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公开(公告)号：US20110229875A1
公开(公告)日：2011-09-22
申请号：US13079269
申请日：2011-04-04
申请人： Yasushi Yamazoe , Kiyoshi Nagata
发明人： Yasushi Yamazoe , Kiyoshi Nagata
CPC分类号： C12Q1/6897 , C12Q1/02 , C12Q1/26 , G01N33/5008 , G01N33/5023 , G01N33/5067 , G01N2333/90245 , G01N2333/90251 , G01N2500/04 , G01N2500/10
摘要： A method for measuring human CYP3A inducibility upon administration of a test drug, characterized in that anon-human animal to which a test drug is administered or a population of human cells cultured in a medium containing a test drug is infected with viruses (A) and (B); virus (A) being an adenovirus which is used as a vector and engineered by incorporating thereto a detectable reporter gene and at least 3 human PXR binding regions falling within an untranslated region of a human CYP3A gene, and virus (B) being an adenovirus which is used as a vector and engineered by incorporating thereto a human PXR cDNA; and subsequently expression level of the reporter gene is determined in the non-human animal or the cultured human cells.The present invention ensures convenient and accurate evaluation of human CYP3A inducibility upon administration of a test drug to a human subject, providing accurate evaluation in terms of the efficacy of the test drug, occurrence of side effects, disappearance of the drug effect, etc.
摘要翻译： 一种在给药试验药物时测定人CYP3A诱导率的方法，其特征在于，在含有试验药物的培养基中培养的肛 - 人动物或受试药物培养的人群受病毒（A）和 （B）; 病毒（A）是腺病毒，其用作载体并通过掺入可检测的报道基因和位于人CYP3A基因的非翻译区内的至少3个人PXR结合区域而工程化，并且病毒（B）是腺病毒， 用作载体并通过掺入人PXR cDNA而工程化; 并且随后在非人动物或培养的人细胞中测定报道基因的表达水平。 本发明确保了将人体受试者给药后的人CYP3A诱导率的方便，准确的评价，在试验药物的功效，副作用的发生，药物作用的消失等方面提供准确的评价。
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公开(公告)号：US20130164735A1
公开(公告)日：2013-06-27
申请号：US13754006
申请日：2013-01-30
申请人： Yasushi Yamazoe , Kiyoshi Nagata
发明人： Yasushi Yamazoe , Kiyoshi Nagata
IPC分类号： C12Q1/66
CPC分类号： C12Q1/6897 , C12Q1/02 , C12Q1/26 , G01N33/5008 , G01N33/5023 , G01N33/5067 , G01N2333/90245 , G01N2333/90251 , G01N2500/04 , G01N2500/10
摘要： A method for measuring human CYP3A inducibility upon administration of a test drug, characterized in that a non-human animal to which a test drug is administered or a population of human cells cultured in a medium containing a test drug is infected with viruses (A) and (B); virus (A) being an adenovirus which is used as a vector and engineered by incorporating thereto a detectable reporter gene and at least 3 human PXR binding regions falling within an untranslated region of a human CYP3A gene, and virus (B) being an adenovirus which is used as a vector and engineered by incorporating thereto a human PXR cDNA; and subsequently expression level of the reporter gene is determined in the non-human animal or the cultured human cells.
摘要翻译： 一种在给药试验药物时测量人CYP3A诱导率的方法，其特征在于，在含有试验药物的培养基中培养的非人动物或受试药物培养的人群受病毒感染（A） 和（B）; 病毒（A）是腺病毒，其用作载体并通过掺入可检测的报道基因和位于人CYP3A基因的非翻译区内的至少3个人PXR结合区域而工程化，并且病毒（B）是腺病毒， 用作载体并通过掺入人PXR cDNA而工程化; 并且随后在非人动物或培养的人细胞中测定报道基因的表达水平。
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公开(公告)号：US20050142064A1
公开(公告)日：2005-06-30
申请号：US10510237
申请日：2003-04-15
申请人： Yasushi Yamazoe , Kiyoshi Nagata
发明人： Yasushi Yamazoe , Kiyoshi Nagata
IPC分类号： C12N15/09 , C12N5/10 , C12N7/00 , C12Q1/02 , C12Q1/26 , C12Q1/66 , C12Q1/70 , G01N33/50 , A61K49/00 , C12N15/86
CPC分类号： C12Q1/6897 , C12Q1/02 , C12Q1/26 , G01N33/5008 , G01N33/5023 , G01N33/5067 , G01N2333/90245 , G01N2333/90251 , G01N2500/04 , G01N2500/10
摘要： A method for measuring human CYP3A inducibility upon administration of a test drug, characterized in that a non-human animal to which a test drug is administered or a population of human cells cultured in a medium containing a test drug is infected with viruses (A) and (B); virus (A) being an adenovirus which is used as a vector and engineered by incorporating thereto a detectable reporter gene and at least 3 human PXR binding regions falling within an untranslated region of a human CYP3A gene, and virus (B) being an adenovirus which is used as a vector and engineered by incorporating thereto a human PXR cDNA; and subsequently expression level of the reporter gene is determined in the non-human animal or the cultured human cells. The present invention ensures convenient and accurate evaluation of human CYP3A inducibility upon administration of a test drug to a human subject, providing accurate evaluation in terms of the efficacy of the test drug, occurrence of side effects, disappearance of the drug effect, etc.
