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1. 发明申请

US20080020424A9 HETEROMERIC UMAMI T1R1/T1R3 TASTE RECEPTORS AND ISOLATED CELLS THAT EXPRESS SAME 有权
标题翻译：异位UMAMI T1R1 / T1R3具有明显特异性的受体和分离的细胞
公开(公告)号：US20080020424A9
公开(公告)日：2008-01-24
申请号：US10179373
申请日：2002-06-26
申请人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
发明人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
IPC分类号： C07K14/705 , C12P21/02 , C12N5/06 , C07H21/04
CPC分类号： G01N33/5041 , A01K2217/05 , C07K14/705 , C07K2319/00 , C12Q1/6876 , C12Q2600/124 , C12Q2600/158 , G01N33/5008 , G01N33/566 , G01N2333/4719 , G01N2333/705 , G01N2333/726 , G01N2500/04
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。特别地，已经发现，T1R1和T1R3的共表达导致对鲜味刺激（包括谷氨酸钠）起反应的味觉感受器。此外，已经发现，T1R2和T1R3受体的共表达导致对包括天然存在的和人造甜味剂的甜味刺激有反应的味觉受体。本发明还涉及在测定中使用包含T1R1 / T1R3和T1R2 / T1R3的异低聚味觉感受器来鉴定分别响应于鲜味刺激和甜味刺激的化合物。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; 在组成型或诱导性条件下。还提供了在基于细胞的测定中使用这些细胞系以鉴定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测定。最后，本发明涉及一些发现，一些化合物，例如乳酸，抑制人T1R2 / T1R3和T1R1 / T1R3受体的活性，因此抑制甜味和鲜味，这表明这些受体可能是唯一的甜味和鲜味受体。

2. 发明申请

US20060127977A1 Isolated (T1R2/T1R3) sweet taste receptors that respond to sweet taste stimuli 有权
标题翻译：分离（T1R2 / T1R3）甜味受体，对甜味刺激有反应
公开(公告)号：US20060127977A1
公开(公告)日：2006-06-15
申请号：US10725037
申请日：2003-12-02
申请人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
发明人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
IPC分类号： A61K38/17 , C07K14/705 , C12N5/06 , C07H21/04 , C12P21/06
CPC分类号： G01N33/5041 , A01K2217/05 , C07K14/705 , C07K2319/00 , C12Q1/6876 , C12Q2600/124 , C12Q2600/158 , G01N33/5008 , G01N33/566 , G01N2333/4719 , G01N2333/705 , G01N2333/726 , G01N2500/04
摘要： Isolated or biologically pure taste receptors comprised of at least one T1R2 and T1R3 polypeptide and compositions containing are provided. These taste receptors specifically bind and/or are specifically activated by sweet taste stimuli such as natural and artificial sweetener compounds. These taste receptors are useful in screening assays for identifying compounds that elicit or modulate (enhance or inhibit) sweet taste. These compounds can be used as additives and flavorants to improve the taste of compositions for human or animal consumption. In preferred embodiments, the T1R2/T1R3 receptor will be comprised of human T1R2/human T1R3 expressed in association with a suitable G protein, preferably Gα15.
摘要翻译：提供了由至少一种T1R2和T1R3多肽组成的分离的或生物学上纯的味觉受体和含有的组合物。这些味觉受体特异性结合和/或由甜味刺激物例如天然和人造甜味剂化合物特异性活化。这些味觉受体可用于鉴定诱导或调节（增强或抑制）甜味的化合物的筛选测定。这些化合物可用作添加剂和调味剂，以改善用于人或动物消费的组合物的味道。在优选的实施方案中，T1R2 / T1R3受体将由与合适的G蛋白（优选Gα15）相关联表达的人T1R2 /人T1R3组成。

