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1. 发明申请

WO2008153881A1 NOVEL CELL-BASED ASSAYS FOR INDENTIFYING ENHANCERS OR INHIBITORS OF T1R TASTE RECEPTORS (T1R2/T1R3 SWEET) AND UMAMI (T1R1/T1R3 UMAMI) TASTE RECEPTORS 审中-公开
标题翻译：用于补充T1R TASTE受体（T1R2 / T1R3 SWEET）和UMAMI（T1R1 / T1R3 UMAMI）药物受体的增强剂或抑制剂的新基于细胞的测定
公开(公告)号：WO2008153881A1
公开(公告)日：2008-12-18
申请号：PCT/US2008/007035
申请日：2008-06-04
申请人： SENOMYX, INC. , SERVANT, Guy , KAMDAR, Poonit , RIVADENEYRA, Adam
发明人： SERVANT, Guy , KAMDAR, Poonit , RIVADENEYRA, Adam
IPC分类号： A61K39/395
CPC分类号： G01N33/5008 , G01N2333/726
摘要： Improved assays for identifying modulators of sweet (TIR2/TIR3) and umami (TIRI/TIR3) taste receptors are disclosed These receptors may be the endogenous TIRs or may be functional variants such as chimeric taste receptors from the extracellular portion of one TIR or a variant or fragment thereof, and the transmembrane portion of another TIR or a variant or fragment thereof, preferably associated with a TIR3 polypeptide and a suitable G protein. The assays preferably use endogenous taste or gastrointestinal cells from mammalian cells or Xenopus oocytes which express TIR taste receptors or recombinant cell which express such TIRs. The modulators identified according to the assays are useful as taste modulators (which is confirmed in taste tests) and/or as therapeutics for treating conditions such as diabetes, obesity weight control, fat metabolism, glucose metabolism, insulin metabolism, satiety and/or the release of satiety peptides such as GLP-1.
摘要翻译：公开了用于鉴定甜味（TIR2 / TIR3）和鲜味（TIRI / TIR3）味觉感受器的调节剂的改进的测定法。这些受体可以是内源性TIR，或者可以是功能性变体，例如来自一个TIR或变体的胞外部分的嵌合味觉受体或其片段，以及另一TIR或其变体或片段的跨膜部分，优选与TIR3多肽和合适的G蛋白相关联。测定优选使用表达TIR味觉受体的哺乳动物细胞或非洲爪蟾卵母细胞的内源性味道或胃肠细胞或表达这种TIR的重组细胞。根据测定法鉴定的调节剂可用作味觉调节剂（其在味觉测试中被证实）和/或用作治疗诸如糖尿病，肥胖体重控制，脂肪代谢，葡萄糖代谢，胰岛素代谢，饱腹感和/或释放饱和肽如GLP-1。

2. 发明申请

WO2007047985A3 TRPM5 BASED ASSAYS AND THE USE THEREOF FOR THE IDENTIFICATION OF MODULATORS OF SWEET, BITTER OR UMAMI (SAVORY) TASTE 审中-公开
公开(公告)号：WO2007047985A3
公开(公告)日：2007-04-26
申请号：PCT/US2006/041152
申请日：2006-10-19
申请人： SENOMYX, INC. , SERVANT, Guy , WILLIAMS, Mark , PATRON, Andrew , KAMDAR, Poonit , CHEN, Qing , MOYER, Bryan , DAHAN, David , DITSCHUN, Tanya , RAY, Sumita , LIGANI, Amy , PATRON, Andrew, P.
发明人： SERVANT, Guy , WILLIAMS, Mark , PATRON, Andrew , KAMDAR, Poonit , CHEN, Qing , MOYER, Bryan , DAHAN, David , DITSCHUN, Tanya , RAY, Sumita , LIGANI, Amy , PATRON, Andrew, P.
IPC分类号： G01N33/566 , C07K14/705
摘要： Robust cell based assays are provided that use cells that express wild-type or modified TRPM5 nucleic acid sequences in order to identify putative taste modulators, preferably sweet, bitter and umami taste modulators. The preferred assays use HEK-293 cells that express TRPM5, optionally at least one GPCR, preferably a taste specific GPCR, and a G protein that couples therewith. These assays detect TRPM5 modulators by use of membrane potential dyes that emit fluorescence on changes in TRPM5 activity based on changes in membrane potential and these changes in fluorescence are detectable using Fluorimetric Imaging Plate Readers (FLIPR).

