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公开(公告)号：WO2008156701A3
公开(公告)日：2008-12-24
申请号：PCT/US2008/007447
申请日：2008-06-13
申请人： THE BRIGHAM AND WOMEN'S HOSPITAL, INC. , PRESIDENT AND FELLOWS OF HARWARD COLLEGE , YALE UNIVERSITY , LEISSRING, Malcolm, A. , SELKOE, Dennis , CUNY, Gregory, D. , CHOI, Sungwoon , STEIN, Ross, L. , TURK, Benjamin , CANTLEY, Lewis, C.
发明人： LEISSRING, Malcolm, A. , SELKOE, Dennis , CUNY, Gregory, D. , CHOI, Sungwoon , STEIN, Ross, L. , TURK, Benjamin , CANTLEY, Lewis, C.
IPC分类号： C07C237/04
摘要： The present invention provides a novel therapeutic approach for the prevention and treatment of infections and for the treatment of diabetes wherein the degradation of insulin is reduced through inhibition of insulin-degrading enzyme (IDE) by hydroxamate inhibitors.
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2.发明申请Methods for identifiying inhibitors of the MTOR pathway as diabetes therapeutics 审中-公开鉴定MTOR途径抑制剂作为糖尿病治疗剂的方法
公开(公告)号：WO2006020755A3
公开(公告)日：2006-07-06
申请号：PCT/US2005028523
申请日：2005-08-10
CPC分类号： G01N33/6893 , C12Q1/485 , G01N2800/042
摘要： The invention relates to inhibition of mTOR, p70S6K1 or Rheb kinase activity for treating disorders including diabetes. The invention also relates to screening for agents that inhibit the activities of mTOR, p70S6K1 or Rheb proteins, which are useful in the treatment of diabetes, as well as preparing compounds for treatment of diabetes.
摘要翻译： 本发明涉及抑制mTOR，p70S6K1或Rheb激酶活性来治疗包括糖尿病在内的疾病。 本发明还涉及抑制可用于治疗糖尿病的mTOR，p70S6K1或Rheb蛋白的活性的药剂的筛选，以及制备用于治疗糖尿病的化合物。
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公开(公告)号：WO2022192643A1
公开(公告)日：2022-09-15
申请号：PCT/US2022/019908
申请日：2022-03-11
申请人： CORNELL UNIVERSITY , THE BRIGHAM AND WOMEN’S HOSPITAL, INC. , CANTLEY, Lewis C. , KUCHROO, Vijay Kumar , SCHRAMM, Markus Alexander , DIXON, Karen Olivia
摘要： Described herein are compositions and methods for inhibiting, degrading, knocking down or knocking out pip4k2c nucleic acids or Pip4k2c protein. Such compositions and methods are useful for treating and inhibiting the onset of cancer.
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4.发明申请
公开(公告)号：WO2005023202A2
公开(公告)日：2005-03-17
申请号：PCT/US2004/029437
申请日：2004-09-09
申请人： BETH ISRAEL DEACONESS MEDICAL CENTER, INC. , DANA-FARBER CANCER INSTITUTE, INC. , CANTLEY, Lewis, C. , SHAW, Reuben, J. , BARDEESY, Nabeel , DEPINHO, Ronald, A.
IPC分类号： A61K
CPC分类号： C12Q1/485 , G01N33/573 , G01N33/574 , G01N2333/9015 , G01N2333/91215 , G01N2500/02 , G01N2800/042
摘要： The invention relates to modulation of LKB1 or AMP kinase protein activity for treating disorders including diabetes and cancer. The invention also relates to screening for agents that modulate the activity of LKB1 or AMP kinase protein, which are useful in the treatment of diabetes and cancer, as well as preparing compounds for treatment of diabetes and cancer.
摘要翻译： 本发明涉及用于治疗包括糖尿病和癌症在内的疾病的LKB1或AMP激酶蛋白活性的调节。 本发明还涉及筛选调节可用于治疗糖尿病和癌症的LKB1或AMP激酶蛋白的活性以及制备用于治疗糖尿病和癌症的化合物的活性的试剂。
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公开(公告)号：WO0238796A3
公开(公告)日：2004-02-26
申请号：PCT/US0146777
申请日：2001-11-08
发明人： TURK BENJAMIN E , CANTLEY LEWIS C
CPC分类号： G01N33/6848 , C07K5/0812 , C07K7/06 , C07K14/8146 , C12Q1/37 , G01N33/6818 , G01N33/6842
摘要： The invention provides methods for rapidly determining protease cleavage site motifs using a mixture-based oriented peptide library approach. The cleavage site motif for a protease involve residues both amino- and carboxy- terminal to the scissile bond (the unprimed and primed sides, respectively). The methods involve the initial determination of the primed side motif and the successive determination of the unprimed side motif. Iterative application of the methods is also provided. Substrates and inhibitors of proteases that include or compete for the cleavage site motifs determined using the methods also are provided, as are methods and compositions for using these substrates and inhibitors.
