公开(公告)号：EP2267458A2

公开(公告)日：2010-12-29

申请号：EP10174532.1

申请日：2005-04-20

申请人： Galapagos N.V.

发明人： Merchiers, Pascal Gerard ,  Spittaels, Koenraad Frederik Florentina ,  Hoffmann, Marcel

IPC分类号： G01N33/68 ,  G01N33/566

CPC分类号： C12Q1/37 ,  G01N33/566 ,  G01N33/6896 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2800/2821

摘要： A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a GPCR polypeptide (GPR12), or fragment thereof, and measuring a compound-GPCR property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of GPCR expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.

摘要翻译： 用于鉴定抑制细胞中淀粉样蛋白β前体蛋白加工的化合物的方法，包括使测试化合物与GPCR多肽（GPR12）或其片段接触，并测量与淀粉状蛋白-β肽的产生相关的化合物-GPCR性质。 所述方法的细胞测定测量指标，包括第二信使和/或淀粉样蛋白β肽水平。 包括有效淀粉样蛋白-β前体加工抑制量的GPCR表达抑制剂的治疗方法和药物组合物可用于治疗涉及认知障碍的疾病如阿尔茨海默病。

公开(公告)号：EP2267458A3

公开(公告)日：2011-04-06

申请号：EP10174532.1

申请日：2005-04-20

申请人： Galapagos N.V.

发明人： Merchiers, Pascal Gerard ,  Spittaels, Koenraad Frederik Florentina ,  Hoffmann, Marcel

IPC分类号： G01N33/68 ,  G01N33/566

CPC分类号： C12Q1/37 ,  G01N33/566 ,  G01N33/6896 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2800/2821

摘要： A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a GPCR polypeptide (GPR12), or fragment thereof, and measuring a compound-GPCR property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of GPCR expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.

公开(公告)号：EP2270513A2

公开(公告)日：2011-01-05

申请号：EP10174529.7

申请日：2005-04-20

申请人： Galapagos N.V.

发明人： Merchiers, Pascal Gerard ,  Spittaels, Koenraad Frederik Florentina ,  Hoffmann, Marcel

IPC分类号： G01N33/68 ,  G01N33/566

CPC分类号： C12Q1/37 ,  G01N33/566 ,  G01N33/6896 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2800/2821

摘要： A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a GPCR polypeptide (GPR6), or fragment thereof, and measuring a compound-GPCR property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of GPCR expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.

摘要翻译： 鉴定抑制细胞中淀粉样-β前体蛋白加工的化合物的方法，包括使测试化合物与GPCR多肽（GPR6）或其片段接触，并测量与产生淀粉样-β肽有关的化合物-GPCR特性。 该方法的细胞分析测量包括第二信使和/或淀粉状蛋白β肽水平的指标。 治疗方法和包括有效抑制淀粉样蛋白前体加工量的GPCR表达抑制剂的药物组合物可用于治疗涉及认知障碍的病症，例如阿尔茨海默病。

公开(公告)号：EP2270513A3

公开(公告)日：2011-04-06

申请号：EP10174529.7

申请日：2005-04-20

申请人： Galapagos N.V.

发明人： Merchiers, Pascal Gerard ,  Spittaels, Koenraad Frederik Florentina ,  Hoffmann, Marcel

IPC分类号： G01N33/68 ,  G01N33/566

CPC分类号： C12Q1/37 ,  G01N33/566 ,  G01N33/6896 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2800/2821

摘要： A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a GPCR polypeptide (GPR6), or fragment thereof, and measuring a compound-GPCR property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of GPCR expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.