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1. 发明申请

WO2007047988A2 CHIMERIC HUMAN SWEET-UMAMI AND UMAMI-SWEET TASTE RECEPTORS 审中-公开
标题翻译： CHIMERIC人类SWEET-UMAMI和UMAMI-SWEET TASTE RECEPTORS
公开(公告)号：WO2007047988A2
公开(公告)日：2007-04-26
申请号：PCT/US2006/041158
申请日：2006-10-19
申请人： SENOMYX, INC. , LI, Xiaodong , ZHANG, Feng , XU, Hong , LI, Qing
发明人： LI, Xiaodong , ZHANG, Feng , XU, Hong , LI, Qing
IPC分类号： C07K14/705
CPC分类号： C07K14/705 , C12N2503/00 , C12N2510/00
摘要： This invention relates to chimeric taste receptors comprising the extracellular portion of one TlR or a variant or fragment thereof, either TlRl or T1R2, and the transmembrane portion of another TlR or a variant or fragment thereof, either TlRl or T1R2, preferably associated with a T1R3 polypeptide and a suitable G protein. These chimeric taste receptors and cells which express such chimeric taste receptors are useful in assays for identifying sweet and umami ligands as well in assays for identifying sweet and umami enhancers. Additionally, these chimeric taste receptors and cells which express same can be used to map and determine where specific sweet and umami ligands interact with their respective receptors and to elucidate the mechanism of receptor activation.
摘要翻译：本发明涉及包含一种TlR的细胞外部分或其变体或片段，即T1R1或T1R2的嵌合味觉感受器，以及T1R1或其变体或片段的跨膜部分，T1R1或T1R2，优选与T1R3相关多肽和合适的G蛋白。这些嵌合味觉受体和表达这种嵌合味觉受体的细胞可用于鉴定甜味和鲜味配体的测定以及用于鉴定甜味和鲜味增强剂的测定中。此外，这些嵌合味觉受体和表达相同的细胞可以用于绘制和确定特定甜味和鲜味配体与其各自受体相互作用的位置，并阐明受体活化的机制。

2. 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。

3. 发明申请

WO2008057470A2 IDENTIFICATION OF BITTER LIGANDS THAT SPECIFICALLY ACTIVATE HUMAN T2R RECEPTORS AND RELATED ASSAYS FOR IDENTIFYING HUMAN BITTER TASTE MODULATORS 审中-公开
标题翻译：识别特异性激活人类T2R受体的苦味物配体和鉴定人类苦味调节剂的相关测定
公开(公告)号：WO2008057470A2
公开(公告)日：2008-05-15
申请号：PCT/US2007/023230
申请日：2007-11-01
申请人： SENOMYX, INC. , LI, Xiaodong , XU, Hong , LI, Qing , TANG, Huixian , PRONIN, Alexey
发明人： LI, Xiaodong , XU, Hong , LI, Qing , TANG, Huixian , PRONIN, Alexey
IPC分类号： C12Q1/02 , C12Q1/68 , G01N33/53
CPC分类号： G01N33/566 , G01N33/5008 , G01N33/5023 , G01N2500/00 , G01N2500/10
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. Also, the invention relates to the discovery of specific hT2R9 alleles and their disparate activity in functional assays with the same biter ligands. The invention further relates to the use of these T2R receptors in assays for identifying ligands that modulate the activation of these taste receptors by specific bitter ligands and related compounds. These compounds may be used as additives and/or removed from foods, beverages, cosmetics and medicinals in order to modify (block) T2R-associated bitter taste. Also T2R ligands may be used as therapeutics to treat and modulate T2R associated gastrointestinal and metabolic functions as well as treat gastrointestinal and metabolic diseases such as eating disorders, food sensing, food absorption, obesity, diabetes, Crohn's diseae, celiac disease, et al.
摘要翻译：本发明涉及T2R味觉受体家族中的特定人味觉受体对特定苦味化合物产生反应的发现。而且，本发明涉及在具有相同配体的功能性分析中发现特异性hT2R9等位基因及其不同活性。本发明进一步涉及这些T2R受体在测定中用于鉴定调节特定苦味配体和相关化合物对这些味觉受体的激活的配体的用途。这些化合物可用作添加剂和/或从食品，饮料，化妆品和药物中除去以改变（阻断）T2R相关的苦味。此外，T2R配体可用作治疗剂以治疗和调节T2R相关的胃肠和代谢功能以及治疗胃肠和代谢疾病，如进食障碍，食物感应，食物吸收，肥胖症，糖尿病，克罗恩氏病，乳糜泻等。

