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1. 发明申请

WO2008063752A3 AN ENZYME REGULATING ETHER LIPID SIGNALING PATHWAYS 审中-公开
标题翻译：一种酶调节脂肪信号途径
公开(公告)号：WO2008063752A3
公开(公告)日：2008-10-30
申请号：PCT/US2007080222
申请日：2007-10-02
申请人： SCRIPPS RESEARCH INST , CRAVATT BENJAMIN F , CHIANG KYLE P , NIESSEN SHERRY , SAGHATELIAN ALAN
发明人： CRAVATT BENJAMIN F , CHIANG KYLE P , NIESSEN SHERRY , SAGHATELIAN ALAN
IPC分类号： A61K31/00 , C12Q1/34
CPC分类号： A61K31/325 , C12Q1/34 , G01N33/92 , G01N2500/02
摘要： A multidimensional profiling strategy that combines activity-based proteomics and metabolomics was used to determine that an active protein, which is a previously uncharacterized enzyme highly elevated in aggressive cancer cells, serves as a central node in an ether lipid signaling network that bridges platelet-activating factor and the lysophospholipids. Biochemical studies confirmed that the active protein regulates this pathway by hydrolyzing the metabolic intermediate 2-acetyl monoalkylglycerol. Inactivation of the active protein disrupted ether lipid metabolism in cancer cells and impaired cell migration and tumor growth in vivo.
摘要翻译：使用结合基于活性的蛋白质组学和代谢组学的多维分析策略来确定在侵袭性癌细胞中高度升高的先前未表征的酶的活性蛋白质作为桥联血小板活化的醚脂质信号传导网络中的中心节点因子和溶血磷脂。生物化学研究证实，活性蛋白通过水解代谢中间体2-乙酰单烷基甘油来调节该途径。活性蛋白的失活破坏了癌细胞中的乙醚脂质代谢，体内细胞迁移和肿瘤生长受损。

2. 发明申请

WO2006004598A3 PROTEOMIC ANALYSIS 审中-公开
公开(公告)号：WO2006004598A3
公开(公告)日：2006-01-12
申请号：PCT/US2005/019378
申请日：2005-06-01
申请人： THE SCRIPPS RESEARCH INSTITUTE , CRAVATT, Benjamin, F. , SAGHATELIAN, Alan , JESSANI, Nadim , JOSEPH, Arul
发明人： CRAVATT, Benjamin, F. , SAGHATELIAN, Alan , JESSANI, Nadim , JOSEPH, Arul
IPC分类号： C12C233/00 , C07D249/04 , C12N9/50 , C12Q1/37
摘要： Activity-based compositions for analyzing metalloproteases are disclosed, where the compositions include a chemical compound including a hydroxamate moiety and a benzophenone moiety. Methods for synthesizing these compounds are also disclosed, as well as methods of using them for determining the bioactivity of a compositions comprising active compounds toward a metalloproteases and for determining the potency of an inhibitor against a metalloprotease.

3. 发明申请

WO2003047509A2 ENZYME ACTIVITY PROFILES 审中-公开
标题翻译：酶活性概况
公开(公告)号：WO2003047509A2
公开(公告)日：2003-06-12
申请号：PCT/US2002/037942
申请日：2002-11-25
申请人： THE SCRIPPS RESEARCH INSTITUTE , CRAVATT, Benjamin, F.
发明人： CRAVATT, Benjamin, F.
IPC分类号： A61K
CPC分类号： C12N9/6424 , C12Q1/34 , G01N33/57496 , G01N2333/914
摘要： Methods and compositions are provided for evaluating cellular status related to neoplasia. Affinity based probes, particularly having fluorophosphonates as a reactive functionality, are employed that react with a family of enzymes having a common catalytic activity, particularly serine/threonine hydrolases. The probe(s) are combined with the cell components and resulting conjugates are characterized, where the profile of reaction indicates cellular status. A novel serine/threonine hydrolase enzyme is provided.
摘要翻译：提供了用于评估与瘤形成有关的细胞状态的方法和组合物。使用基于亲和性的探针，特别是具有氟代膦酸酯作为反应性官能团的探针，其与具有共同催化活性的酶家族特别是丝氨酸/苏氨酸水解酶反应。将探针与细胞组分结合，并对所得缀合物进行表征，其中反应曲线指示细胞状态。提供了一种新的丝氨酸/苏氨酸水解酶。

