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公开(公告)号：US20100196930A1
公开(公告)日：2010-08-05
申请号：US12683527
申请日：2010-01-07
申请人： Jian-Shen Qi , Wensheng Lang , Margery A. Connelly
发明人： Jian-Shen Qi , Wensheng Lang , Margery A. Connelly
IPC分类号： G01N33/567
CPC分类号： G01N33/5038 , C12Q1/48 , G01N33/60 , G01N33/92
摘要： A method for identifying a compound which modulates the activity of acyl-coA: diacylglycerol acyltransferase comprises the steps of contacting a stable isotope labeled fatty acid with cells in either presence or absence of the compound, extracting the cells with isopropyl alcohol, and determining the level of a stable isotope labeled triglyceride in the presence or absence of the compound; wherein a change in the level of the stable isotope labeled triglyceride indicates that the compound modulates the DGAT activity.
摘要翻译： 用于鉴定调节酰基-CoA：二酰基甘油酰基转移酶的活性的化合物的方法包括以下步骤：在化合物的存在或不存在下使稳定同位素标记的脂肪酸与细胞接触，用异丙醇萃取细胞，并测定水平 的化合物存在或不存在下的稳定同位素标记的甘油三酸酯; 其中稳定同位素标记的甘油三酯水平的变化表明该化合物调节DGAT活性。
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公开(公告)号：US06803203B1
公开(公告)日：2004-10-12
申请号：US09695437
申请日：2000-10-24
IPC分类号： C12Q148
摘要： The present invention provides a method for detecting DNA-activated protein kinase (DNA-PK) activity in a biological sample. The method includes contacting a biological sample with a detectably-labeled phosphate donor and a synthetic peptide substrate defined by the following features to provide specific recognition and phosphorylation by DNA-PK: (1) a phosphate-accepting amino acid pair which may include serine-glutamine (Ser-Gln) (SQ), threonine-glutamine (Thr-Gln) (TQ), glutamine-serine (Gln-Ser) (QS), or glutamine-threonine (Gln-Thr) (QT); (2) enhancer amino acids which may include glutamic acid or glutamine immediately adjacent at the amino- or carboxyl- side of the amino acid pair and forming an amino acid pair-enhancer unit; (3) a first spacer sequence at the amino terminus of the amino acid pair-enhancer unit; (4) a second spacer sequence at the carboxyl terminus of the amino acid pair-enhancer unit, which spacer sequences may include any combination of amino acids that does not provide a phosphorylation site consensus sequence motif; and, (5) a tag moiety, which may be an amino acid sequence or another chemical entity that permits separating the synthetic peptide from the phosphate donor. A compostion and a kit for the detection of DNA-PK activity are also provided. Methods for detecting DNA, protein phosphatases and substances that alter the activity of DNA-PK are also provided. The present invention also provides a method of monitoring protein kinase and DNA-PK activity in living cells. -A composition and a kit for monitoring protein kinase activity in vitro and a composition and a kit for monitoring DNA-PK activities in living cells are also provided. A method for identifying agents that alter protein kinase activity in vitro and a method for identifying agents that alter DNA-PK activity in living cells are also provided.