4. 发明申请

WO2008154286A2 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：WO2008154286A2
公开(公告)日：2008-12-18
申请号：PCT/US2008/065907
申请日：2008-06-05
申请人： SENOMYX, INC. , LI, Xiaodong , ZHANG, Feng , XU, Hong , TACHDJIAN, Catherine , ADAMSKI-WERNER, Sara , PATRON, Andrew , ZLOTNIK, Albert , ZOLLER, Mark , KLEBANSKY, Boris , FINE, Richard , KANG, Xinshan
发明人： LI, Xiaodong , ZHANG, Feng , XU, Hong , TACHDJIAN, Catherine , ADAMSKI-WERNER, Sara , PATRON, Andrew , ZLOTNIK, Albert , ZOLLER, Mark , KLEBANSKY, Boris , FINE, Richard , KANG, Xinshan
IPC分类号： A61K31/495 , A61P27/00 , C07D487/00 , C12N5/06 , G01N33/53 , G06G7/48
CPC分类号： A61K31/495 , C07F9/65586 , C07F9/65616 , G01N33/566 , G01N2333/726 , G01N2500/04 , G06F19/16 , G06F19/18
摘要： The present invention provides screening 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 as well as modifiers capable of modulating chemosensory receptors and their ligands.
摘要翻译：本发明提供了用于鉴定化学感受器及其配体的调节剂的筛选方法，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受器及其配体。

5. 发明申请

WO2008030429A2 NOVEL HAPLOTYPE OF HUMAN T2R RECEPTOR HT2R50 AND ITS USE IN ASSAYS FOR IDENTIFYING HUMAN BITTER TASTE MODULATORS 审中-公开
标题翻译：人类T2R受体HT2R50的新型HAPLOTYPE及其在鉴定人类口干调节剂中的应用
公开(公告)号：WO2008030429A2
公开(公告)日：2008-03-13
申请号：PCT/US2007/019300
申请日：2007-09-05
申请人： SENOMYX, INC. , LI, Xiaodong , PRONIN, Alexey , XU, Hong
发明人： LI, Xiaodong , PRONIN, Alexey , XU, Hong
IPC分类号： C07K14/705
CPC分类号： C07K14/705
摘要： The present invention relates to the discovery of a novel haplotype of the human taste receptor hT2R50 in the T2R taste receptor family that responds to particular bitter ligands, i.e. , 2-acetylpyrazine and ethylpyrazine. The present invention also relates to the use of this novel haplotype in assays for identifying ligands that modulate the activation of the hT2R50 taste receptor. These compounds potentially may be used as additives in foods, beverages and medicinals for modifying (blocking) hT2R50-associated bitter taste.
摘要翻译：本发明涉及T2R味觉受体家族中人味觉受体hT2R50的新型单倍型的发现，其对特定的苦味配体即2-乙酰基吡嗪和乙基吡嗪。本发明还涉及这种新型单元型在用于鉴定调节hT2R50味觉受体活化的配体的测定中的用途。这些化合物可能在食品，饮料和药物中用作修饰（阻断）hT2R50相关苦味的添加剂。

