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1. 发明申请

WO2005014848A3 IMPROVED ELECTROPHYSIOLOGICAL ASSAYS USING OOCYTES THAT EXPRESS HUMAN ENaC AND THE USE OF PHENAMIL TO IMPROVE THE EFFECT OF ENaC ENHANCERS IN ASSAYS USING MEMBRANE POTENTIAL REPORTING DYES 审中-公开
标题翻译：采用膜表达人类表达和使用苯胺类改善ENaC增强剂在测定中使用膜电位报告染料的效果的改进的电生理学测定
公开(公告)号：WO2005014848A3
公开(公告)日：2005-05-06
申请号：PCT/US2004021853
申请日：2004-07-09
申请人： SENOMYX INC , SERVANT GUY , CHANG HONG , REDCROW CYRIL , RAY SUMITA , CLARK IMRAN
发明人： SERVANT GUY , CHANG HONG , REDCROW CYRIL , RAY SUMITA , CLARK IMRAN
IPC分类号： C07H21/04 , C07K1/00 , C12N1/20 , C12P21/06 , C12Q20060101 , G01N33/50 , G01N33/53 , G01N33/566 , G01N33/567 , G01N33/68
CPC分类号： C12Q1/025 , C12N15/85 , C12N2320/10 , C12N2503/02 , G01N33/5044 , G01N33/6872 , G01N2500/10
摘要： In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should thereby modulate salty taste in humans.
摘要翻译：一方面，本发明涉及用于分析和筛选从人肾c-DNA文库克隆的人上皮钠通道（hENaC）的基于哺乳动物细胞的高通量测定法，并且还在包括人味觉的其他组织中表达组织。本发明进一步涉及用于鉴定人ENaC调节剂，优选ENaC增强子的基于两栖动物卵母细胞的中等通量电生理测定。预期在基于细胞的ENaC测定中调节ENaC功能的化合物会影响人类的咸味。本文所述的测定相对于现有的细胞表达系统具有优势。在哺乳动物细胞的情况下，这种测定可以在高通量模式下在标准96或384孔培养板中进行，通过使用抑制ENaC功能的化合物，优选阿米洛利衍生物如Phenamil实现增强的测定结果。在本发明的卵母细胞电生理学测定法（双电极电压钳技术）的情况下，这些测定法有助于鉴定特异性调节人ENaC的化合物。本发明的测定法提供了用于检测促进（增强）或抑制hENaC功能的化合物的强力筛选。因此增强或阻断人类ENaC通道活性的化合物应该调节人类的咸味。

2. 发明专利

BRPI0412471A 未知
公开(公告)号：BRPI0412471A
公开(公告)日：2006-09-19
申请号：BRPI0412471
申请日：2004-07-09
申请人： SENOMYX INC
发明人： SEVANT GUY , CHANG HONG , REDCROW CYRIL , SUMITA RAY , CLARK IMRAN
IPC分类号： C07H21/04 , C07K1/00 , C12N1/20 , C12P21/06 , C12Q20060101 , G01N33/50 , G01N33/53 , G01N33/566 , G01N33/567 , G01N33/68
摘要： In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should thereby-modulate salty taste in humans.

3. 发明专利

NO20060078L 未知
公开(公告)号：NO20060078L
公开(公告)日：2006-04-07
申请号：NO20060078
申请日：2006-01-05
申请人： SENOMYX INC
发明人： SERVANT GUY , CHANG HONG , REDCROW CYRIL , SUMITA RAY , CLARK IMRAN
IPC分类号： G01N33/48 , C07H21/04 , C07K1/00 , C12N1/20 , C12P21/06 , C12Q20060101 , G01N33/50 , G01N33/53 , G01N33/566 , G01N33/567 , G01N33/68
摘要： In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should thereby-modulate salty taste in humans.

4. 发明专利

AU2004263845A1 Improved electrophysiological assays using oocytes that express human ENaC and the use of phenamil to improve the effect of ENaC enhancers in assays using membrane potential reporting dyes 未知
公开(公告)号：AU2004263845A1
公开(公告)日：2005-02-17
申请号：AU2004263845
申请日：2004-07-09
申请人： SENOMYX INC
发明人： RAY SUMITA , CLARK IMRAN , CHANG HONG , REDCROW CYRIL , SERVANT GUY
IPC分类号： G01N33/566 , C07H21/04 , C07K1/00 , C12N1/20 , C12P21/06 , C12Q20060101 , G01N33/50 , G01N33/53 , G01N33/567 , G01N33/68
摘要： In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should thereby-modulate salty taste in humans.

