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11 条记录 (耗时 0.041 秒)

    Compounds useful for the treatment of cancer, compositions thereof and methods therewith
    1.
    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

    申请人： Jeffrey McKenna ,  Frank Mercurio ,  Veronique Plantevin ,  Weilin Xie ,  Michele Pagano

    发明人： Jeffrey McKenna ,  Frank Mercurio ,  Veronique Plantevin ,  Weilin Xie ,  Michele Pagano

    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。

    COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER, COMPOSITIONS THEREOF AND METHODS THEREWITH
    3.
    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

    申请人： Jeffrey McKenna ,  Frank Mercurio ,  Veronique Plantevin ,  Weilin Xie

    发明人： Jeffrey McKenna ,  Frank Mercurio ,  Veronique Plantevin ,  Weilin Xie

    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。

    Methods To Identify Compounds Useful For The Treatment Of Proliferative And Differentiative Disorders
    5.
    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

    申请人： Michele Pagano ,  Frank Mercurio ,  Weilin Xie ,  Antonia Lopez-Girona ,  Angelo Peschiaroli

    发明人： Michele Pagano ,  Frank Mercurio ,  Weilin Xie ,  Antonia Lopez-Girona ,  Angelo Peschiaroli

    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。

    Methods to identify compounds useful for the treatment of proliferative and differentiative disorders
    6.
    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

    申请人： Michele Pagano ,  Frank Mercurio ,  Weilin Xie ,  Antonia Lopez-Girona ,  Angelo Peschiaroli

    发明人： Michele Pagano ,  Frank Mercurio ,  Weilin Xie ,  Antonia Lopez-Girona ,  Angelo Peschiaroli

    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。

    Methods to identify compounds useful for the treatment of proliferative and differentiative disorders
    7.
    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

    申请人： Michele Pagano ,  Frank Mercurio ,  Weilin Xie ,  Antonia Lopez-Girona ,  Angelo Peschiaroli

    发明人： Michele Pagano ,  Frank Mercurio ,  Weilin Xie ,  Antonia Lopez-Girona ,  Angelo Peschiaroli

    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。

    P27 ubiquitination assay and methods of use
    8.
    发明申请
    P27 ubiquitination assay and methods of use 审中-公开
    P27泛素化测定法及使用方法

    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。

    Methods for modulating signal transduction mediated by TGF-β and related proteins
    9.
    发明授权
    Methods for modulating signal transduction mediated by TGF-β and related proteins 失效
    调节由TGF-β和相关蛋白介导的信号转导的方法

    公开(公告)号：US07358056B1

    公开(公告)日：2008-04-15

    申请号：US09385918

    申请日：1999-08-30

    申请人： Merl F. Hoekstra ,  Weilin Xie ,  Brion W. Murray ,  Frank M. Mercurio

    发明人： Merl F. Hoekstra ,  Weilin Xie ,  Brion W. Murray ,  Frank M. Mercurio

    IPC分类号： G01N33/53

    CPC分类号： G01N33/74 ,  C12Q1/25 ,  G01N2333/495 ,  G01N2500/10

    摘要： Methods are provided for identifying agents that modulate signaling mediated by transforming growth factor beta (TGF-β) and members of the TGF-β family, such as bone morphogenic protein (BMP). Such agents may be identified using screens that evaluate candidate agents for the ability to modulate Smad protein degradation. Agents identified as described herein may be used to augment or inhibit signaling mediated by one or more TGF-β family members in a variety of cell types and for therapeutic purposes.

    摘要翻译： 提供了用于鉴定调节由转化生长因子β（TGF-β）和TGF-β家族成员如骨形态发生蛋白（BMP）介导的信号传导的试剂的方法。 可以使用筛选评估候选试剂以调节Smad蛋白降解能力的筛选来鉴定此类试剂。 如本文所述鉴定的药剂可用于增强或抑制由多种细胞类型中的一种或多种TGF-β家族成员介导的信号传导和用于治疗目的。