6. 发明申请

WO2005015158A3 T1R HETERO-OLIGOMERIC TASTE RECEPTORS, CELL LINES THAT EXPRESS SAID RECEPTORS, AND TASTE COMPOUNDS 审中-公开
公开(公告)号：WO2005015158A3
公开(公告)日：2005-02-17
申请号：PCT/US2004/025459
申请日：2004-08-06
申请人： SENOMYX INC. , LI, Xiaodong , STASZEWSKI, Lena , XU, Hong
发明人： LI, Xiaodong , STASZEWSKI, Lena , XU, Hong
IPC分类号： C12P21/06
摘要： The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or subunits thereof. The present invention also relates to the use of hetero-oligomeric and chimeric 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.

7. 发明申请

WO2003001876A3 T1R HETERO-OLIGOMERIC TASTE RECEPTORS AND CELL LINES THAT EXPRESS SAID RECEPTORS AND USE THEREOF FOR IDENTIFICATION OF TASTE COMPOUNDS 审中-公开
公开(公告)号：WO2003001876A3
公开(公告)日：2003-01-09
申请号：PCT/US2002/019970
申请日：2002-06-26
申请人： SENOMYX, INC. , ZOLLER, Mark, T. , LI, Xiaodong , STASZEWSKI, Lena , O'CONNELL, Shawn , ZOZULYA, Sergey , ADLER, Jon, Elliott , XU, Hong , ECHEVERRI, Fernando
发明人： ZOLLER, Mark, T. , LI, Xiaodong , STASZEWSKI, Lena , O'CONNELL, Shawn , ZOZULYA, Sergey , ADLER, Jon, Elliott , XU, Hong , ECHEVERRI, Fernando
IPC分类号： G01N33/53
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.

8. 发明申请

WO2009120313A2 IDENTIFICATION OF HUMAN T2R RECEPTORS THAT RESPOND TO BITTER LIGANDS IN SOY AND RELATED ASSAYS FOR IDENTIFYING BITTER TASTE MODULATORS 审中-公开
标题翻译：响应大豆中苦味配体的人类T2R受体的鉴定以及鉴定苦味调节剂的相关试验
公开(公告)号：WO2009120313A2
公开(公告)日：2009-10-01
申请号：PCT/US2009/001829
申请日：2009-03-24
申请人： SENOMYX, INC. , LI, Xiaodong , XU, Hong , ZHANG, Lan , LIU, Hanghui , WU, Keping
发明人： LI, Xiaodong , XU, Hong , ZHANG, Lan , LIU, Hanghui , WU, Keping
IPC分类号： C12Q1/68 , G01N33/567 , G01N33/566 , C12Q1/00 , C07K14/705 , A61K36/48 , A23L1/20
CPC分类号： C12Q1/6895 , G01N33/5008 , G01N33/566 , G01N2500/00
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 hydrolyzed soy protein derived materials. The invention further relates to the use of these T2R receptors in assays for identifying ligands that modulate the activation of these taste receptors by specific bitter ligands present in hydrolyzed soy protein materials and derivatives thereof and related compounds. These compounds may be used as additives and/or removed from soy-based foods, beverages, cosmetics and medicinals in order to modify (block) T2R-associated bitter taste elicited by bitter ligands present in hydrolyzed soy protein materials. Also these T2R ligands potentially may be used as therapeutics to treat and modulate hT2R1, hT2R8, hT2R14, hT2R44, hT2R55, hT2R61, hT2R63, hT2R64, hT2R67 and hT2R71 associated gastrointestinal and metabolic functions such as serum cholesterol levels as well as treat gastrointestinal and metabolic diseases such as eating disorders, food sensing, food absorption, obesity, diabetes, Crohn's disease, celiac disease, et al.
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水解的大豆蛋白衍生物质中的特定苦味化合物的反应。本发明进一步涉及这些T2R受体在测定中用于鉴定配体的用途，所述配体通过存在于水解大豆蛋白材料及其衍生物和相关化合物中的特定苦味配体调节这些味觉受体的活化。这些化合物可用作添加剂和/或从大豆基食品，饮料，化妆品和药物中除去，以修饰（阻断）水解大豆蛋白材料中存在的苦配体引起的T2R相关的苦味。此外，这些T2R配体可用作治疗剂以治疗和调节hT2R1，hT2R8，hT2R14，hT2R44，hT2R55，hT2R61，hT2R63，hT2R64，hT2R67和hT2R71相关的胃肠和代谢功能如血清胆固醇水平以及治疗胃肠和代谢疾病如进食障碍，食物感应，食物吸收，肥胖症，糖尿病，克罗恩氏病，乳糜泻等等。

