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1.发明授权Methods of assaying receptor activity and constructs useful in such methods 有权测定受体活性的方法和在这些方法中有用的构建体
公开(公告)号：US6110693A
公开(公告)日：2000-08-29
申请号：US233530
申请日：1999-01-20
CPC分类号： G01N33/5008 , C07K14/47 , C12N15/62 , C07K2319/00 , C07K2319/60 , G01N2333/726 , G01N2333/91
摘要： Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G Protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process. Constructs useful in such methods are described.
摘要翻译： 描述了体内和体外检测G蛋白偶联受体（GPCR）活性的方法; 测定GPCR活性的方法; 和筛选GPCR配体，G蛋白偶联受体激酶（GRK）活性和与GPCR调节过程的组分相互作用的化合物的方法。 描述在这些方法中有用的构造。
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公开(公告)号：US5891646A
公开(公告)日：1999-04-06
申请号：US869568
申请日：1997-06-05
CPC分类号： G01N33/5008 , C07K14/47 , C12N15/62 , C07K2319/00 , C07K2319/60 , G01N2333/726 , G01N2333/91
摘要： Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process. Constructs useful in such methods are described.
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公开(公告)号：US07572888B2
公开(公告)日：2009-08-11
申请号：US10785841
申请日：2004-02-24
IPC分类号： C07K14/00 , C07K17/00 , G01N33/53 , G01N33/567
CPC分类号： C12N15/8509 , A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/03 , A01K2267/0356 , A01K2267/0393 , C07K14/47 , C07K14/4702 , C07K2319/00 , C07K2319/60 , C12N15/62
摘要： Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process. Constructs useful in such methods are described.
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公开(公告)号：US06770449B2
公开(公告)日：2004-08-03
申请号：US09772644
申请日：2001-01-30
IPC分类号： G01N33567
CPC分类号： C12N15/8509 , A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/03 , A01K2267/0356 , A01K2267/0393 , C07K14/47 , C07K14/4702 , C07K2319/00 , C07K2319/60 , C12N15/62
摘要： Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process. Constructs useful in such methods are described.
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公开(公告)号：US07138240B2
公开(公告)日：2006-11-21
申请号：US10141725
申请日：2002-05-09
IPC分类号： G01N33/566 , G01N21/76 , G01N33/53
CPC分类号： G01N33/5008 , C07K14/47 , C07K2319/00 , C07K2319/60 , C12N15/62 , G01N2333/726 , G01N2333/91
摘要： Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G Protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process.
摘要翻译： 描述了体内和体外检测G蛋白偶联受体（GPCR）活性的方法; 测定GPCR活性的方法; 和筛选GPCR配体，G蛋白偶联受体激酶（GRK）活性和与GPCR调节过程的组分相互作用的化合物的方法。
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6.发明申请Methods of assaying receptor activity and constructs useful in such methods 审中-公开测定受体活性的方法和在这些方法中有用的构建体公开(公告)号：US20080261256A1
公开(公告)日：2008-10-23
申请号：US11875581
申请日：2007-10-19
CPC分类号： G01N33/5008 , C07K14/47 , C07K2319/00 , C07K2319/60 , C12N15/62 , G01N2333/726 , G01N2333/91
摘要： Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process. Constructs useful in such methods are described.
摘要翻译： 描述了体内和体外检测G蛋白偶联受体（GPCR）活性的方法; 测定GPCR活性的方法; 和筛选GPCR配体，G蛋白偶联受体激酶（GRK）活性和与GPCR调节过程的组分相互作用的化合物的方法。 描述在这些方法中有用的构造。
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7.发明申请METHOD OF SCREENING THE ACTIVITY OF THE SMOOTHENED RECEPTOR TO IDENTIFY THERAPUTIC MODULATION AGENTS OR DIAGNOSE DISEASE 审中-公开筛选平滑肌受体活性鉴定治疗药物或诊断疾病的方法公开(公告)号：US20090263317A1
公开(公告)日：2009-10-22
申请号：US12097697
申请日：2006-12-14
申请人： Wei Chen , Lawrence S. Barak , Marc G. Caron , Robert Lefkowitz
发明人： Wei Chen , Lawrence S. Barak , Marc G. Caron , Robert Lefkowitz
CPC分类号： G01N33/5011 , G01N33/57492
摘要： The invention relates to a screening method for the Smoothened receptor for testing compositions as potential Smoothened receptor ligands, either agonist or antagonist activity, by use of an arrestin-reporter molecule conjugate. It also relates to testing cells and individuals by administering a smoothened receptor ligand-reporter molecule conjugate and observing locations where the ligand binds and then using an increased number of surface Smoothened receptors compared to a pre-established criteria as an indication of a cancerous growth or tumor.
