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1. 发明专利

JP2007037546A Generic kinase assay 有权
标题翻译：一般激酶测定
公开(公告)号：JP2007037546A
公开(公告)日：2007-02-15
申请号：JP2006207285
申请日：2006-07-31
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： ENDERLE THILO , ROTH DORIS
IPC分类号： C12Q1/42 , C12Q1/48 , G01N33/542
CPC分类号： C12Q1/485 , C12Q1/42 , G01N33/542
摘要： PROBLEM TO BE SOLVED: To provide an effective method of determining kinase or phosphatase activity based on measuring energy transfer between an energy donor and an energy acceptor.
SOLUTION: The invention relates to the method of determining kinase or phosphatase activity based on a three parts system. The method comprises contacting a binding partner (a metal ion on a bead) which can bind phosphorylated peptides, a detection molecule and a substrate peptide. Determination of activities is achieved by measuring energy transfer between an energy donor (Ru-luminophore) and an energy acceptor (phosphor) that are present on the detection molecule and the substrate molecule.
COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：要解决的问题：提供基于测量能量供体和能量受体之间的能量转移来确定激酶或磷酸酶活性的有效方法。解决方案：本发明涉及基于三部分系统确定激酶或磷酸酶活性的方法。该方法包括使可结合磷酸化肽的结合配偶体（珠粒上的金属离子），检测分子和底物肽接触。通过测量存在于检测分子和底物分子上的能量供体（Ru-发光体）和能量受体（荧光体）之间的能量转移来实现活性的测定。版权所有（C）2007，JPO＆INPIT

2. 发明专利

JP2008157939A METHOD FOR DETECTION OF cAMP AND cGMP 有权
标题翻译：检测cAMP和cGMP的方法
公开(公告)号：JP2008157939A
公开(公告)日：2008-07-10
申请号：JP2007326193
申请日：2007-12-18
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： ENDERLE THILO , MATILE HUGUES , ROTH DORIS
IPC分类号： G01N33/542 , G01N21/78 , G01N33/53
CPC分类号： G01N33/542 , C12Q1/68 , G01N33/5735
摘要： PROBLEM TO BE SOLVED: To provide a simple assay for detecting cAMP (cyclic adenosine monophosphate formed upon modulation of adenylyl cyclase activity), and an in vitro method for indirectly detecting receptor activity and for screening of ligands. SOLUTION: The in vitro method for detecting cAMP or cGMP comprises: (a) contacting a mixture with a complex of a tracer and a dequencher, wherein the tracer is a fluorophore covalently linked to cAMP quencher; and (b) measuring the change in fluorescence. Furthermore, the method is used for determining the cAMP or cGMP concentration in the mixture, for determining the activity of a receptor wherein the signal transduction of the receptor comprises cAMP or cGMP, and for screening of a ligand for such a receptor. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供用于检测cAMP（调节腺苷酸环化酶活性时形成的环状腺苷一磷酸）的简单测定法，以及间接检测受体活性和筛选配体的体外方法。解决方案：用于检测cAMP或cGMP的体外方法包括：（a）使混合物与示踪剂和去屑剂的复合物接触，其中示踪剂是与cAMP猝灭剂共价连接的荧光团; 和（b）测量荧光的变化。此外，该方法用于确定混合物中的cAMP或cGMP浓度，用于确定受体的活性，其中受体的信号转导包含cAMP或cGMP，并用于筛选这种受体的配体。版权所有（C）2008，JPO＆INPIT

3. 发明专利

CA2804856A1 METHOD FOR THE IDENTIFICATION OF CATECHOL O-METHYLTRANSFERASE MODULATORS 未知
公开(公告)号：CA2804856A1
公开(公告)日：2012-02-02
申请号：CA2804856
申请日：2011-07-25
申请人： HOFFMANN LA ROCHE
发明人： ENDERLE THILO , ROTH DORIS
IPC分类号： G01N33/58 , C12Q1/48 , G01N33/542 , G01N33/573
摘要： The present invention relates to a method for the identification of modulators of catechol O-methyltransferase enzyme activity (COMT).

4. 发明专利

CA2837957A1 A METHOD FOR THE IDENTIFICATION OF BETA-SHEET AGGREGATED PROTEIN LIGANDS 未知
公开(公告)号：CA2837957A1
公开(公告)日：2012-12-27
申请号：CA2837957
申请日：2012-06-19
申请人： HOFFMANN LA ROCHE
发明人： BORRONI EDILIO , CZECH CHRISTIAN , DORN ARNULF , GOBBI LUCA , GOETSCHY-MEYER VALERIE , GRUENINGER FIONA , ROTH DORIS
IPC分类号： G01N33/68
摘要： The present invention provides an assay for the identification of beta-sheet aggregated protein ligands using Thiazine Red R.

5. 发明专利

ES2368669T3 ENSAYO GENERICO DE DETECCION DE ACTIVIDAD QUINASA/FOSFATASA CON UNA UNICA LECTURA. 未知
公开(公告)号：ES2368669T3
公开(公告)日：2011-11-21
申请号：ES08801776
申请日：2008-09-01
申请人： HOFFMANN LA ROCHE
发明人： ENDERLE THILO , ROTH DORIS
IPC分类号： C12Q1/42 , C12Q1/48 , G01N33/542
摘要： Un método para detectar una actividad quinasa o actividad fosfatasa que comprende los pasos: a) incubar una muestra con actividad quinasa o fosfatasa con una molécula sustrato quinasa o fosfatasa que comprende un fluoróforo con un marcaje detectable, b) incubar la mezcla del paso a) con una entidad de detección que comprende un grupo aromático que se selecciona de entre el grupo que consiste en los aminoácidos triptófano, tirosina y fenilalanina, y una pareja de unión, en la que ambas molécula de sustrato fosforilado y la entidad de detección son capaces de unirse a la pareja de unión y la unión de la molécula sustrato y la entidad de detección a la pareja de unión conduce a una lectura alterada del fluoróforo, en el que la lectura alterada del fluoróforo se debe al bloqueo estático o dinámico que resulta de la interacción directa de orbitales moleculares del fluoróforo de la molécula sustrato y el grupo aromático de la entidad de detección, y c) medir el marcaje del fluoróforo en la mezcla del paso b), en el que una lectura alterada del fluoróforo en comparación con el blanco es indicativo de la presencia de una actividad quinasa o fosfatasa en la muestra.