摘要翻译： 一种在给药试验药物时测量人CYP3A诱导率的方法，其特征在于，在含有试验药物的培养基中培养的非人动物或受试药物培养的人群受病毒感染（A） 和（B）; 病毒（A）是腺病毒，其用作载体并通过掺入可检测的报道基因和位于人CYP3A基因的非翻译区内的至少3个人PXR结合区域而工程化，并且病毒（B）是腺病毒， 用作载体并通过掺入人PXR cDNA而工程化; 并且随后在非人动物或培养的人细胞中测定报道基因的表达水平。 本发明确保了将人体受试者给药后的人CYP3A诱导率的方便，准确的评价，在试验药物的功效，副作用的发生，药物作用的消失等方面提供准确的评价。
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公开(公告)号：US07910362B2
公开(公告)日：2011-03-22
申请号：US11995398
申请日：2006-07-12
申请人： Rika Ueda , Kazutomi Kusano , Yasushi Yamazoe , Kiyoshi Nagata
发明人： Rika Ueda , Kazutomi Kusano , Yasushi Yamazoe , Kiyoshi Nagata
CPC分类号： C12N15/1086
摘要： A reporter vector which can evaluate the ability of a drug to induce CYP1A2 or both of CYP1A1 and CYP1A2 and a method for evaluation of the ability of a drug to induce CYP1A2 or both of CYP1A1 and CYP1A2 by using the reporter vector. A reporter system which can evaluate the ability of a drug capable of inducing CYP1A2 or both of CYP1A1 and CYP1A2 is completed by constructing a reporter vector having a reporter gene linked to the 3′ end of a region between CYP1A1 and CYP1A2 or a reporter vector having different reporter genes linked to the both ends of the region, respectively, so as to sandwich the region, and a reporter vector having a deletion mutation in the region, and confirming that the expression of a reporter molecule is increased by the drug capable of inducing CYP1A2 or both of CYP1A1 and CYP1A2 in the reporter system using the reporter vector.
摘要翻译： 可以评估药物诱导CYP1A2或CYP1A1和CYP1A2两者的能力的报告载体，以及通过使用报道载体评价药物诱导CYP1A2或CYP1A1和CYP1A2两者能力的方法。 可以通过构建具有与CYP1A1和CYP1A2之间的区域的3'末端连接的报道基因的报道载体或具有CYP1A1和CYP1A2两者的报道载体的报道载体来完成能够评价能够诱导CYP1A2或CYP1A1和CYP1A2两者的药物的能力的报道体系， 分别与区域两端连接的不同的报道基因以夹持该区域，以及在该区域具有缺失突变的报道载体，并证实报告分子的表达由能诱导的药物增加 CYP1A2或两者CYP1A1和CYP1A2在报告系统中使用报告载体。
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公开(公告)号：US20090317800A1
公开(公告)日：2009-12-24
申请号：US11995398
申请日：2006-07-12
申请人： Rika Ueda , Kazutomi Kusano , Yasushi Yamazoe , Kiyoshi Nagata
发明人： Rika Ueda , Kazutomi Kusano , Yasushi Yamazoe , Kiyoshi Nagata
CPC分类号： C12N15/1086
摘要： A reporter vector which can evaluate the ability of a drug to induce CYP1A2 or both of CYP1A1 and CYP1A2 and a method for evaluation of the ability of a drug to induce CYP1A2 or both of CYP1A1 and CYP1A2 by using the reporter vector. A reporter system which can evaluate the ability of a drug capable of inducing CYP1A2 or both of CYP1A1 and CYP1A2 is completed by constructing a reporter vector having a reporter gene linked to the 3′ end of a region between CYP1A1 and CYP1A2 or a reporter vector having different reporter genes linked to the both ends of the region, respectively, so as to sandwich the region, and a reporter vector having a deletion mutation in the region, and confirming that the expression of a reporter molecule is increased by the drug capable of inducing CYP1A2 or both of CYP1A1 and CYP1A2 in the reporter system using the reporter vector.
