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1. 发明申请

WO2010099363A1 METHODS FOR THE IDENTIFICATION OF AGENTS THAT INHIBIT MESENCHYMAL-LIKE TUMOR CELLS OR THEIR FORMATION 审中-公开
标题翻译：鉴别抑制类似肿瘤细胞或其形成的药物的方法
公开(公告)号：WO2010099363A1
公开(公告)日：2010-09-02
申请号：PCT/US2010/025473
申请日：2010-02-26
申请人： OSI PHARMACEUTICALS, INC. , FRANKLIN, Maryland , KAN, Julie , KRUEGER, Joseph, S. , SHAABAN, Salam, A. , WILD, Robert, C.
发明人： FRANKLIN, Maryland , KAN, Julie , KRUEGER, Joseph, S. , SHAABAN, Salam, A. , WILD, Robert, C.
IPC分类号： G01N33/50
CPC分类号： G01N33/5017 , G01N33/5011 , G01N33/5044
摘要： The present invention provides tumor cell preparations for use as models of the EMT process for use in the identification of anti-cancer agents, wherein said tumor cell preparations comprise cells of the epithelial tumor cell line CFPAC-I, which are stimulated by receptor ligands to induce EMT, or which have been engineered to inducibly express a protein that stimulates EMT. The present invention also provides methods of identifying potential anti-cancer agents by using such tumor cell preparations to identify agents that inhibit EMT, stimulate MET, or inhibit the growth of mesenchymal-like cells. Such agents should be particularly useful when used in conjunction with other anti-cancer drugs such as EGFR and IGF-IR kinase inhibitors, which appear to be less effective at inhibiting tumor cells that have undergone an EMT.
摘要翻译：本发明提供用作鉴定抗癌剂的EMT方法的模型的肿瘤细胞制剂，其中所述肿瘤细胞制剂包含上皮肿瘤细胞系CFPAC-1的细胞，其被受体配体刺激诱导EMT，或已被设计成可诱导表达刺激EMT的蛋白质。本发明还提供了通过使用这样的肿瘤细胞制剂鉴定潜在的抗癌剂的方法来鉴定抑制EMT，刺激MET或抑制间充质细胞生长的药剂。当与其它抗癌药物如EGFR和IGF-1R激酶抑制剂联合使用时，这些药剂应该特别有用，这对于抑制已经经历EMT的肿瘤细胞来说效果较差。

2. 发明申请

WO2009111067A9 METHODS FOR THE IDENTIFICATION OF AGENTS THAT INHIBIT MESENCHYMAL -LIKE TUMOR CELLS OR THEIR FORMATION 审中-公开
标题翻译：鉴定抑制MESENCHYMAL-LUM肿瘤细胞或其形成的药物的方法
公开(公告)号：WO2009111067A9
公开(公告)日：2009-12-23
申请号：PCT/US2009001456
申请日：2009-03-06
申请人： OSI PHARM INC , HALEY JOHN D , THOMSON STUART , KAN JULIE , SHAABAN SALAM A
发明人： HALEY JOHN D , THOMSON STUART , KAN JULIE , SHAABAN SALAM A
IPC分类号： G01N33/574
CPC分类号： G01N33/5011 , G01N2333/475 , G01N2333/485 , G01N2333/495 , G01N2333/525
摘要： The present invention provides tumor cell preparations for use as models of the EMT process for use in the identification of anti-cancer agents, wherein said tumor cell preparations comprise cells of the epithelial tumor cell line H358, which are stimulated by receptor ligands to induce EMT, or which have been engineered to inducibly express a protein that stimulates EMT. The present invention also provides methods of identifying potential anti-cancer agents by using such tumor cell preparations to identify agents that inhibit EMT, stimulate MET, or inhibit the growth of mesenchymal-like cells. Such agents should be particularly useful when used in conjunction with other anti-cancer drugs such as EGFR and IGF-IR kinase inhibitors, which appear to be less effective at inhibiting tumor cells that have undergone an EMT.
摘要翻译：本发明提供用作鉴定抗癌剂的EMT方法的模型的肿瘤细胞制剂，其中所述肿瘤细胞制剂包含受体配体刺激以诱导EMT的上皮肿瘤细胞系H358的细胞，或已被设计成可诱导地表达刺激EMT的蛋白质。本发明还提供了通过使用这样的肿瘤细胞制剂鉴定潜在的抗癌剂的方法来鉴定抑制EMT，刺激MET或抑制间充质细胞生长的药剂。当与其它抗癌药物如EGFR和IGF-1R激酶抑制剂联合使用时，这些药剂应该特别有用，这对于抑制已经经历EMT的肿瘤细胞来说效果较差。