摘要翻译： 本发明提供了检测生物样品中DNA-活化蛋白激酶（DNA-PK）活性的方法。 该方法包括使生物样品与可检测标记的磷酸供体和由以下特征定义的合成肽底物接触，以通过DNA-PK提供特异性识别和磷酸化：（1）磷酸受体氨基酸对，其可以包括丝氨酸 - 谷氨酰胺（Ser-Gln）（SQ），苏氨酸 - 谷氨酰胺（Thr-Gln）（TQ），谷氨酰胺 - 丝氨酸（Gln-Ser）（QS）或谷氨酰胺 - 苏氨酸（Gln-Thr）（QT） （2）增强子氨基酸，其可以包括在氨基酸对的氨基或羧基侧紧邻的谷氨酸或谷氨酰胺，并形成氨基酸对增强子单元; （3）氨基酸对增强子单元的氨基末端的第一间隔序列; （4）在氨基酸对增强子单元的羧基末端的第二间隔序列，该间隔序列可以包括不提供磷酸化位点共有序列基序的氨基酸的任何组合; 和（5）标签部分，其可以是允许从磷酸盐供体分离合成肽的氨基酸序列或另一种化学实体。 还提供了用于检测DNA-PK活性的组合物和试剂盒。 还提供了检测DNA，蛋白磷酸酶和改变DNA-PK活性的物质的方法。 本发明还提供了一种在活细胞中监测蛋白激酶和DNA-PK活性的方法。 还提供了用于在体外监测蛋白激酶活性的组合物和试剂盒，还提供了用于监测活细胞中的DNA-PK活性的组合物和试剂盒。 还提供了用于鉴定在体外改变蛋白激酶活性的试剂的方法和用于鉴定改变活细胞中DNA-PK活性的试剂的方法。
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3.发明授权公开(公告)号：US06803204B2
公开(公告)日：2004-10-12
申请号：US10188937
申请日：2002-07-03
IPC分类号： C12Q148
CPC分类号： C12N9/12
摘要： The present invention provides isolated I&kgr;B kinases that regulate NF&kgr;B gene transcription that lack both a leucine zipper like &agr;-helix domain and helix-loop-helix domain. Also provided are the amino acid sequences of these kinases and the nucleotide sequence encoding these kinases, and other related protein and nucleic acid molecules.
摘要翻译： 本发明提供了分离的IkappaB激酶，其调节缺乏亮氨酸拉链如α-螺旋结构域和螺旋 - 环 - 螺旋结构域的NFkappaB基因转录。 还提供了这些激酶的氨基酸序列和编码这些激酶的核苷酸序列以及其它相关的蛋白质和核酸分子。
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公开(公告)号：US08852556B2
公开(公告)日：2014-10-07
申请号：US12603360
申请日：2009-10-21
IPC分类号： A61K49/00
CPC分类号： A61K49/0008
摘要： A method for evaluating the effect of a compound on vasomotor response in vivo comprises the steps of administering said compound to a rabbit and measuring the diameter of the vessel lumen of a central ear artery of said rabbit in comparison with the baseline diameter of the vessel lumen of said central ear artery of said rabbit, said baseline diameter being measured prior to the administration of said compound.
摘要翻译： 用于评估化合物对体内血管舒缩反应的影响的方法包括以下步骤：将所述化合物给予兔子，并测量所述兔子的中枢动脉的血管腔的直径与血管腔的基线直径相比 的所述兔的所述中枢动脉，所述基线直径在施用所述化合物之前测量。
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5.发明授权公开(公告)号：US06489151B1
公开(公告)日：2002-12-03
申请号：US09536882
申请日：2000-03-27
IPC分类号： C12N912
CPC分类号： C12N9/12
摘要： The present invention provides isolated I&kgr;B kinases that regulate NF&kgr;B gene transcription that lack both a leucine zipper like &agr;-helix domain and helix-loop-helix domain. Also provided are the amino acid sequences of these kinases and the nucleotide sequence encoding these kinases, and other related protein and nucleic acid molecules.
摘要翻译： 本发明提供了分离的IkappaB激酶，其调节缺乏亮氨酸拉链如α-螺旋结构域和螺旋 - 环 - 螺旋结构域的NFkappaB基因转录。 还提供了这些激酶的氨基酸序列和编码这些激酶的核苷酸序列以及其它相关的蛋白质和核酸分子。
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公开(公告)号：US09012159B2
公开(公告)日：2015-04-21
申请号：US12683527
申请日：2010-01-07
申请人： Jian-Shen Qi , Wensheng Lang , Margery A. Connelly
发明人： Jian-Shen Qi , Wensheng Lang , Margery A. Connelly
IPC分类号： G01N33/567 , G01N33/50 , C12Q1/48 , G01N33/60 , G01N33/92
CPC分类号： G01N33/5038 , C12Q1/48 , G01N33/60 , G01N33/92
摘要： A method for identifying a compound which modulates the activity of acyl-coA: diacylglycerol acyltransferase comprises the steps of contacting a stable isotope labeled fatty acid with cells in either presence or absence of the compound, extracting the cells with isopropyl alcohol, and determining the level of a stable isotope labeled triglyceride in the presence or absence of the compound; wherein a change in the level of the stable isotope labeled triglyceride indicates that the compound modulates the DGAT activity.