6. 发明专利

CA2552986A1 GENERIC KINASE ASSAY 未知
公开(公告)号：CA2552986A1
公开(公告)日：2007-01-29
申请号：CA2552986
申请日：2006-07-20
申请人： HOFFMANN LA ROCHE
发明人： ENDERLE THILO , ROTH DORIS
IPC分类号： C12Q1/48 , C12Q1/42 , G01N33/573 , G01N33/58
摘要： The present invention relates to a method of determining kinase or phosphata se activity based on a three parts system. The method comprises contacting a binding partner which can bind phosphorylated peptides, a detection molecule and a substrate peptide. Determination of activities is achieved by measuring energy transfe r between an energy donor and an energy acceptor that are present on the detection molecu le and the substrate molecule.

7. 发明专利

ES2548902T3 Procedimiento para la identificación de moduladores de catecol O-metiltransferasa 未知
公开(公告)号：ES2548902T3
公开(公告)日：2015-10-21
申请号：ES11738203
申请日：2011-07-25
申请人： HOFFMANN LA ROCHE
发明人： ENDERLE THILO , ROTH DORIS
IPC分类号： G01N33/58 , C12Q1/48 , G01N33/542 , G01N33/573
摘要： Un procedimiento para la identificación de un modulador de la actividad de la enzima catecol Ometiltransferasa (COMT) que comprende las etapas de: a) proporcionar 4-nitrocatecol ligado covalentemente con Alexa Fluor 488 que tiene la fórmula I, b) poner en contacto la molécula de la etapa a) con una enzima catecol O-metiltransferasa (COMT), Sadenosilmetionina (SAM) y un compuesto candidato y c) medir la lectura de fluorescencia de la mezcla de la etapa b), en el que una lectura de fluorescencia alterada en presencia del compuesto candidato en comparación con un blanco es indicativa de un modulador de enzima catecol O-metiltransferasa (COMT).**Fórmula**

8. 发明专利

CA2698926C GENERIC KINASE/PHOSPHATASE ASSAY WITH SINGLE READOUT 未知
公开(公告)号：CA2698926C
公开(公告)日：2012-08-14
申请号：CA2698926
申请日：2008-09-01
申请人： HOFFMANN LA ROCHE
发明人： ENDERLE THILO , ROTH DORIS
IPC分类号： C12Q1/42 , C12Q1/48 , G01N33/542
摘要： The present invention relates to a generic method for detecting a kinase or phosphatase activity. The method comprises the following steps: incubating a kinase or phosphatase activity sample with a kinase or phosphatase substrate molecule comprising either a fluorophore having a detectable readout or molecule with an aromatic group which serves as a quencher of the fluorophore, incubating the mixture of step a) with a detection entity comprising either a fluorophore or a molecule with an aromatic group and a binding partner, wherein the substrate molecule and the detection entity are capable of binding to the binding partner and the binding of the substrate molecule and the detection entity to the binding partner lead to an altered readout of the fluorophore, and measuring the readout of the fluorophore in the mixture of step b), wherein an altered readout of the fluorophore compared to a blank is indicative for the presence of a kinase or phosphatase activity in the sample.

9. 发明专利

CA2698926A1 GENERIC KINASE/PHOSPHATASE ASSAY WITH SINGLE READOUT 未知
公开(公告)号：CA2698926A1
公开(公告)日：2009-03-19
申请号：CA2698926
申请日：2008-09-01
申请人： HOFFMANN LA ROCHE
发明人： ENDERLE THILO , ROTH DORIS
IPC分类号： C12Q1/42 , C12Q1/48 , G01N33/542
摘要： The present invention relates to a generic method for detecting a kinase or phosphatase activity. The method comprises the following steps: incubating a kinase or phosphatase activity sample with a kinase or phosphatase substrate molecule comprising either a fluorophore having a detectable readout or molecule with an aromatic group which serves as a quencher of the fluorophore, incubating the mixture of step a) with a detection entity comprising either a fluorophore or a molecule with an aromatic group and a binding partner, wherein the substrate molecule and the detection entity are capable of binding to the binding partner and the binding of the substrate molecule and the detection entity to the binding partner lead to an altered readout of the fluorophore, and measuring the readout of the fluorophore in the mixture of step b), wherein an altered readout of the fluorophore compared to a blank is indicative for the presence of a kinase or phosphatase activity in the sample.

10. 发明专利

AT405673T 未知
公开(公告)号：AT405673T
公开(公告)日：2008-09-15
申请号：AT06117450
申请日：2006-07-19
申请人： HOFFMANN LA ROCHE
发明人： ENDERLE THILO , ROTH DORIS
IPC分类号： C12Q1/48 , C12Q1/42 , G01N33/542
摘要： The present invention relates to a method of determining kinase or phosphatase activity based on a three parts system. The method comprises contacting a binding partner which can bind phosphorylated peptides, a detection molecule and a substrate peptide. Determination of activities is achieved by measuring energy transfer between an energy donor and an energy acceptor that are present on the detection molecule and the substrate molecule.

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