9. 发明申请

WO2007002026A3 IDENTIFICATION OF HUMAN T2R RECEPORS THAT ARE ACTIVATED BY BITTER MOLECULES IN COFFEE (CHLOROGENIC LACTONES) AND RELATED ASSAYS FOR IDENTIFYING HUMAN BITTER TASTE MODULATORS 审中-公开
公开(公告)号：WO2007002026A3
公开(公告)日：2007-01-04
申请号：PCT/US2006/023892
申请日：2006-06-20
申请人： SENOMYX, INC. , LI, Xiadong , XU, Hong , LI, Qing , TANG, Huixian
发明人： LI, Xiadong , XU, Hong , LI, Qing , TANG, Huixian
IPC分类号： G01N33/53 , C07K14/00 , A23L1/211 , A23F5/16
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, i.e., chlorogenic lactone compounds that contribute at least partially to the bitter taste of many coffee beverages. The present invention further relates to the use of these receptors in assays for identifying ligands that modulate the activation of these taste receptors by chlorogenic lactones and related compounds and which may be used as additives and/or removed from foods, beverages and medicinals in order to modify (block) T2R-associated bitter taste. A preferred embodiment is the use of the identified compounds as additives in coffee and coffee-flavored foods, beverages and medicinals.

10. 发明申请

WO2007011859A2 IDENTIFICATION OF A NOVEL BITTER TASTE RECEPTOR T2R76 THAT SPECIFICALLY RESPONDS TO BRUCINE AND PROP BITTER LIGANDS 审中-公开
标题翻译：鉴定对BRUCINE和PROP BITTER LIGANDS的特殊反应的新型双体态TASTE RECEPTOR T2R76
公开(公告)号：WO2007011859A2
公开(公告)日：2007-01-25
申请号：PCT/US2006/027656
申请日：2006-07-17
申请人： SENOMYX , XU, Hong , LI, Xiaodong
发明人： XU, Hong , LI, Xiaodong
IPC分类号： C07K14/705 , C07H21/04 , C12P21/06
CPC分类号： C07K14/705 , A61K38/00 , C12N2799/026 , G01N2500/00
摘要： Isolated nucleic acids encoding T2R76 polypeptides, recombinants expressed T2R76 polypeptides, heterologous expression systems for recombinant expression of T2R76 polypeptides, assay methods employing the same, and methods for altering taste perception via administration of a T2R76 modulator. These T22R76 polypeptides can be expressed alone or co-expressed with another T2R polypeptide, preferably a different human T2R polypeptide. These T2R76 polypeptides specifcally respond to bitter ligands including brucine and propylthiouracil (PROP) and therefore can be used in assays that identify compounds that modulate, preferably block bitter taste.
摘要翻译：编码T2R76多肽的分离的核酸，表达T2R76多肽的重组体，用于重组表达T2R76多肽的异源表达系统，使用该多肽的测定方法，以及通过施用T2R76调节剂改变味觉的方法。这些T22R76多肽可以单独表达或与另一个T2R多肽，优选不同的人T2R多肽共表达。这些T2R76多肽特异性地响应苦味配体，包括芥子酸和丙基硫尿嘧啶（PROP），因此可以用于鉴别调节，优选阻断苦味的化合物的测定中。

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