3. 发明申请

WO2008128050A2 METHODS FOR IDENTIFICATION OF MODULATORS OF CARM1 METHYL TRANSFERASE ACTIVITY 审中-公开
标题翻译：鉴定CARM1甲基转移酶活性调节剂的方法
公开(公告)号：WO2008128050A2
公开(公告)日：2008-10-23
申请号：PCT/US2008/060043
申请日：2008-04-11
申请人： OSI PHARMACEUTICALS, INC. , SGX PHARMACEUTICALS, INC. , FOREMAN, Kenneth, William , SHAABAN, Salam , PARK, Frances, E. , SAUDER, Michael
发明人： FOREMAN, Kenneth, William , SHAABAN, Salam , PARK, Frances, E. , SAUDER, Michael
IPC分类号： C12N9/10 , G06F19/00 , C12Q1/48
CPC分类号： C12N9/1029 , C07K2299/00
摘要： This invention relates to CARM1, CARM1 binding pockets, or CARM1-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to CARM1 protein, complexes of CARM1 protein, homologs thereof, or CARM1-like protein or protein complexes. The invention also relates to crystallizable compositions and crystals comprising a CARM1 protein or homologs thereof. The invention also relates to methods of identifying binders of CARM1 proteins. The invention also relates to methods for determining the intracellular activity of CARM1 methyltransferase and methods for identifying an agent that inhibits the intracellular activity of CARM1 methyltransferase.
摘要翻译：本发明涉及CARM1，CARM1结合袋或CARM1样结合袋。本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。本发明涉及使用结构坐标来筛选和设计结合CARM1蛋白，CARM1蛋白的复合物，其同系物或CARM1样蛋白或蛋白质复合物的化合物的方法。本发明还涉及可结晶组合物和包含CARM1蛋白或其同系物的晶体。本发明还涉及鉴定CARM1蛋白的结合物的方法。本发明还涉及确定CARM1甲基转移酶的细胞内活性的方法以及鉴定抑制CARM1甲基转移酶细胞内活性的试剂的方法。

4. 发明申请

WO2006018662A3 ARYL UREA DERIVATIVES FOR TREATING OBESITY 审中-公开
公开(公告)号：WO2006018662A3
公开(公告)日：2006-02-23
申请号：PCT/GB2005/050131
申请日：2005-08-16
申请人： PROSIDION LIMITED , BLOXHAM, Jason , FYFE, Matthew, Colin, Thor , HORSWILL, James , JEEVARATNAM, Revathy, Perpetua , KEILY, John , PROCTER, Martin, James , SCHOFIELD, Karen, Lesley , SHAABAN, Salam , SWAIN, Simon, Andrew , WONG-KAI-IN, Philippe
发明人： BLOXHAM, Jason , FYFE, Matthew, Colin, Thor , HORSWILL, James , JEEVARATNAM, Revathy, Perpetua , KEILY, John , PROCTER, Martin, James , SCHOFIELD, Karen, Lesley , SHAABAN, Salam , SWAIN, Simon, Andrew , WONG-KAI-IN, Philippe
IPC分类号： A61K31/426 , A61K31/381 , A61K31/428 , A61K31/341 , A61K31/404 , A61K31/44 , A61K31/455 , A61P25/18 , A61P25/08 , A61P3/04 , A61P25/16 , A61P25/28 , A61P25/32 , A61P25/34 , A61P25/36
摘要： A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.

5. 发明申请

WO2009111067A3 METHODS FOR THE IDENTIFICATION OF AGENTS THAT INHIBIT MESENCHYMAL -LIKE TUMOR CELLS OR THEIR FORMATION 审中-公开
公开(公告)号：WO2009111067A3
公开(公告)日：2009-09-11
申请号：PCT/US2009/001456
申请日：2009-03-06
申请人： OSI PHARMACEUTICALS, INC. , HALEY, John, D. , THOMSON, Stuart , KAN, Julie , SHAABAN, Salam, A.
发明人： HALEY, John, D. , THOMSON, Stuart , KAN, Julie , SHAABAN, Salam, A.
IPC分类号： G01N33/574
摘要： The present invention provides tumor cell preparations for use as models of the EMT process for use in the identification of anti-cancer agents, wherein said tumor cell preparations comprise cells of the epithelial tumor cell line H358, which are stimulated by receptor ligands to induce EMT, or which have been engineered to inducibly express a protein that stimulates EMT. The present invention also provides methods of identifying potential anti-cancer agents by using such tumor cell preparations to identify agents that inhibit EMT, stimulate MET, or inhibit the growth of mesenchymal-like cells. Such agents should be particularly useful when used in conjunction with other anti-cancer drugs such as EGFR and IGF-IR kinase inhibitors, which appear to be less effective at inhibiting tumor cells that have undergone an EMT.

