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1. 发明授权

EP2293067B1 T1R hetero-oligomeric taste receptors and cell lines that express said receptors and use thereof for identification of taste compounds 有权
标题翻译：异源寡聚T1R味觉受体，并且这些受体表达细胞系及其对风味化合物的鉴定使用
公开(公告)号：EP2293067B1
公开(公告)日：2016-04-20
申请号：EP10180335.1
申请日：2002-06-26
申请人： Senomyx, Inc.
发明人： Zoller, Mark T. , Li, Xiaodong , Staszewski, Lena , O'Connell, Shawn , Zozulya, Sergey , Adler, Jon Elliot , Xu, Hong , Echeverri, Fernando
IPC分类号： G01N33/53 , G01N33/567 , C12P21/06 , C12N1/20 , C12N15/00 , C12N15/09 , C12N15/63 , C12N15/70 , C12N15/74 , A01N37/18 , A61K38/00
CPC分类号： C07K14/705 , A01K2217/00 , A01K2217/05 , G01N2333/726

2. 发明公开

EP2327985A3 T1R Hetero-oligomeric taste receptors and cell lines that express said receptors and use thereof for identification of taste compounds 有权转让
标题翻译：异源寡聚T1R味觉受体，并且这些受体表达细胞系及其对风味化合物的鉴定使用
公开(公告)号：EP2327985A3
公开(公告)日：2012-01-18
申请号：EP10180331.0
申请日：2002-06-26
申请人： Senomyx, Inc.
发明人： Zoller, Mark T. , Li, Xiaodong , Staszewski, Lena , O'Connell, Shawn , Zozulya, Sergey , Adler, Jon Elliot , Xu, Hong , Echeverri, Fernando
IPC分类号： G01N33/53 , G01N33/567 , C12P21/06 , C12N1/20 , C12N15/00 , C12N15/09 , C12N15/63 , C12N15/70 , C12N15/74 , A01N37/18 , A61K38/00
CPC分类号： C07K14/705 , A01K2217/00 , A01K2217/05 , G01N2333/726
摘要： The present invention relates to the discovery that the T1R receptors assemble to form functional taste receptors. Particularly, it has been discovered that co-expression of T1R1 and T1R3 results in a taste receptor that responds to umami taste stimuli, including monosodium glutamate. Also, it has been discovered that co-expression of the T1R2 and T1R3 receptors results in a taste receptor that responds to sweet taste stimuli including naturally occurring and artificial sweeteners. Also the present invention relates to the use of hetero-oligomeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging. Finally, the invention relates to the discovery that some compounds, e.g., lactisole, inhibit both the activities of human T1R2/T1R3 and T1R1/T1R3 receptors, and accordingly the sweet and umami taste, suggesting that these receptors may be the only sweet and umami receptors.

