds or derivatives and analogues of the novel and known ubiquitin ligases which modulate activity of the novel and known ubiquitin ligases for the treatment of proliferative and differentiative disorders, such as cancer, major opportunistic infections, immune disorders, certain cardiovascular diseases, and inflammatory disorders. The invention further encompasses therapeutic protocols and pharmaceutical compositions designed to target ubiquitin ligases and their substrates for the treatment of proliferative and differentiative disorders.
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3.发明申请Methods To Identify Compounds Useful For The Treatment Of Proliferative And Differentiative Disorders 审中-公开识别可用于增殖和分化障碍治疗的化合物的方法公开(公告)号：US20120164656A1
公开(公告)日：2012-06-28
申请号：US13323227
申请日：2011-12-12
IPC分类号： C12Q1/68 , G01N33/566 , G01N33/53
CPC分类号： G01N33/5023 , A61K31/7088 , A61K38/02 , A61K38/1709 , A61K39/3955 , G01N33/573 , G01N33/574 , G01N2333/4703 , G01N2333/9015 , G01N2500/00 , G01N2500/04
摘要： The present invention relates to the discovery, identification and characterization of nucleotide sequences that encode novel substrate-targeting subunits of ubiquitin ligases. The invention encompasses nucleotides encoding novel substrate-targeting subunits of ubiquitin ligases, and transgenic mice, knock-out mice, host-cell expression systems and proteins encoded by the nucleotides of the novel substrate-targeting subunits. The present invention relates to screening assays that use novel and known substrate-targeting subunits of ubiquitin ligases to identify potential therapeutic agents such as small molecules, compounds or derivatives and analogues of the novel and known ubiquitin ligases which modulate activity of the novel and known ubiquitin ligases for the treatment of proliferative and differentiative disorders, such as cancer, major opportunistic infections, immune disorders, certain cardiovascular diseases, and inflammatory disorders. The invention further encompasses therapeutic protocols and pharmaceutical compositions designed to target ubiquitin ligases and their substrates for the treatment of proliferative and differentiative disorders.
摘要翻译： 本发明涉及编码泛素连接酶的新的底物靶向亚基的核苷酸序列的发现，鉴定和表征。 本发明包括编码泛素连接酶的新的底物靶向亚基的核苷酸，以及转基因小鼠，敲除小鼠，宿主细胞表达系统和由新型底物靶向亚基的核苷酸编码的蛋白质。 本发明涉及使用泛素连接酶的新型和已知的底物靶向亚基的筛选测定法来鉴定潜在的治疗剂，例如调节新型和已知的泛素的活性的新型和已知的泛素连接酶的小分子，化合物或衍生物和类似物 用于治疗增殖性和分化性疾病如癌症，主要机会性感染，免疫疾病，某些心血管疾病和炎症性疾病的连接酶。 本发明还包括旨在靶向泛素连接酶及其底物以治疗增殖性和分化性疾病的治疗方案和药物组合物。
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4.发明授权Methods to identify compounds useful for the treatment of proliferative and differentiative disorders 有权鉴定可用于治疗增殖性和分化性疾病的化合物的方法公开(公告)号：US08119421B2
公开(公告)日：2012-02-21
申请号：US12315862
申请日：2008-12-05
IPC分类号： G01N33/566 , G01N33/53 , C12Q1/00 , C12Q1/68
CPC分类号： G01N33/5023 , A61K31/7088 , A61K38/02 , A61K38/1709 , A61K39/3955 , G01N33/573 , G01N33/574 , G01N2333/4703 , G01N2333/9015 , G01N2500/00 , G01N2500/04
摘要： The present invention relates to the discovery, identification and characterization of nucleotide sequences that encode novel substrate-targeting subunits of ubiquitin ligases. The invention encompasses nucleotides encoding novel substrate-targeting subunits of ubiquitin ligases: FBP1, FBP2, FBP3, FBP4, FBP5, FBP6, FBP7, FBP8, FBP9, FBP10, FBP11, FBP12, FBP13, FBP14, FBP15, FBP16, FBP17, FBP18, FBP19, FBP20, FBP21, FBP22, FBP23, FBP24, and FBP25, transgenic mice, knock-out mice, host-cell expression systems and proteins encoded by the nucleotides of the novel substrate-targeting subunits. The present invention relates to screening assays that use novel and known substrate-targeting subunits of ubiquitin ligases to identify potential therapeutic agents such as small molecules, compounds or derivatives and analogues of the novel and known ubiquitin ligases which modulate activity of the novel and known ubiquitin ligases for the treatment of proliferative and differentiative disorders, such as cancer, major opportunistic infections, immune disorders, certain cardiovascular diseases, and inflammatory disorders. The invention further encompasses therapeutic protocols and pharmaceutical compositions designed to target ubiquitin ligases and their substrates for the treatment of proliferative and differentiative disorders.