摘要翻译： 本发明涉及平滑化受体的筛选方法，通过使用抑制蛋白 - 报告分子缀合物将组合物测试为潜在的平滑受体配体，即激动剂或拮抗剂活性。 它还涉及通过施用平滑化的受体配体 - 报告分子缀合物和观察配体结合的位置，然后使用增加数目的表面平滑受体来测试细胞和个体，与预先确定的标准相比，作为癌性生长的指示或 瘤。
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8.发明申请Single-cell biosensor for the measurement of GPCR ligands in a test sample 审中-公开用于测试样品中GPCR配体的单细胞生物传感器公开(公告)号：US20090226949A1
公开(公告)日：2009-09-10
申请号：US12398027
申请日：2009-03-04
IPC分类号： C12Q1/46
CPC分类号： G01N33/5035 , G01N33/5008 , G01N33/5014 , G01N33/5091 , G01N33/74 , G01N2333/5758 , G01N2333/70571 , G01N2333/726
摘要： The present invention is related to the detection of GPCR ligands in a test sample by using a single cell biosensor expressing a GPCR. Preferably, the test sample is derived from a biological or environmental sample. This invention may be used to detect the presence of a disease or to detect the presence of a harmful agent in the environment. Included in the present invention is an array of biosensors that detect ligands of various GPCRs.
摘要翻译： 本发明涉及通过使用表达GPCR的单细胞生物传感器检测测试样品中的GPCR配体。 优选地，测试样品来自生物或环境样品。 本发明可用于检测疾病的存在或检测环境中有害物质的存在。 本发明包括检测各种GPCR的配体的生物传感器阵列。
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9.发明授权Methods of screening compositions for G protein-coupled receptor desensitization inhibitory activity 有权筛选G蛋白偶联受体脱敏抑制活性组合物的方法公开(公告)号：US07163800B2
公开(公告)日：2007-01-16
申请号：US10633438
申请日：2003-08-01
IPC分类号： G01N33/566
CPC分类号： C07K14/705
摘要： The methods of the present invention allow the screening of a test composition for non-receptor-specific GPCR desensitization inhibitory activity. The methods involve screening a test composition for an indication of GPCR desensitization inhibitory activity against two or more GPCRs that are different from each other. When there is an indication that a particular test composition has GPCR desensitization inhibitory activity with respect to each of the two or more GPCRs that are different from one another, then, according to the present invention, there is an indication that the test composition has non-receptor-specific GPCR desensitization inhibitory activity.
摘要翻译： 本发明的方法允许筛选非受体特异性GPCR脱敏抑制活性的测试组合物。 所述方法包括筛选测试组合物以对于彼此不同的两个或多个GPCR的GPCR脱敏抑制活性的指示。 当存在特定测试组合物相对于彼此不同的两个或更多个GPCR中的每一个具有GPCR脱敏抑制活性的指示时，根据本发明，存在测试组合物具有非 - - 受体特异性GPCR脱敏抑制活性。
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公开(公告)号：US07018812B2
公开(公告)日：2006-03-28
申请号：US09993844
申请日：2001-11-05
IPC分类号： C07K14/705 , C07K19/00 , C12N15/62
CPC分类号： C07K14/705
摘要： The present invention relates to modified G-protein coupled receptors (GPCRs). The modified GPCRs of the present invention include GPCRs that have been modified to have carboxyl terminal tails comprising one or more sites of phosphorylation, preferably one or more clusters of phosphorylation sites. The modified GPCRs of the present invention may comprise a retained portion of a carboxyl-terminus region from a first GPCR fused to a polypeptide, wherein the polypeptide comprises the one or more clusters of phosphorylation. The present invention also relates to methods of screening compounds and sample solutions for GPCR activity using the modified GPCRs.
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