4. 发明申请

WO2001077684A3 PROTEOMIC ANALYSIS USING ACTIVITY-BASED PROBE LIBRARIES 审中-公开
公开(公告)号：WO2001077684A3
公开(公告)日：2001-10-18
申请号：PCT/US2000/034187
申请日：2000-12-15
申请人： THE SCRIPPS RESEARCH INSTITUTE , CRAVATT, Benjamin, F. , SORENSEN, Erik , PATRICELLI, Matthew , LOVATO, Martha , ADAM, Gregory
发明人： CRAVATT, Benjamin, F. , SORENSEN, Erik , PATRICELLI, Matthew , LOVATO, Martha , ADAM, Gregory
IPC分类号： G01N33/68
摘要： The present invention provides methods for analyzing proteomes, as cells or lysates. The analysis is based on the use of probes that have specificity to the active form of proteins, particularly enzymes and receptors. The probes can be identified in different ways. In accordance with the present invention, a method is provided for generating and screening compound libraries that are used for the identification of lead molecules, and for the parallel identification of their biological targets. By appending specific functionalities and/or groups to one or more binding moieties, the reactive functionalities gain binding affinity and specificity for particular proteins and classes of proteins. Such libraries of candidate compounds, referred to herein as activity-based probes, or ABPs, are used to screen for one or more desired biological activities or target proteins.

5. 发明申请

WO2004044169A2 CRYSTALLINE FORM OF FATTY ACID AMINE HYDROLASE (FAAH) 审中-公开
标题翻译：脂肪酸胺水解酶（FAAH）的结晶形式
公开(公告)号：WO2004044169A2
公开(公告)日：2004-05-27
申请号：PCT/US2003/036125
申请日：2003-11-14
申请人： THE SCRIPPS RESEARCH INSTITUTE , BRACEY, Michael, H. , HANSON, Michael, A. , STEVENS, Raymond, C. , CRAVATT, Benjamin, F.
发明人： BRACEY, Michael, H. , HANSON, Michael, A. , STEVENS, Raymond, C. , CRAVATT, Benjamin, F.
IPC分类号： C12N
CPC分类号： C12N9/78 , C07K2299/00
摘要： The present invention is directed to FAAH crystals in complex with the inhibitor methoxyarachidonyl fluorophosphonate (MAFP) and to the use of these crystals to determine the three-dimensional structure of FAAH. This invention id further directed to the use of this structure for the modeling or determination of the structures of related proteins. This invention is further directed to the use of this structure in the pursuit of drug design to identify, characterize, or optimize agents which bind to the active site, substrate channels, product channels, or regulatory sites of FAAH, and to the evaluation of these agents to identify agents which may stimulate, inhibit, relocalize, stabilize, or destabilize FAAH and/or its activity. This invention is further directed to the use of this structure in the development of engineered FAAH variants which display altered solubility, catalytic profiles, or substrate specificity. This invention is further directed to the use of this structure in the development of engineered heterologous proteins with altered membrane tropism.
摘要翻译：本发明涉及与抑制剂甲氧基花生酸酯氟磷酸酯（MAFP）复合的FAAH晶体以及涉及这些晶体用于确定FAAH的三维结构的用途。本发明还进一步涉及该结构用于建模或确定相关蛋白质的结构。本发明进一步涉及该结构在追求药物设计中的用途，以鉴定，表征或优化与FAAH的活性位点，底物通道，产物通道或调节位点结合的试剂，并评估这些识别可刺激，抑制，再定位，稳定FAAH和/或其活性的试剂的试剂。本发明进一步涉及该结构在显示改变的溶解度，催化特征或底物特异性的工程化FAAH变体的开发中的用途。本发明进一步涉及该结构在开发具有改变的膜向性的工程异源蛋白质中的用途。