6. 发明申请

WO2006018662A2 ARYL UREA DERIVATIVES 审中-公开
公开(公告)号：WO2006018662A2
公开(公告)日：2006-02-23
申请号：PCT/GB2005050131
申请日：2005-08-16
申请人： PROSIDION LTD , BLOXHAM JASON , FYFE MATTHEW COLIN THOR , HORSWILL JAMES , JEEVARATNAM REVATHY PERPETUA , KEILY JOHN , PROCTER MARTIN JAMES , SCHOFIELD KAREN LESLEY , SHAABAN SALAM , SWAIN SIMON ANDREW , WONG-KAI-IN PHILIPPE
发明人： BLOXHAM JASON , FYFE MATTHEW COLIN THOR , HORSWILL JAMES , JEEVARATNAM REVATHY PERPETUA , KEILY JOHN , PROCTER MARTIN JAMES , SCHOFIELD KAREN LESLEY , SHAABAN SALAM , SWAIN SIMON ANDREW , WONG-KAI-IN PHILIPPE
IPC分类号： A61K31/426 , A61K31/341 , A61K31/381 , A61K31/404 , A61K31/428 , A61K31/44 , A61K31/455 , A61P1/00 , A61P3/04 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/34 , A61P25/36 , A61P43/00
CPC分类号： A61K31/381 , A61K31/341 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/44 , A61K31/455
摘要： A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.
摘要翻译：通过向需要这种治疗的受试者施用有效量的芳基脲CB-1受体调节化合物来治疗与CB-1受体相关的病症，特别是肥胖症的方法。

7. 发明申请

WO2009111067A2 METHODS FOR THE IDENTIFICATION OF AGENTS THAT INHIBIT MESENCHYMAL -LIKE TUMOR CELLS OR THEIR FORMATION 审中-公开
公开(公告)号：WO2009111067A2
公开(公告)日：2009-09-11
申请号：PCT/US2009001456
申请日：2009-03-06
申请人： OSI PHARM INC , HALEY JOHN D , THOMSON STUART , KAN JULIE , SHAABAN SALAM A
发明人： HALEY JOHN D , THOMSON STUART , KAN JULIE , SHAABAN SALAM A
IPC分类号： G01N33/574
CPC分类号： G01N33/5011 , G01N2333/475 , G01N2333/485 , G01N2333/495 , G01N2333/525
摘要： The present invention provides tumor cell preparations for use as models of the EMT process for use in the identification of anti-cancer agents, wherein said tumor cell preparations comprise cells of the epithelial tumor cell line H358, which are stimulated by receptor ligands to induce EMT, or which have been engineered to inducibly express a protein that stimulates EMT. The present invention also provides methods of identifying potential anti-cancer agents by using such tumor cell preparations to identify agents that inhibit EMT, stimulate MET, or inhibit the growth of mesenchymal-like cells. Such agents should be particularly useful when used in conjunction with other anti-cancer drugs such as EGFR and IGF-IR kinase inhibitors, which appear to be less effective at inhibiting tumor cells that have undergone an EMT.

8. 发明申请

WO2008128050A3 METHODS FOR IDENTIFICATION OF MODULATORS OF CARM1 METHYL TRANSFERASE ACTIVITY 审中-公开
标题翻译：鉴定CARM1甲基转移酶活性调节剂的方法
公开(公告)号：WO2008128050A3
公开(公告)日：2009-02-26
申请号：PCT/US2008060043
申请日：2008-04-11
申请人： OSI PHARM INC , SGX PHARMACEUTICALS INC , FOREMAN KENNETH WILLIAM , SHAABAN SALAM , PARK FRANCES E , SAUDER MICHAEL
发明人： FOREMAN KENNETH WILLIAM , SHAABAN SALAM , PARK FRANCES E , SAUDER MICHAEL
IPC分类号： C12N9/10 , C12Q1/48 , G06F19/00
CPC分类号： C12N9/1029 , C07K2299/00
摘要： This invention relates to CARM1, CARM1 binding pockets, or CARM1-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to CARM1 protein, complexes of CARM1 protein, homologs thereof, or CARM1-like protein or protein complexes. The invention also relates to crystallizable compositions and crystals comprising a CARM1 protein or homologs thereof. The invention also relates to methods of identifying binders of CARM1 proteins. The invention also relates to methods for determining the intracellular activity of CARM1 methyltransferase and methods for identifying an agent that inhibits the intracellular activity of CARM1 methyltransferase.
摘要翻译：本发明涉及CARM1，CARM1结合袋或CARM1样结合袋。本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。本发明涉及使用结构坐标来筛选和设计结合CARM1蛋白，CARM1蛋白的复合物，其同系物或CARM1样蛋白或蛋白质复合物的化合物的方法。本发明还涉及可结晶组合物和包含CARM1蛋白或其同系物的晶体。本发明还涉及鉴定CARM1蛋白的结合物的方法。本发明还涉及确定CARM1甲基转移酶的细胞内活性的方法以及鉴定抑制CARM1甲基转移酶细胞内活性的试剂的方法。

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