3. 发明申请

WO2007047127A2 OPTIMIZED TRPM8 NUCLEIC ACID SEQUENCES AND THEIR USE IN CELL BASED ASSAYS AND TEST KITS TO IDENTIFY TRPM8 MODULATORS 审中-公开
标题翻译：优化的TRPM8核酸序列及其在基于细胞的测定中的用途以及鉴定TRPM8调节剂的测试工具
公开(公告)号：WO2007047127A2
公开(公告)日：2007-04-26
申请号：PCT/US2006/038962
申请日：2006-10-04
申请人： SENOMYX, INC. , SERVANT, Guy , BRUST, Paul , MOYER, Bryan , LU, Min , ECHEVERRI, Fernando , DAHAN, David , ZOLLER, Mark , WILLIAMS, Mark , KIMMICH, Rachel , KAMDAR, Poonit , DITSCHUN, Tanya , PATRON, Andrew
发明人： SERVANT, Guy , BRUST, Paul , MOYER, Bryan , LU, Min , ECHEVERRI, Fernando , DAHAN, David , ZOLLER, Mark , WILLIAMS, Mark , KIMMICH, Rachel , KAMDAR, Poonit , DITSCHUN, Tanya , PATRON, Andrew
IPC分类号： E01C3/06
CPC分类号： C07K14/705
摘要： Modified human TRPM8 nucleic acid sequences which are efficiently expressed in human cells and cell-based assays and test kits containing same are provided. These assays identify TRPM8 modulators using cells that express a modified human TRPM8 nucleic acid sequence according to the invention, wherein said sequence has been modified relative to a wild-type human TRPM8 nucleic acid sequence in order to optimize ion channel expression in desired cells. Assays using these modified TRPM8 sequences have been shown to identify compounds that modulate the human TRPM8 ion channel better or comparably to known coolants such as menthol and icilin.
摘要翻译：提供了在人细胞中有效表达的修饰的人TRPM8核酸序列和基于细胞的测定法和含有其的测试试剂盒。这些测定使用表达根据本发明的修饰的人TRPM8核酸序列的细胞鉴定TRPM8调节剂，其中相对于野生型人TRPM8核酸序列已经修饰了所述序列，以便优化所需细胞中的离子通道表达。已经显示使用这些修饰的TRPM8序列的测定来鉴定与已知的冷却剂如薄荷醇和icilin更好或相当地调节人类TRPM8离子通道的化合物。

4. 发明申请

WO2011123693A1 SWEET FLAVOR MODIFIER 审中-公开
标题翻译：甜味调味剂
公开(公告)号：WO2011123693A1
公开(公告)日：2011-10-06
申请号：PCT/US2011/030802
申请日：2011-03-31
申请人： SENOMYX, INC. , TACHDJIAN, Catherine , TANG, Xiao-Qing , KARANEWSKY, Donald, S. , SERVANT, Guy , LI, Xiaodong , ZHANG, Feng , CHEN, Qing , ZHANG, Hong , DAVIS, Timothy , DARMOHUSODO, Vincent , WONG, Melissa , SELCHAU, Victor
发明人： TACHDJIAN, Catherine , TANG, Xiao-Qing , KARANEWSKY, Donald, S. , SERVANT, Guy , LI, Xiaodong , ZHANG, Feng , CHEN, Qing , ZHANG, Hong , DAVIS, Timothy , DARMOHUSODO, Vincent , WONG, Melissa , SELCHAU, Victor
IPC分类号： A01N43/42 , A61K31/47
CPC分类号： C07D495/04 , A23L2/56 , A23L27/2054 , A23L27/88 , A23V2002/00 , A61K47/22 , C07D215/54 , C07D215/60 , C07D401/12 , C07D405/12 , C07D471/04 , C07D491/048
摘要： The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.
摘要翻译：本发明包括具有结构式（I）的化合物或其药学上可接受的盐，溶剂化物和/或酯。这些化合物可用作甜味调味剂。本发明还包括包含本发明化合物的组合物和增强可摄入组合物的甜味的方法。此外，本发明提供了制备化合物的方法。