6. 发明申请

WO2003011220A2 ANIMAL MODEL FOR FATTY ACID AMIDE-RELATED NEUROBEHAVIORS 审中-公开
标题翻译：动物模型脂肪酸酰胺相关的神经病变
公开(公告)号：WO2003011220A2
公开(公告)日：2003-02-13
申请号：PCT/US2002/024140
申请日：2002-07-30
申请人： THE SCRIPPS RESEARCH INSTITUTE , CRAVATT, Benjamin, F.
发明人： CRAVATT, Benjamin, F.
IPC分类号： A61K
CPC分类号： C12N15/8509 , A01K67/0276 , A01K2217/072 , A01K2217/075 , A01K2227/105 , A01K2267/03 , A01K2267/0356 , A61K49/0008 , C12N9/16 , C12N9/80 , C12N2830/008
摘要： The invention relates to animal model for studying behavior related to fatty acid amide and hydrolysis of fatty acid amide. The invention provides transgenic animals in which the protein fatty acid amide hydrolase is not expressed, and methods of using such animals.
摘要翻译：本发明涉及用于研究与脂肪酸酰胺相关的行为和脂肪酸酰胺水解的动物模型。本发明提供了其中不表达蛋白质脂肪酸酰胺水解酶的转基因动物以及使用这种动物的方法。

7. 发明申请

WO0177684A2 PROTEOMIC ANALYSIS 审中-公开
标题翻译：蛋白质组学分析
公开(公告)号：WO0177684A2
公开(公告)日：2001-10-18
申请号：PCT/US0034187
申请日：2000-12-15
申请人： SCRIPPS RESEARCH INST , CRAVATT BENJAMIN F , SORENSEN ERIK , PATRICELLI MATTHEW , LOVATO MARTHA , ADAM GREGORY
发明人： CRAVATT BENJAMIN F , SORENSEN ERIK , PATRICELLI MATTHEW , LOVATO MARTHA , ADAM GREGORY
IPC分类号： G01N33/50 , C07C309/66 , C07C309/73 , C07D495/04 , C07K14/00 , C12Q1/25 , C12Q1/26 , C12Q1/32 , C12Q1/34 , C12Q1/37 , C40B20/04 , C40B30/04 , C40B40/02 , C40B40/04 , C40B50/06 , G01N33/15 , G01N33/535 , G01N33/557 , G01N33/68 , G06F19/18 , G06F19/00
CPC分类号： C40B30/04 , C12Q1/26 , C12Q1/32 , C12Q1/37 , C40B40/04 , G01N33/535 , G01N33/557 , G01N33/6842 , G01N33/6845 , G01N2500/20 , G06F19/18 , Y10T436/16 , Y10T436/18
摘要： The present invention provides methods for analyzing proteomes, as cells or lysates. The analysis is based on the use of probes that have specificity to the active form of proteins, particularly enzymes and receptors. The probes can be identified in different ways. In accordance with the present invention, a method is provided for generating and screening compound libraries that are used for the identification of lead molecules, and for the parallel identification of their biological targets. By appending specific functionalities and/or groups to one or more binding moieties, the reactive functionalities gain binding affinity and specificity for particular proteins and classes of proteins. Such libraries of candidate compounds, referred to herein as activity-based probes, or ABPs, are used to screen for one or more desired biological activities or target proteins.
摘要翻译：本发明提供了用于分析蛋白质组作为细胞或裂解物的方法。分析基于使用对蛋白质的活性形式具有特异性的探针，特别是酶和受体。探针可以用不同的方式标识。根据本发明，提供了一种用于产生和筛选用于鉴定前导分子以及平行鉴定其生物学靶标的化合物文库的方法。通过将特定官能团和/或基团附加到一个或多个结合部分，反应性官能团获得对特定蛋白质和蛋白质类别的结合亲和力和特异性。这种称为基于活性的探针或ABP的候选化合物文库用于筛选一种或多种所需的生物活性或靶蛋白。