摘要翻译： 可以评估药物诱导CYP1A2或CYP1A1和CYP1A2两者的能力的报告载体，以及通过使用报道载体评价药物诱导CYP1A2或CYP1A1和CYP1A2两者能力的方法。 可以通过构建具有与CYP1A1和CYP1A2之间的区域的3'末端连接的报道基因的报道载体或具有CYP1A1和CYP1A2两者的报道载体的报道载体来完成能够评价能够诱导CYP1A2或CYP1A1和CYP1A2两者的药物的能力的报道体系， 分别与区域两端连接的不同的报道基因以夹持该区域，以及在该区域具有缺失突变的报道载体，并证实报告分子的表达由能诱导的药物增加 CYP1A2或两者CYP1A1和CYP1A2在报告系统中使用报告载体。
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公开(公告)号：US20060194248A1
公开(公告)日：2006-08-31
申请号：US11414189
申请日：2006-05-01
申请人： Yasushi Yamazoe , Kiyoshi Nagata
发明人： Yasushi Yamazoe , Kiyoshi Nagata
CPC分类号： C12Q1/6897 , C12Q1/02 , C12Q1/26 , G01N33/5008 , G01N33/5023 , G01N33/5067 , G01N2333/90245 , G01N2333/90251 , G01N2500/04 , G01N2500/10
摘要： A method for measuring human CYP3A inducibility upon administration of a test drug, characterized in that a non-human animal to which a test drug is administered or a population of human cells cultured in a medium containing a test drug is infected with viruses (A) and (B); virus (A) being an adenovirus which is used as a vector and engineered by incorporating thereto a detectable reporter gene and at least 3 human PXR binding regions falling within an untranslated region of a human CYP3A gene, and virus (B) being an adenovirus which is used as a vector and engineered by incorporating thereto a human PXR cDNA; and subsequently expression level of the reporter gene is determined in the non-human animal or the cultured human cells. The present invention ensures convenient and accurate evaluation of human CYP3A inducibility upon administration of a test drug to a human subject, providing accurate evaluation in terms of the efficacy of the test drug, occurrence of side effects, disappearance of the drug effect, etc.
摘要翻译： 一种在给药试验药物时测量人CYP3A诱导率的方法，其特征在于，在含有试验药物的培养基中培养的非人动物或受试药物培养的人群受病毒感染（A） 和（B）; 病毒（A）是腺病毒，其用作载体并通过掺入可检测的报道基因和位于人CYP3A基因的非翻译区内的至少3个人PXR结合区域而工程化，并且病毒（B）是腺病毒， 用作载体并通过掺入人PXR cDNA而工程化; 并且随后在非人动物或培养的人细胞中测定报道基因的表达水平。 本发明确保了将人体受试者给药后的人CYP3A诱导率的方便，准确的评价，在试验药物的功效，副作用的发生，药物作用的消失等方面提供准确的评价。
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公开(公告)号：US20110029296A1
公开(公告)日：2011-02-03
申请号：US12801900
申请日：2010-06-30
IPC分类号： G06G7/60
摘要： A ring structure of a predicted target compound which is in a two-dimensional structural formula is arranged so as to be in an identical position as a ring structure of a template produced by superimposing two-dimensional structural formulae of compounds capable of forming a complex with a predetermined enzyme. Among predicted target compounds overlapping with a metabolic target site of the template, predicted target compounds other than those determined as being unable to access a metabolic active center site of the enzyme, or those having the same charge as that of the metabolic active center site, are determined to be metabolizable compounds. Based on the level of contribution of each atom included in the template during a metabolic reaction of the enzyme, a structural formula of a compound obtained after the metabolic reaction of the metabolizable compound whose metabolic target site has been determined is determined.
摘要翻译： 将具有二维结构式的预测目标化合物的环结构排列成与通过将能够形成络合物的化合物的二维结构式叠加而形成的模板的环结构相同的位置 预定的酶。 在与模板的代谢靶位点重叠的预测目标化合物中，除了被确定为不能进入酶的代谢活性中心位点的那些或与代谢活性中心位点具有相同电荷的那些之外的预测目标化合物， 被确定为可代谢的化合物。 基于酶代谢反应期间包含在模板中的每个原子的贡献水平，确定在已经测定其代谢靶位点的代谢反应后的代谢反应后获得的化合物的结构式。
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公开(公告)号：US20070016392A1
公开(公告)日：2007-01-18
申请号：US11524208
申请日：2006-09-21
申请人： Masato Kitajima , Jose Ciloy , Yasushi Yamazoe
发明人： Masato Kitajima , Jose Ciloy , Yasushi Yamazoe
摘要： A drug-metabolizing enzyme prediction apparatus acquires compound structure information, identifies binding site information and molecular species information based on a binding-site identifying condition, specifies a pinching point that is an atom binding at least between a reactive site and a binding site, acquires pinching point information on the specified pinching point and reactive site information on the reactive site bound to the pinching point, and identifies the acquired reactive site information based on a reactive-site identifying condition and the acquired pinching point information based on a pinching-point identifying condition.
摘要翻译： 药物代谢酶预测装置获取化合物结构信息，基于结合位点识别条件鉴定结合位点信息和分子种类信息，指定至少在反应位点与结合位点之间结合的原子的夹点，获取 针对绑定点的反应性站点上的指定收敛点和反应站点信息的收集点信息，并且基于反应站点识别条件识别所获取的反应站点信息，并且基于收集点标识来获取所获取的收缩点信息 条件。
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