5. 发明申请

WO2008154221A2 MODULATION OF CHEMOSENSORY RECEPTORS AND LIGANDS ASSOCIATED THEREWITH 审中-公开
标题翻译：化学感受器的调节和与之相关的配体
公开(公告)号：WO2008154221A2
公开(公告)日：2008-12-18
申请号：PCT/US2008/065650
申请日：2008-06-03
申请人： SENOMYX, INC. , TACHDJIAN, Catherine , KARANEWSKY, Donald S. , TANG, Xiao-qing , LI, Xiaodong , ZHANG, Feng , SERVANT, Guy , CHEN, Qing , DARMOHUSODO, Vincent , FINE, Richard , FOTSING, Joseph R. , HAMMAKER, Jeffrey Robert , KANG, Xinshan , KIMMICH, Rachel, D.A. , KLEBANSKY, Boris , LIU, Haitian , PETROVIC, Goran , RINNOVA, Marketa , ADAMSKI-WERNER, Sara , YAMAMOTO, Jeffrey , ZHANG, Hong , ZLOTNIK, Albert , ZOLLER, Mark
发明人： TACHDJIAN, Catherine , KARANEWSKY, Donald S. , TANG, Xiao-qing , LI, Xiaodong , ZHANG, Feng , SERVANT, Guy , CHEN, Qing , DARMOHUSODO, Vincent , FINE, Richard , FOTSING, Joseph R. , HAMMAKER, Jeffrey Robert , KANG, Xinshan , KIMMICH, Rachel, D.A. , KLEBANSKY, Boris , LIU, Haitian , PETROVIC, Goran , RINNOVA, Marketa , ADAMSKI-WERNER, Sara , YAMAMOTO, Jeffrey , ZHANG, Hong , ZLOTNIK, Albert , ZOLLER, Mark
IPC分类号： A61K31/495 , A61K31/517 , A61K31/519 , A61P27/00 , C07D487/00 , C12N5/06 , G01N33/53
CPC分类号： C07D513/04 , A23L2/39 , A23L2/60 , A23L27/30 , A23L27/31 , A23L27/33 , A23L27/34 , A23L27/88 , C07D215/42 , C07D215/54 , C07D215/56 , C07D239/70 , C07D239/84 , C07D239/94 , C07D239/95 , C07D285/16 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/056 , C07D493/04 , C07D495/04 , C07D495/14 , C07D513/20 , G01N33/566
摘要： The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
摘要翻译：本发明包括用于鉴定化学感受器及其配体的调节剂的方法，例如通过确定测试实体是否适合与化学感应受体的金星蝇捕获区域内的一个或多个相互作用位点相互作用，以及能够调节化学感应受体及其配体。本发明还包括具有式（I），其亚属和特定化合物的化学感应受体及其配体的改性剂。此外，本发明包括含有化学感应受体调节剂及其配体的可摄入组合物，以及使用化学感应受体及其配体改性剂增强可摄入组合物的甜味或治疗与化学感觉受体相关的病症的方法。此外，本发明包括制备化学感受器及其配体的改性剂的方法。