摘要翻译： 用于鉴定调节酰基-CoA：二酰基甘油酰基转移酶的活性的化合物的方法包括以下步骤：在化合物的存在或不存在下使稳定同位素标记的脂肪酸与细胞接触，用异丙醇萃取细胞，并测定水平 的化合物存在或不存在下的稳定同位素标记的甘油三酸酯; 其中稳定同位素标记的甘油三酯水平的变化表明该化合物调节DGAT活性。
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7.发明申请公开(公告)号：US20120077847A1
公开(公告)日：2012-03-29
申请号：US13245137
申请日：2011-09-26
申请人： Michael N. Greco , Margery A. Connelly , Shyamali Ghosh , Dennis J. Hlasta , Edward C. Lawson , Eric Strobel , Michele A. Weidner-Wells , Hong Ye
发明人： Michael N. Greco , Margery A. Connelly , Shyamali Ghosh , Dennis J. Hlasta , Edward C. Lawson , Eric Strobel , Michele A. Weidner-Wells , Hong Ye
IPC分类号： A61K31/4245 , C07D285/12 , C07D417/12 , A61P7/00 , A61K31/4439 , A61P9/10 , A61P3/06 , C07D271/107 , A61K31/433
CPC分类号： C07D271/10 , C07D249/08 , C07D285/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention is directed to α-ketoamide derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
摘要翻译： 本发明涉及α-酮酰胺衍生物，含有它们的药物组合物及其用于治疗由内皮脂肪酶调节的病症和状况的用途，例如心血管疾病。
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公开(公告)号：US08476302B2
公开(公告)日：2013-07-02
申请号：US13245137
申请日：2011-09-26
申请人： Michael N. Greco , Margery A. Connelly , Shyamali Ghosh , Dennis J. Hlasta , Edward C. Lawson , Eric Strobel , Michele A. Weidner-Wells , Hong Ye
发明人： Michael N. Greco , Margery A. Connelly , Shyamali Ghosh , Dennis J. Hlasta , Edward C. Lawson , Eric Strobel , Michele A. Weidner-Wells , Hong Ye
IPC分类号： A61K31/4245 , A61K31/4439 , A61K31/433 , C07D285/12 , C07D417/12 , C07D271/107
CPC分类号： C07D271/10 , C07D249/08 , C07D285/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention is directed to α-ketoamide derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
摘要翻译： 本发明涉及α-酮酰胺衍生物，含有它们的药物组合物及其用于治疗由内皮脂肪酶调节的病症和状况的用途，例如心血管疾病。
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公开(公告)号：US20100189654A1
公开(公告)日：2010-07-29
申请号：US12603360
申请日：2009-10-21
IPC分类号： A61K49/00
CPC分类号： A61K49/0008
摘要： A method for evaluating the effect of a compound on vasomotor response in vivo comprises the steps of administering said compound to a rabbit and measuring the diameter of the vessel lumen of a central ear artery of said rabbit in comparison with the baseline diameter of the vessel lumen of said central ear artery of said rabbit, said baseline diameter being measured prior to the administration of said compound.
摘要翻译： 用于评估化合物对体内血管舒缩反应的影响的方法包括以下步骤：将所述化合物给予兔子，并测量所述兔子的中枢动脉的血管腔的直径与血管腔的基线直径相比 的所述兔的所述中枢动脉，所述基线直径在施用所述化合物之前测量。
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