摘要翻译： 本发明涉及编码泛素连接酶的新的底物靶向亚基的核苷酸序列的发现，鉴定和表征。 本发明包括编码泛素连接酶的新型底物靶向亚基的核苷酸：FBP1，FBP2，FBP3，FBP4，FBP5，FBP6，FBP7，FBP8，FBP9，FBP10，FBP11，FBP12，FBP13，FBP14，FBP15，FBP16，FBP17，FBP18， FBP19，FBP20，FBP21，FBP22，FBP23，FBP24和FBP25，转基因小鼠，敲除小鼠，宿主细胞表达系统和由新型底物靶向亚基的核苷酸编码的蛋白质。 本发明涉及使用泛素连接酶的新型和已知的底物靶向亚基的筛选测定法来鉴定潜在的治疗剂，例如调节新型和已知的泛素的活性的新型和已知的泛素连接酶的小分子，化合物或衍生物和类似物 用于治疗增殖性和分化性疾病如癌症，主要机会性感染，免疫疾病，某些心血管疾病和炎症性疾病的连接酶。 本发明还包括旨在靶向泛素连接酶及其底物以治疗增殖性和分化性疾病的治疗方案和药物组合物。
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5.发明授权Compounds useful for the treatment of cancer, compositions thereof and methods therewith 失效可用于治疗癌症的化合物，其组合物和方法公开(公告)号：US07037936B2
公开(公告)日：2006-05-02
申请号：US10463009
申请日：2003-06-16
IPC分类号： A61K31/35
CPC分类号： A61K31/351 , A61K31/135 , A61K31/4025
摘要： The present invention generally relates to compounds and compositions useful for the modulation of ligase activity. The invention further relates to Compounds of the Invention, compositions thereof, and methods for treating or preventing cancer, a neoplastic disorder, acute or chronic renal failure, an inflammatory disorder, an immune disorder, a cardiovascular disease, an effect of aging or an infectious disease comprising administering an effective amount of a Compound of the Invention. The invention further relates to the use of a Compound of the Invention as a preservative of a cell, blood, tissue or an organ or as an agent to modulate stem cells.
摘要翻译： 本发明一般涉及可用于调节连接酶活性的化合物和组合物。 本发明还涉及本发明的化合物，其组合物，以及用于治疗或预防癌症，肿瘤性疾病，急性或慢性肾功能衰竭，炎症性疾病，免疫疾病，心血管疾病，衰老或感染性的影响的方法 疾病，包括施用有效量的本发明化合物。 本发明还涉及本发明的化合物作为细胞，血液，组织或器官的防腐剂或作为调节干细胞的药剂的用途。
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6.发明申请公开(公告)号：US20060142352A1
公开(公告)日：2006-06-29
申请号：US11357774
申请日：2006-02-17
IPC分类号： A61K31/44 , A61K31/40 , A61K31/277 , A61K31/195 , A61K31/165 , A61K31/137 , A61K31/18 , A61K31/175
CPC分类号： A61K31/351 , A61K31/135 , A61K31/4025
摘要： The present invention generally relates to compounds and compositions useful for the modulation of ligase activity. The invention further relates to Compounds of the Invention, compositions thereof, and methods for treating or preventing cancer, a neoplastic disorder, acute or chronic renal failure, an inflammatory disorder, an immune disorder, a cardiovascular disease, an effect of aging or an infectious disease comprising administering an effective amount of a Compound of the Invention. The invention further relates to the use of a Compound of the Invention as a preservative of a cell, blood, tissue or an organ or as an agent to modulate stem cells.
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7.发明申请COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER, COMPOSITIONS THEREOF AND METHODS THEREWITH 失效用于治疗癌症的组合物及其组合物及其方法公开(公告)号：US20060030617A1
公开(公告)日：2006-02-09
申请号：US10463009
申请日：2003-06-16
IPC分类号： A61K31/35 , A61K31/277 , A61K31/195 , A61K31/137
CPC分类号： A61K31/351 , A61K31/135 , A61K31/4025
摘要： The present invention generally relates to compounds and compositions useful for the modulation of ligase activity. The invention further relates to Compounds of the Invention, compositions thereof, and methods for treating or preventing cancer, a neoplastic disorder, acute or chronic renal failure, an inflammatory disorder, an immune disorder, a cardiovascular disease, an effect of aging or an infectious disease comprising administering an effective amount of a Compound of the Invention. The invention further relates to the use of a Compound of the Invention as a preservative of a cell, blood, tissue or an organ or as an agent to modulate stem cells.
摘要翻译： 本发明一般涉及可用于调节连接酶活性的化合物和组合物。 本发明还涉及本发明的化合物，其组合物，以及用于治疗或预防癌症，肿瘤性疾病，急性或慢性肾功能衰竭，炎症性疾病，免疫疾病，心血管疾病，衰老或感染性的影响的方法 疾病，包括施用有效量的本发明化合物。 本发明还涉及本发明的化合物作为细胞，血液，组织或器官的防腐剂或作为调节干细胞的药剂的用途。
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公开(公告)号：US20060194262A1
公开(公告)日：2006-08-31
申请号：US11253128
申请日：2005-10-17
申请人： Shuichan Xu , Sarah Cox , Weilin Xie , Frank Mercurio
发明人： Shuichan Xu , Sarah Cox , Weilin Xie , Frank Mercurio
IPC分类号： G01N33/53
CPC分类号： C12Q1/25 , G01N33/68 , G01N33/6842 , G01N33/6845 , G01N2500/00
摘要： This invention relates to easy and reliable assays for the ubiquitination of p27. Because the assay can be performed as a plate capture assay, or as a homogenous time-resolved fluorescence resonance energy transfer assay, with defined, easily replicatable reaction conditions, it is particularly useful for high-throughput screening of, for example, a prospective anticancer agent. The invention provides methods to determine the amount of ubiquitination of p27, or of any protein, and use of the method to identify compounds that modulate the ubiquitination of p27, or any protein.
摘要翻译： 本发明涉及用于p27泛素化的容易且可靠的测定。 因为测定可以作为板捕获测定法或作为具有确定的易于复制的反应条件的均匀时间分辨荧光共振能量转移测定来进行，所以它对于例如预期的抗癌剂的高通量筛选是特别有用的 代理商 本发明提供了确定p27或任何蛋白质的泛素化量的方法，以及使用该方法鉴定调节p27或任何蛋白质的泛素化的化合物。
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公开(公告)号：USD632434S1
公开(公告)日：2011-02-08
申请号：US29341645
申请日：2009-08-10
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公开(公告)号：USD621096S1
公开(公告)日：2010-08-03
申请号：US29341643
申请日：2009-08-10
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