6. 发明申请

WO2005014848A2 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：改进的电生理测定使用表达人类健康的化学物质和使用PHENAMIL来改善ENCC增强剂对使用膜潜在报告染料的测定的影响
公开(公告)号：WO2005014848A2
公开(公告)日：2005-02-17
申请号：PCT/US2004/021853
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： C12Q
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，本发明涉及用于从人肾c-DNA文库克隆的人上皮钠通道（hENaC）的分析和筛选的基于哺乳动物细胞的高通量测定，并且还在包括人类味道的其它组织中表达组织。本发明还涉及用于鉴定人类ENaC调节剂，优选ENaC增强子的两栖动物基于卵母细胞的中等通量电生理测定法。在基于细胞的ENaC测定中调节ENaC功能的化合物预期会影响人类的咸味。本文所述的测定法优于现有的细胞表达系统。在哺乳动物细胞的情况下，这种测定可以在高通量模式的标准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，如苯胺，可以实现增强的测定结果。在本发明的卵母细胞电生理测定（双电极电压钳技术）的情况下，这些测定有助于鉴定特异性调节人类ENaC的化合物。本发明的测定提供了可用于检测促进（增强）或抑制hENaC功能的化合物的强壮屏幕。增强或阻断人类ENaC通道活性的化合物应该调节人体的咸味。

7. 发明申请

WO2003004611A3 HUMAN OLFACTORY NUCLEOTIDE-GATED ION CHANNELS 审中-公开
公开(公告)号：WO2003004611A3
公开(公告)日：2003-01-16
申请号：PCT/US2002/021184
申请日：2002-07-08
申请人： SENOMYX, INC. , ZOLLER, Mark, T. , XU, Hong , STASZEWSKI, Lena , MOYER, Bryan , PRONIN, Alexy , ADLER, Jon, Elliott , SERVANT, Guy , CALLAMARAS, Nicholas
发明人： ZOLLER, Mark, T. , XU, Hong , STASZEWSKI, Lena , MOYER, Bryan , PRONIN, Alexy , ADLER, Jon, Elliott , SERVANT, Guy , CALLAMARAS, Nicholas
IPC分类号： C07K14/705
摘要： The present invention relates to isolated nucleic acid sequences that encode human olfactory cyclic nucleotide gated (CNG) channel subunits, and the corresponding polypeptides. The invention further relates to the use of human CNG channels to profile, screen for, and identify compounds that modulate the human olfactory CNG channel. More specifically, the invention relates to the expression of the human olfactory CNG channel in cells, preferably mammalian cells, and the use of these cells in high throughput cell-based assays to identify compounds that enhance or block human olfactory CNG function. Compounds that activate the olfactory CNG channel will enhance smell and can be used to make foods more palatable for individuals with attenuated olfactory function. Conversely, compounds that inhibit the olfactory CNG channel will inhibit smell and can be use to block malodors. Additionally, the invention relates to the use of cell-based olfactory CNG channel assays to identify modulates of G-protein coupled receptor (GPCRs) and other proteins that regulate cyclic nucleotide levels.