8. 发明申请

WO2010056309A3 METHODS AND COMPOSITIONS RELATED TO TARGETING MONOACYLGLYCEROL LIPASE 审中-公开
标题翻译：与靶向单乙酰甘油脂酶有关的方法和组合物
公开(公告)号：WO2010056309A3
公开(公告)日：2010-07-01
申请号：PCT/US2009006045
申请日：2009-11-10
申请人： SCRIPPS RESEARCH INST , CRAVATT BENJAMIN F , LONG JONATHAN Z , LI WEIWEI , NOMURA DANIEL K
发明人： CRAVATT BENJAMIN F , LONG JONATHAN Z , LI WEIWEI , NOMURA DANIEL K
IPC分类号： A61K31/70
CPC分类号： A61K31/00 , A61K31/496 , C12N15/1137 , C12N2310/14 , C12N2310/531
摘要： This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.
摘要翻译：本发明提供了选择性抑制单酰甘油脂肪酶（MAGL）的化合物。本发明还提供了使用MAGL选择性抑制剂在体内刺激2-花生四烯酰甘油（2-AG）介导的内源性大麻素信号传导以及治疗与内源性大麻素信号传导相关或相关的病症的方法。本发明另外提供了通过用MAGL特异性抑制剂靶向MAGL来治疗癌症或抑制肿瘤生长的方法。本发明进一步提供了筛选具有改善的生物化学和药学性质的MAGL抑制剂的方法。

9. 发明申请

WO2010056309A2 METHODS AND COMPOSITIONS RELATED TO TARGETING MONOACYLGLYCEROL LIPASE 审中-公开
标题翻译：与单糖胆固醇相关的方法和组合物
公开(公告)号：WO2010056309A2
公开(公告)日：2010-05-20
申请号：PCT/US2009/006045
申请日：2009-11-10
申请人： THE SCRIPPS RESEARCH INSTITUTE , CRAVATT, Benjamin, F. , LONG, Jonathan, Z. , LI, Weiwei , NOMURA, Daniel, K.
发明人： CRAVATT, Benjamin, F. , LONG, Jonathan, Z. , LI, Weiwei , NOMURA, Daniel, K.
IPC分类号： A61K31/496
CPC分类号： A61K31/00 , A61K31/496 , C12N15/1137 , C12N2310/14 , C12N2310/531
摘要： This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.
摘要翻译：本发明提供选择性抑制单酰基甘油脂肪酶（MAGL）的化合物。本发明还提供使用MAGL选择性抑制剂在体内刺激2-花生四烯酰甘油（2-AG）介导的内源性大麻素信号传导的方法，并且治疗与内源性大麻素信号传导相关或连接的病症。本发明还提供了通过用MAGL特异性抑制剂靶向MAGL来治疗癌症或抑制肿瘤生长的方法。本发明进一步提供筛选具有改进的生物化学和药物性质的MAGL抑制剂的方法。

10. 发明申请

WO2008063752A2 AN ENZYME REGULATING ETHER LIPID SIGNALING PATHWAYS 审中-公开
标题翻译：一种调节醚脂质信号通路的酶
公开(公告)号：WO2008063752A2
公开(公告)日：2008-05-29
申请号：PCT/US2007/080222
申请日：2007-10-02
申请人： THE SCRIPPS RESEARCH INSTITUTE , CRAVATT, Benjamin, F. , CHIANG, Kyle, P. , NIESSEN, Sherry , SAGHATELIAN, Alan
发明人： CRAVATT, Benjamin, F. , CHIANG, Kyle, P. , NIESSEN, Sherry , SAGHATELIAN, Alan
IPC分类号： A61K31/325
CPC分类号： A61K31/325 , C12Q1/34 , G01N33/92 , G01N2500/02
摘要： A multidimensional profiling strategy that combines activity-based proteomics and metabolomics was used to determine that an active protein, which is a previously uncharacterized enzyme highly elevated in aggressive cancer cells, serves as a central node in an ether lipid signaling network that bridges platelet-activating factor and the lysophospholipids. Biochemical studies confirmed that the active protein regulates this pathway by hydrolyzing the metabolic intermediate 2-acetyl monoalkylglycerol. Inactivation of the active protein disrupted ether lipid metabolism in cancer cells and impaired cell migration and tumor growth in vivo .
摘要翻译：使用基于活性的蛋白质组学和代谢组学的多维分布策略来确定活性蛋白质，其是先前在侵略性癌细胞中高度升高的未表征的酶，其在乙醚中充当中央节点脂质信号网络，桥接血小板活化因子和溶血磷脂。生物化学研究证实，活性蛋白质通过水解代谢中间体2-乙酰基单烷基甘油来调节该途径。体内活性蛋白质失活破坏了癌细胞中的醚脂质代谢并且损害了细胞迁移和肿瘤生长。

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