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公开(公告)号：US20100216853A1
公开(公告)日：2010-08-26
申请号：US12665751
申请日：2008-06-19
申请人： Ronen Marmorstein , Xin Liu , Philip A. Cole , Ling Wang , Erin M. Bowers , David J. Meyers , Chandrani Mukherjee
发明人： Ronen Marmorstein , Xin Liu , Philip A. Cole , Ling Wang , Erin M. Bowers , David J. Meyers , Chandrani Mukherjee
IPC分类号： A61K31/426 , C40B30/04 , C07D413/06 , A61K31/4155 , C12N9/96 , C07D277/00 , C07D263/56 , A61K31/423 , A61P3/04 , A61P3/10 , A61P35/04
CPC分类号： A61K31/5585 , A61K31/4015 , A61K31/402 , A61K31/4025 , C07D405/06 , C12N9/1029 , C12Q1/48 , C12Y203/01048 , C40B30/02 , G01N2333/91057 , G01N2500/04 , Y02A90/26
摘要： The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.
摘要翻译： 本发明涉及鉴定调节p300 / CBP活性的化合物的方法。 通过设计或筛选与p300 / CBP的HAT结构域的新鉴定的赖氨酸-CoA抑制剂结合位点，L1环，电负性口袋或电负性沟槽的至少一个氨基酸残基相结合的化合物来鉴定本发明化合物 并测试该化合物调节p300 / CBP活性的能力。 还提供了用于预防或治疗与p300 / CBP相关的疾病或病症的组合物和方法以及半合成HAT结构域的制备方法。
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公开(公告)号：US08476458B2
公开(公告)日：2013-07-02
申请号：US12665751
申请日：2008-06-19
申请人： Ronen Marmorstein , Xin Liu , Philip A. Cole , Ling Wang , Erin M. Bowers , David J. Meyers , Chandrani Mukherjee
发明人： Ronen Marmorstein , Xin Liu , Philip A. Cole , Ling Wang , Erin M. Bowers , David J. Meyers , Chandrani Mukherjee
IPC分类号： C07D231/00 , C07D231/06 , C07D307/00 , C07D317/00 , C07D323/02
CPC分类号： A61K31/5585 , A61K31/4015 , A61K31/402 , A61K31/4025 , C07D405/06 , C12N9/1029 , C12Q1/48 , C12Y203/01048 , C40B30/02 , G01N2333/91057 , G01N2500/04 , Y02A90/26
摘要： The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.
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3.发明授权公开(公告)号：US08180580B2
公开(公告)日：2012-05-15
申请号：US12023287
申请日：2008-01-31
CPC分类号： C12Q1/25 , G01N2333/986 , G01N2500/04
摘要： The present invention relates to a method for identifying compounds that modulate the activity of sirtuin deacetylase protein family members. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified nicotinamide inhibition and base exchange site of Sir2 and testing the compound for its ability to modulate the activity of the Sir2 protein. Compositions and methods for preventing or treating diseases or disorders associated with Sir2 are also provided.
摘要翻译： 本发明涉及一种鉴定调节沉默调节蛋白脱乙酰酶蛋白家族成员活性的化合物的方法。 通过设计或筛选与新鉴定的Sir2的烟酰胺抑制和碱基交换位点的至少一个氨基酸残基并测试该化合物调节Sir2蛋白活性的能力的化合物来鉴定本发明的化合物。 还提供了用于预防或治疗与Sir2相关的疾病或病症的组合物和方法。
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公开(公告)号：US20090326007A1
公开(公告)日：2009-12-31
申请号：US12511679
申请日：2009-07-29
IPC分类号： A61K31/47
CPC分类号： A61K31/47
摘要： The present invention embraces compounds that modulate the activity of sirtuin deacetylase protein family members and use thereof for modulating Sir2 activity as well as for preventing or treating diseases or disorders associated with Sir2.