4. 发明公开

EP2327985A2 T1R Hetero-oligomeric taste receptors and cell lines that express said receptors and use thereof for identification of taste compounds 有权转让
标题翻译： T1R异源寡聚味觉受体和表达所述受体的细胞系及其用于鉴定味道化合物的用途
公开(公告)号：EP2327985A2
公开(公告)日：2011-06-01
申请号：EP10180331.0
申请日：2002-06-26
申请人： Senomyx, Inc.
发明人： Zoller, Mark T. , Li, Xiaodong , Staszewski, Lena , O'Connell, Shawn , Zozulya, Sergey , Adler, Jon Elliot , Xu, Hong , Echeverri, Fernando
IPC分类号： G01N33/53 , G01N33/567 , C12P21/06 , C12N1/20 , C12N15/00 , C12N15/09 , C12N15/63 , C12N15/70 , C12N15/74 , A01N37/18 , A61K38/00
CPC分类号： C07K14/705 , A01K2217/00 , A01K2217/05 , G01N2333/726
摘要： The present invention relates to the discovery that the T1R receptors assemble to form functional taste receptors. Particularly, it has been discovered that co-expression of T1R1 and T1R3 results in a taste receptor that responds to umami taste stimuli, including monosodium glutamate. Also, it has been discovered that co-expression of the T1R2 and T1R3 receptors results in a taste receptor that responds to sweet taste stimuli including naturally occurring and artificial sweeteners. Also the present invention relates to the use of hetero-oligomeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging. Finally, the invention relates to the discovery that some compounds, e.g., lactisole, inhibit both the activities of human T1R2/T1R3 and T1R1/T1R3 receptors, and accordingly the sweet and umami taste, suggesting that these receptors may be the only sweet and umami receptors.
摘要翻译：本发明涉及T1R受体组装形成功能性味觉受体的发现。特别是，已经发现T1R1和T1R3的共表达导致对鲜味刺激（包括谷氨酸一钠）有反应的味觉受体。而且，已经发现T1R2和T1R3受体的共表达导致对甜味刺激物（包括天然存在的和人造甜味剂）响应的味觉受体。本发明还涉及在测定中使用包含T1R1 / T1R3和T1R2 / T1R3的异源低聚味觉受体来鉴别分别对鲜味刺激和甜味刺激作出反应的化合物。此外，本发明涉及稳定或瞬时共表达T1R1和T1R3的组合的细胞系的组成; 或T1R2和T1R3; 在构成或诱导条件下。还提供了这些细胞系在基于细胞的分析中用于鉴别鲜味和甜味调节化合物，特别是通过使用荧光成像检测受体活性的高通量筛选分析。最后，本发明涉及发现一些化合物例如lactisole抑制人类T1R2 / T1R3和T1R1 / T1R3受体的活性，并因此抑制甜味和鲜味，表明这些受体可能是唯一的甜味和鲜味受体。

5. 发明公开

EP1985630A3 T1R taste receptors and genes encoding same 有权转让
标题翻译： T1R-Geschmacksrezeptoren unddafürkodierende Gene
公开(公告)号：EP1985630A3
公开(公告)日：2009-02-18
申请号：EP08153652.6
申请日：2002-01-03
申请人： Senomyx, Inc.
发明人： Adler, Jon, Elliott , Li, Xiaodong , Staszewski, Lena , O'Connell, Shawn , Zozulya, Sergey
IPC分类号： C07K14/705 , C12N15/12 , C12N15/62 , C07K16/18 , C12Q1/68 , C12N5/10 , G01N33/50
CPC分类号： C07K14/723 , C07K14/705 , C07K2319/00 , C12Q1/6883 , G01N33/5041 , G01N33/6872 , G01N33/74 , G01N2333/726 , G06F19/12
摘要： Newly identified mammalian taste-cell-specific G protein-coupled receptors, and the genes and cDNA encoding said receptors are described. Specifically, T1R G protein-coupled receptors active in taste signaling, and the genes and cDNA encoding the same, are described, along with methods for isolating such genes and for isolating and expressing such receptors. Methods for representing taste perception of a particular taste stimulus in a mammal are also described, as are methods for generating novel molecules or combinations of molecules that clicit a predetermined taste perception in a mammal, and methods for simulating one or more tastes. Further, methods for stimulating or blocking taste perception in a mammal are also disclosed.
摘要翻译：描述了新鉴定的哺乳动物味细胞特异性G蛋白偶联受体，以及编码所述受体的基因和cDNA。具体来说，描述了活跃于味觉信号传导中的T1R G蛋白偶联受体以及编码相同基因的cDNA以及用于分离这些基因并用于分离和表达此类受体的方法。还描述了用于表示哺乳动物中特定味觉刺激的味觉感觉的方法，以及用于产生新鲜分子或分泌哺乳动物预定味觉的分子组合的方法，以及用于模拟一种或多种口味的方法。此外，还公开了哺乳动物刺激或阻止味觉的方法。