8. 发明申请

WO2010065863A2 ASSAYS FOR IDENTIFYING GENES ENCODING SALTY TASTE RECEPTORS AND MODULATORS 审中-公开
标题翻译：用于鉴定编码盐味受体和调节剂的基因的测定
公开(公告)号：WO2010065863A2
公开(公告)日：2010-06-10
申请号：PCT/US2009/066788
申请日：2009-12-04
申请人： SENOMYX, INC. , MOYER, Bryan , ZLOTNIK, Albert , HEVEZI, Peter , SOTO, Hortensia , LU, Min , GAO, Na , SAGANICH, Michael , DAHAN, Michael , LAITA, Bianca , SERVANT, Guy , BRUST, Paul , WILLIAMS, Mark
发明人： MOYER, Bryan , ZLOTNIK, Albert , HEVEZI, Peter , SOTO, Hortensia , LU, Min , GAO, Na , SAGANICH, Michael , DAHAN, Michael , LAITA, Bianca , SERVANT, Guy , BRUST, Paul , WILLIAMS, Mark
IPC分类号： A01K67/00 , C12Q1/68 , C12Q1/02 , C12N5/10 , C12N1/00
CPC分类号： G01N33/5008 , A01K2267/03 , C07K14/705 , G01N2333/705
摘要： The present invention relates to rationales for selecting salty taste receptors from a discrete set of taste specific genes disclosed infra by use of methods including electrophysiology, bioiirformatics, and quantitative gene expression assays using transgenic animals as well as functional assays wherein these salty taste receptors may be expressed alone or in association with other taste specific polypeptides such as TRPML3, PKD2L1 or GPRl 13. In addition the invention relates to the use of the identified salty taste receptors in assays, preferably high- throughput, in order to identify modulators which maybe used as flavor additives to modulate salty taste. Preferably, the invention provides high- throughput mammalian and medium- throughput oocyte- based electrophysiological assays for identifying human TRPML3 modulators, preferably TRPML3 enhancers. Compounds that modulate TRPML3 function in the assay are expected to affect salty taste in humans. The inventive electrophysiological assays, such as the two-electrode voltage-clamp technique, facilitate the identification of compounds which specifically modulate human TRPML3. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit TRPML3 function. Compounds that enhance or block TRPML3 channel activity should thereby modulate salty taste. In addition, these compounds maybe used to regulate sodium excretion, urinary output and other biological functions relating to sodium levels. This invention relates to the elucidation that TRPML3 is involved in salty taste perception in primates including humans and likely other mammals (given the significance of sodium and other ions to physiological functions and conditions this phenotype is likely strongly conserved in different animals). The TRPML3 gene also modulates one or more of sodium metabolism, sodium excretion, blood pressure, fluid retention, cardiac function and urinary functions such as urine production and excretion.
摘要翻译：本发明涉及通过使用包括电生理学，生物信息学和使用转基因动物的定量基因表达测定法的方法从下文公开的一组离体味觉特异性基因中选择咸味受体的基本原理以及功能其中这些咸味受体可以单独表达或与其他味道特异性多肽例如TRPML3，PKD2L1或GPR113结合表达。另外，本发明涉及鉴定的咸味受体在测定中的用途，优选高通量为了鉴定可能用作香料添加剂来调节咸味的调节剂。优选地，本发明提供了用于鉴定人TRPML3调节剂，优选TRPML3增强子的高通量哺乳动物和中等通量的基于卵母细胞的电生理学测定法。期望在测定中调节TRPML3功能的化合物影响人类的咸味。本发明的电生理学测定法，例如双电极电压钳技术有助于鉴定特异性调节人TRPML3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TRPML3功能的化合物的有力筛选。因此增强或阻断TRPML3通道活性的化合物应调节咸味。此外，这些化合物可用于调节钠排泄，尿量和与钠水平有关的其他生物学功能。本发明涉及说明TRPML3参与包括人类和可能的其他哺乳动物（考虑到钠和其它离子对生理功能和条件的重要性，这种表型在不同动物中强烈保守）的灵长类中的咸味感知。 TRPML3基因还调节钠代谢，钠排泄，血压，体液潴留，心脏功能和泌尿功能如尿液产生和排泄中的一种或多种。