5. 发明专利

MXPA06000266A ENSAYOS ELECTROFISIOLOGICOS MEJORADOS UTILIZANDO OOCITOS QUE EXPRESAN UN ENAC HUMANO Y EL USO DE FENAMILO PARA MEJORAR EL EFECTO DE INTENSIFICADORES DEL ENAC EN ENSAYOS. 未知
公开(公告)号：MXPA06000266A
公开(公告)日：2006-03-30
申请号：MXPA06000266
申请日：2004-07-09
申请人： SENOMYX INC
发明人： CLARK IMRAN
IPC分类号： C07H21/04 , C07K1/00 , C12N1/20 , C12P21/06 , C12Q20060101 , G01N33/50 , G01N33/53 , G01N33/566 , G01N33/567 , G01N33/68 , C12Q00/00
摘要： En un aspecto, la presente invencion se refiere a un ensayo de alto rendimiento basado en celulas de mamifero para el perfilado y seleccion de un canal de sodio epitelial humano (hENaC) clonado de una biblioteca de ADNc de rinon humano y tambien es expresado en otros tejidos que incluyen el tejido gustativo humano. La presente invencion se refiere ademas a ensayos electrofisiologicos de rendimiento intermedio basados en oocitos de anfibio para identificar moduladores del ENaC humano, preferiblemente intensificadores del ENaC. Se espera que los compuestos que modulan la funcion del ENaC en un ensayo de ENaC basado en celulas afecten el sabor salado en humanos. Los ensayos descritos en este documento tienen ventajas sobre los sistemas de expresion celulares existentes. En el caso de celulas de mamifero, estos ensayos pueden conducirse en placas de cultivo de 96 a 384 pocillos estandar en un modo de alto rendimiento con resultados de ensayo mejorados que son logrados mediante el uso de un compuesto que inhibe la funcion del ENaC, preferiblemente un derivado de amilorida tal como fenamilo. En el caso de los ensayos electrofisiologicos de oocitos inventivos (tecnica de fijacion de voltaje de dos electrodos), estos ensayos facilitan la identificacion de compuestos que modulan especificamente un ENaC humano. Los ensayos de la invencion proporcionan una seleccion robusta que es util para detectar compuestos que facilitan (intensifican) o inhiben la funcion del ENaC. Los compuestos que intensifican o bloquean la actividad del canal ENaC humano deben modular con lo cual el sabor salado en humanos.

6. 发明专利

NO20060078A 未知
公开(公告)号：NO20060078A
公开(公告)日：2006-04-07
申请号：NO20060078
申请日：2006-01-05
申请人： SENOMYX INC
发明人： SERVANT GUY , CHANG HONG , REDCROW CYRIL , SUMITA RAY , CLARK IMRAN
IPC分类号： G01N33/48 , C07H21/04 , C07K1/00 , C12N1/20 , C12P21/06 , C12Q20060101 , G01N33/50 , G01N33/53 , G01N33/566 , G01N33/567 , G01N33/68
CPC分类号： C12Q1/025 , C12N15/85 , C12N2320/10 , C12N2503/02 , G01N33/5044 , G01N33/6872 , G01N2500/10
摘要： In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should thereby modulate salty taste in humans.

7. 发明专利

CA2530497A1 IMPROVED ELECTROPHYSIOLOGICAL ASSAYS USING OOCYTES THAT EXPRESS HUMAN ENAC AND THE USE OF PHENAMIL TO IMPROVE THE EFFECT OF ENAC ENHANCERS IN ASSAYS USING MEMBRANE POTENTIAL REPORTING DYES 未知
公开(公告)号：CA2530497A1
公开(公告)日：2005-02-17
申请号：CA2530497
申请日：2004-07-09
申请人： SENOMYX INC
发明人： CHANG HONG , SUMITA RAY , REDCROW CYRIL , CLARK IMRAN , SERVANT GUY
IPC分类号： G01N33/566 , C07H21/04 , C07K1/00 , C12N1/20 , C12P21/06 , C12Q20060101 , G01N33/50 , G01N33/53 , G01N33/567 , G01N33/68
摘要： In one aspect, the present invention relates to a mammalian cell-based high- throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also express ed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expecte d to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high- throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative suc h as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assa ys of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should thereby modulate salty taste in humans.

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