6. 发明公开

EP2573559A1 Modulation of chemosensory receptors and ligands associated 有权
标题翻译：调制化学传感器Rezeptoren und damit verbundene Liganden
公开(公告)号：EP2573559A1
公开(公告)日：2013-03-27
申请号：EP12175764.5
申请日：2008-06-03
申请人： Senomyx, Inc.
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： G01N33/53 , C07D487/04 , C07D215/42 , C07D215/54 , C07D215/56 , C07D239/70 , C07D239/94 , C07D239/95 , C07D417/12 , C07D471/04 , C07D493/04 , C07D495/04 , C07D495/14 , C07D513/20
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 includes 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应受体及其配体的改性剂的方法，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结构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的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的改性剂以增强可摄取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应受体及其配体改性剂的方法。

7. 发明授权

EP2298802B1 T1R3 taste receptors domains and genes encoding the same 有权转让
标题翻译： T1R3味觉感受器域及其编码基因
公开(公告)号：EP2298802B1
公开(公告)日：2012-10-24
申请号：EP10180329.4
申请日：2001-03-07
申请人： Senomyx, Inc.
发明人： Alder, Jon Elliot , Zozulya, Sergey , O'Connell, Shawn M , Li, Xiaodong , Staszewski, Lena
IPC分类号： C07K14/705 , C12N15/12 , C12N15/62 , C07K16/18 , C12Q1/68 , C12N5/10 , G01N33/50
CPC分类号： C07K14/723 , C07K14/705 , C07K2319/00
摘要： Newly identified mammalian taste-cell-specific G protein-coupled receptors, and the genes and cDNA encoding said receptors are described. Specifically, T1R G protein-coupled receptors active in taste signaling, and the genes and cDNA encoding the same, are described, along with methods for isolating such genes and for isolating and expressing such receptors. Methods for representing taste perception of a particular tastant in a mammal are also described, as are methods for generating novel molecules or combinations of molecules that elicit a predetermined taste perception in a mammal, and methods for simulating one or more tastes. Further, methods for stimulating or blocking taste perception in a mammal arc also disclosed.

8. 发明授权

EP1944319B1 T1R1 Taste Receptors and Genes Encoding Same 有权转让
标题翻译： T1R1味觉感受器，而这些加密的基因
公开(公告)号：EP1944319B1
公开(公告)日：2010-01-27
申请号：EP08152887.9
申请日：2001-03-07
申请人： Senomyx, Inc.
发明人： Adler, Jon Elliot , Staszewski, Lena , Li, Xiaodong , O'Connell, Shawn M , Zozulya, Sergey
IPC分类号： C07K14/705 , C12N15/12 , C12N15/62 , C07K16/18 , C12Q1/68 , C12N5/10 , G01N33/50
CPC分类号： C07K14/723 , C07K14/705 , C07K2319/00
摘要： Newly identified mammalian taste-cell-specific G protein-coupled receptors, and the genes and cDNA encoding said receptors are described. Specifically, T1R G protein-coupled receptors active in taste signaling, and the genes and cDNA encoding the same, are described, along with methods for isolating such genes and for isolating and expressing such receptors. Methods for representing taste perception of a particular tastant in a mammal are also described, as are methods for generating novel molecules or combinations of molecules that elicit a predetermined taste perception in a mammal, and methods for simulating one or more tastes. Further, methods for stimulating or blocking taste perception in a mammal arc also disclosed.

10. 发明公开

EP2568287A2 Modulation of chemosensory receptors and ligands associated 审中-公开
标题翻译：调节化学感应受体和配体相关
公开(公告)号：EP2568287A2
公开(公告)日：2013-03-13
申请号：EP12175761.1
申请日：2008-06-03
申请人： Senomyx, Inc.
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： G01N33/53 , C07D487/04
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 includes 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应受体及其配体的修饰物的方法，例如通过确定测试实体是否适合于与化学感应受体的金星蝇domains结构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的修饰物和它们的配体。本发明还包括化学感应受体的修饰物及其具有式（I）的配体，其亚属和特定化合物。此外，本发明包括包含化学感应受体及其配体的调节剂的可摄取组合物以及使用化学感应受体及其配体的调节剂来增强可摄入组合物的甜味或治疗与化学感应受体相关的病症的方法。另外，本发明包括制备化学感应受体及其配体的修饰物的方法。

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