9. 发明申请

WO2009025793A2 IDENTIFICATION OF HUMAN T2R RECEPTORS THAT RESPOND TO BITTER COMPOUNDS THAT ELICIT THE BITTER TASTE IN COMPOSITIONS, AND THE USE THEREOF IN ASSAYS TO IDENTIFY COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITIONS AND USE THEREOF 审中-公开
标题翻译：识别符合组合物中双歧杆菌组合物的双特异度化合物的人类T2R受体，以及其在测定中的用途，以鉴定组合物中的禁止（块状）双歧杆菌组合物及其用途的化合物
公开(公告)号：WO2009025793A2
公开(公告)日：2009-02-26
申请号：PCT/US2008/009864
申请日：2008-08-19
申请人： SENOMYX, INC. , LI, Xiaodong , PATRON, Andrew , TACHDJIAN, Catherine , XU, Hong , LI, Qing , PRONIN, Alexey , SERVANT, Guy , ZHANG, Lan , BRADY, Thomas , DARMOHUSODO, Vincent , ARELLANO, Melissa , SELCHAU, Victor , CHING, Brett Weylan , KARANEWSKY, Donald S. , BRUST, Paul , LING, Jing , ZHAO, Wen , PRIEST, Chad
发明人： LI, Xiaodong , PATRON, Andrew , TACHDJIAN, Catherine , XU, Hong , LI, Qing , PRONIN, Alexey , SERVANT, Guy , ZHANG, Lan , BRADY, Thomas , DARMOHUSODO, Vincent , ARELLANO, Melissa , SELCHAU, Victor , CHING, Brett Weylan , KARANEWSKY, Donald S. , BRUST, Paul , LING, Jing , ZHAO, Wen , PRIEST, Chad
IPC分类号： C12Q1/68
CPC分类号： C07C311/17 , A23L27/86 , A61K8/46 , A61K8/466 , A61K8/4933 , A61K8/494 , A61K8/4973 , A61K8/498 , A61K8/4986 , A61K31/135 , A61K31/4439 , A61K31/485 , A61K31/60 , A61K31/704 , A61K45/06 , A61Q11/00 , C07C233/73 , C07C311/04 , C07C311/13 , C07C311/16 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07C311/46 , C07C323/49 , C07C335/16 , C07C335/18 , C07D213/42 , C07D213/71 , C07D217/08 , C07D223/18 , C07D307/14 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/34 , A61K2300/00
摘要： The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
摘要翻译：本发明涉及T2R味觉受体家族中的特定人味受体对存在于例如咖啡中的特定苦味化合物的反应的发现。此外，本发明涉及含有作为苦味抑制剂的特定化合物和组合物的发现，以及其作为例如咖啡和咖啡风味食品，饮料和药物中的苦味抑制剂或风味调节剂的用途。此外，本发明涉及一种拮抗多种不同人类T2R的化合物的发现及其在测定中的用途以及用于摄取人类和动物的组合物中的苦味阻滞剂。

10. 发明申请

WO2004069191A2 FUNCTIONAL COUPLING OF T1RS AND T2RS BY GI PROTEINS, AND CELL-BASED ASSAYS FOR THE IDENTIFICATION OF T1R AND T2R MODULATORS 审中-公开
标题翻译：通过GI蛋白的T1RS和T2RS的功能性联合，以及用于鉴定T1R和T2R调节剂的基于细胞的测定
公开(公告)号：WO2004069191A2
公开(公告)日：2004-08-19
申请号：PCT/US2004/002987
申请日：2004-02-03
申请人： SENOMYX INC. , SERVANT, Guy , OZECK, Mark , BRUST, Paul , XU, Hong
发明人： SERVANT, Guy , OZECK, Mark , BRUST, Paul , XU, Hong
IPC分类号： A61K
CPC分类号： G01N33/5041 , G01N33/5008 , G01N33/566 , G01N2333/726 , G01N2500/10
摘要： The invention resides in part in the discovery that G proteins other than Gα 15 couples to T1R and T2R taste receptors, particularly G i proteins such as G αi . Related to this discovery, the invention provides cell-based assay methods for identifying compounds that modulate the activity of specific T1R or T2R taste receptors or which modulate the effect of other T1R or T2R modulators on T1R or T2R activity. These assay methods preferably detect the effect of a putative T1R or T2R modulator compound on MAPK activation, cAMP accumulation, or adenylyl cyclase activity or another signaling pathway regulated by G i proteins. The level of MAPK activation, cAMP accumulation or adenylyl cyclase is preferably determined by immunoassay methods that use ligands (monoclonal or polyclonal antibodies) that specifically bind an activated (phosphorylated) MAPK, cAMP, or adenylyl cyclase.
摘要翻译：本发明部分在于发现除了Galpha15之外的G蛋白与T1R和T2R味觉受体特别是Gi蛋白如Galphai偶联。与这一发现有关，本发明提供基于细胞的测定方法，用于鉴定调节特异性T1R或T2R味觉受体的活性或调节其他T1R或T2R调节剂对T1R或T2R活性的影响的化合物。这些测定方法优选检测推定的T1R或T2R调节剂化合物对MAPK激活，cAMP积聚或腺苷酸环化酶活性或由Gi蛋白调节的另一信号传导途径的影响。 MAPK活化水平，cAMP积聚或腺苷酸环化酶优选通过使用特异性结合活化（磷酸化）MAPK，cAMP或腺苷酸环化酶的配体（单克隆或多克隆抗体）的免疫测定方法来确定。

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