摘要翻译： 本发明提供了使用基于混合物的定向肽文库方法快速确定蛋白酶切割位点基序的方法。 蛋白酶的切割位点基序涉及易切断键的氨基和羧基末端残基（分别为非底漆侧和底漆侧）。 这些方法涉及初始化的侧面图案的初始测定和未涂底漆侧面图案的连续测定。 还提供了方法的迭代应用。 还提供了包括或竞争使用该方法确定的切割位点基序的蛋白酶底物和抑制剂，以及使用这些底物和抑制剂的方法和组合物。
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6.发明申请
公开(公告)号：WO2022140554A1
公开(公告)日：2022-06-30
申请号：PCT/US2021/064880
申请日：2021-12-22
申请人： DANA-FARBER CANCER INSTITUTE, INC. , CORNELL UNIVERSITY , GRAY, Nathanael S. , ZHANG, Tinghu , CANTLEY, Lewis C. , SIVAKUMAREN, Carmen , MANZ, Theresa , WANG, Eric , JI, Wenzhi , FISCHER, Eric S. , DONOVAN, Katherine
发明人： GRAY, Nathanael S. , ZHANG, Tinghu , CANTLEY, Lewis C. , SIVAKUMAREN, Carmen , MANZ, Theresa , WANG, Eric , JI, Wenzhi , FISCHER, Eric S. , DONOVAN, Katherine
IPC分类号： A61K31/495 , A61K31/4965 , A61K31/497 , C07D239/42 , C07D403/02 , C07D403/04
摘要： The present invention relates to bifunctional compounds, compositions, and methods for treating diseases or conditions by modulating (e.g., reducing) the level or activity of at least one of PIP4K2A, PIP4K2B, and PIP4K2C.
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公开(公告)号：WO2019232403A1
公开(公告)日：2019-12-05
申请号：PCT/US2019/034949
申请日：2019-05-31
申请人： CORNELL UNIVERSITY , CANTLEY, Lewis C. , HOPKINS, Benjamin , MUKHERJEE, Siddhartha , GONCALVES, Marcus
IPC分类号： A23L33/20 , A61K31/155 , A61K38/00 , A61P3/10 , A61P35/00 , C07C279/00
摘要： Described herein are compositions and methods for treating a disease or disorder associated with PI3K signaling. For example, such compositions can include use of modulators of glucose metabolism, use of at least one kinase in the insulin-receptor/PI3K/AKT/mTOR pathway, and/or use of diet that influences the subject's metabolic state.
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8.发明申请SMALL MOLECULE INHIBITOR OF 3-PHOSPHOGLYCERATE DEHYDROGENASE AND USES THEREOF 审中-公开小分子3-磷酸甘油脱氢酶的分子抑制剂及其应用
公开(公告)号：WO2017117532A1
公开(公告)日：2017-07-06
申请号：PCT/US2016/069496
申请日：2016-12-30
IPC分类号： C07D409/12 , A61K31/381 , A61P35/00
CPC分类号： C07D409/12
摘要： Embodiments of the present invention are directed to small molecule inhibitors of PHGDH. Other embodiments of the present invention relate to methods of treating cancers using the small molecule inhibitors of PHGDH disclosed herein. Still other embodiments of the present invention relate to methods for using the small molecule inhibitors of PHGDH to study serine metabolism.
摘要翻译： 本发明的实施方案涉及PHGDH的小分子抑制剂。 本发明的其它实施方案涉及使用本文公开的PHGDH的小分子抑制剂治疗癌症的方法。 本发明的其他实施方案涉及使用PHGDH的小分子抑制剂研究丝氨酸代谢的方法。
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9.发明申请METHODS AND COMPOSITIONS FOR THE DIAGNOSIS AND TREATMENT OF CELLULAR PROLIFERATIVE DISORDERS 审中-公开诊断和治疗细胞增殖性疾病的方法和组合
公开(公告)号：WO2011150256A3
公开(公告)日：2014-03-20
申请号：PCT/US2011038208
申请日：2011-05-26
CPC分类号： C12Q1/6886 , C12Q2600/156
摘要： The present invention features methods and compositions for the diagnosis, prognosis, treatment, and/or amelioration of cellular proliferative disorders utilizing enzymes of the serine biosynthetic pathway (e.g., phosphoglycerate dehydrogenase (PHGDH), phosphoserine aminotransferase (PSAT), or phosphoserine phosphatase (PSPH)).
摘要翻译： 本发明的特征在于利用丝氨酸生物合成途径的酶（例如磷酸甘油酸脱氢酶（PHGDH），磷酸丝氨酸氨基转移酶（PSAT）或磷酸丝氨酸磷酸酶（PSPH））来诊断，预后，治疗和/或改善细胞增殖性疾病的方法和组合物 ））。
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公开(公告)号：WO2008127710A3
公开(公告)日：2008-12-04
申请号：PCT/US2008004804
申请日：2008-04-11
申请人： DANA FARBER CANCER INST INC , BETH ISRAEL HOSPITAL , MASSACHUSETTS GEN HOSPITAL , JANNE PASI A , ENGELMAN JEFFREY , CANTLEY LEWIS C
发明人： JANNE PASI A , ENGELMAN JEFFREY , CANTLEY LEWIS C
IPC分类号： A61K45/06 , A61K31/404 , A61K31/517 , A61K39/395 , A61P35/00
CPC分类号： C12Q1/6886 , A61K31/404 , A61K31/517 , A61K39/395 , A61K45/06 , C12Q2600/106 , C12Q2600/156
摘要： Provided herein are methods for treating cancer that is resistant to treatment with an anti- ErbB therapeutic agent and which is associated with an activating MET gene mutation or a MET gene amplification. The methods involve administering to a subject a combination of an anti- ErbB therapeutic and an anti-MET therapeutic. Also provided are methods for reducing ErbB mediated signaling or PI3 kinase mediated signaling in a cancer cell.
摘要翻译： 本文提供了用抗ErbB治疗剂治疗耐药性并与活化MET基因突变或MET基因扩增相关的癌症治疗方法。 所述方法包括向受试者施用抗ErbB治疗剂和抗MET治疗剂的组合。 还提供了用于在癌细胞中减少ErbB介导的信号传导或PI3激酶介导的信号传导的方法。
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