摘要翻译： 本发明包括调节沉默调节蛋白脱乙酰酶蛋白家族成员的活性的化合物及其用于调节Sir2活性以及用于预防或治疗与Sir2相关的疾病或病症的化合物。
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公开(公告)号：US20090275547A1
公开(公告)日：2009-11-05
申请号：US12112748
申请日：2008-04-30
申请人： Eric Meggers , Peng Xie , Douglas S. Williams , Ronen Marmorstein
发明人： Eric Meggers , Peng Xie , Douglas S. Williams , Ronen Marmorstein
IPC分类号： A61K31/295 , C07F15/00
CPC分类号： C07D498/22 , C07D487/14
摘要： Provided are novel organometallic compounds that inhibit PI3K lipid kinase and phospho-AKT in human melanoma cells, and also inhibit the migration of melanoma cells. The present invention is also directed to methods for inhibiting cancer cell proliferation, migration or both comprising contacting a cancer cell with a disclosed organometallic kinase inhibitor. Also disclosed are methods for treating a kinase-affected disease or condition comprising administering to a subject in need thereof a therapeutically effective amount of a disclosed organometallic kinase inhibitor.
摘要翻译： 提供了抑制人黑素瘤细胞中PI3K脂质激酶和磷酸化AKT的新型有机金属化合物，并且还抑制黑素瘤细胞的迁移。 本发明还涉及抑制癌细胞增殖，迁移或两者的方法，包括使癌细胞与公开的有机金属激酶抑制剂接触。 还公开了用于治疗激酶受影响的疾病或病症的方法，包括向有需要的受试者施用治疗有效量的所公开的有机金属激酶抑制剂。
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6.发明申请公开(公告)号：US20080305496A1
公开(公告)日：2008-12-11
申请号：US12023287
申请日：2008-01-31
IPC分类号： G01N33/573 , C12N9/00
CPC分类号： C12Q1/25 , G01N2333/986 , G01N2500/04
摘要： The present invention relates to a method for identifying compounds that modulate the activity of sirtuin deacetylase protein family members. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified nicotinamide inhibition and base exchange site of Sir2 and testing the compound for its ability to modulate the activity of the Sir2 protein. Compositions and methods for preventing or treating diseases or disorders associated with Sir2 are also provided.
摘要翻译： 本发明涉及一种鉴定调节沉默调节蛋白脱乙酰酶蛋白家族成员活性的化合物的方法。 通过设计或筛选与新鉴定的Sir2的烟酰胺抑制和碱基交换位点的至少一个氨基酸残基并测试该化合物调节Sir2蛋白活性的能力的化合物来鉴定本发明的化合物。 还提供了用于预防或治疗与Sir2相关的疾病或病症的组合物和方法。
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公开(公告)号：US08106039B2
公开(公告)日：2012-01-31
申请号：US12112748
申请日：2008-04-30
申请人： Eric Meggers , Peng Xie , Douglas S. Williams , Ronen Marmorstein
发明人： Eric Meggers , Peng Xie , Douglas S. Williams , Ronen Marmorstein
IPC分类号： A61K31/555 , C07F15/00
CPC分类号： C07D498/22 , C07D487/14
摘要： Provided are novel organometallic compounds that inhibit PI3K lipid kinase and phospho-AKT in human melanoma cells, and also inhibit the migration of melanoma cells. The present invention is also directed to methods for inhibiting cancer cell proliferation, migration or both comprising contacting a cancer cell with a disclosed organometallic kinase inhibitor. Also disclosed are methods for treating a kinase-affected disease or condition comprising administering to a subject in need thereof a therapeutically effective amount of a disclosed organometallic kinase inhibitor.
摘要翻译： 提供了抑制人黑素瘤细胞中PI3K脂质激酶和磷酸化AKT的新型有机金属化合物，并且还抑制黑素瘤细胞的迁移。 本发明还涉及抑制癌细胞增殖，迁移或两者的方法，包括使癌细胞与公开的有机金属激酶抑制剂接触。 还公开了用于治疗激酶受影响的疾病或病症的方法，包括向有需要的受试者施用治疗有效量的所公开的有机金属激酶抑制剂。
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