3. 发明申请

US20060014208A1 Functional assays for identifying compounds that modulate T1R2/T1R3 (sweet) taste 有权
标题翻译：用于鉴定调节T1R2 / T1R3（甜味）味道的化合物的功能测定
公开(公告)号：US20060014208A1
公开(公告)日：2006-01-19
申请号：US10725475
申请日：2003-12-03
申请人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
发明人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
IPC分类号： G01N33/53 , C07H21/04 , C12P21/06 , C07K14/705
CPC分类号： G01N33/5041 , A01K2217/05 , C07K14/705 , C07K2319/00 , C12Q1/6876 , C12Q2600/124 , C12Q2600/158 , G01N33/5008 , G01N33/566 , G01N2333/4719 , G01N2333/705 , G01N2333/726 , G01N2500/04
摘要： Functional assays for identifying compounds that activate or modulate the activation of the T1R2/T1R3 (sweet) taste receptor are provided. These assays detect the effect of one or more compounds on the activation of T1R2/T1R3 (sweet) taste receptor or on the activation of T1R2/T1R3 sweet taste receptor by another, compound e.g., saccharin or another artificial or natural sweetener. These assays preferably are cell-based functional assays and typically use cells, e.g., HEK-293 cells that stably express a G protein such as Gα15, Gα16 or gustducin. Compounds identified in the disclosed functional assays are potentially useful as additives in compositions for human or animal consumption.
摘要翻译：提供用于鉴定激活或调节T1R2 / T1R3（甜味）味觉受体的活化的化合物的功能测定。这些测定法检测一种或多种化合物对T1R2 / T1R3（甜味）感受器的激活或另一种化合物例如糖精或另一种人造或天然甜味剂对T1R2 / T1R3甜味受体的活化的影响。这些测定优选是基于细胞的功能测定，并且通常使用细胞，例如稳定表达G蛋白如GαA，αα16或gustducin的HEK-293细胞。在所公开的功能测定中鉴定的化合物潜在地用作用于人或动物消费的组合物中的添加剂。

4. 发明申请

US20050084932A1 Binding assays that use the T1R1/T1R3 (Umami) taste receptor to identify compounds that elicit or modulate umami taste 有权
标题翻译：使用T1R1 / T1R3（Umami）味觉受体的结合测定法鉴定引发或调节鲜味的化合物
公开(公告)号：US20050084932A1
公开(公告)日：2005-04-21
申请号：US10725418
申请日：2003-12-03
申请人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
发明人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
IPC分类号： C07K14/705 , A61K38/17 , C07H21/04
CPC分类号： C07K14/705 , A01K2217/05 , G01N2333/726
摘要： Binding assays for identifying compounds that induce or modulate the T1R1/T1R3 (umami) receptor-associated taste are provided. These binding assays detect the specific binding of a compound to a T1R1/T1R3 (umami) taste receptor or detect the modulation (inhibition or enhancement) of the binding of another compound, e.g., L-glutamate, L-aspartate or lactisole to a T1R1/T1R3 umami taste receptor. Compounds that are identified in these binding assays have potential application as T1R1/T1R3 umami taste modulators and therefore can be used as flavor additives in compositions for human or animal consumption.
摘要翻译：提供了用于鉴定诱导或调节T1R1 / T1R3（鲜味）受体相关味道的化合物的结合测定法。这些结合测定法检测化合物与T1R1 / T1R3（鲜味）味觉受体的特异性结合，或检测另一种化合物（例如L-谷氨酸，L-天冬氨酸或乳清蛋白）与T1R1的结合的调节（抑制或增强） / T1R3鲜味受体。在这些结合测定中鉴定的化合物具有作为T1R1 / T1R3鲜味调节剂的潜在应用，因此可用作人或动物消费组合物中的风味添加剂。

5. 发明申请

US20070292944A1 T1R Taste Receptors and Genes Encoding Same 有权
标题翻译： T1R口味受体和编码相同的基因
公开(公告)号：US20070292944A1
公开(公告)日：2007-12-20
申请号：US11745857
申请日：2007-05-08
申请人： Jon ADLER , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya
发明人： Jon ADLER , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya
IPC分类号： C12N15/64
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 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 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。具体地说，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知的方法，以及用于产生哺乳动物中引发预定味觉的新颖分子或分子组合的方法，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. 发明申请

US20050032158A1 Binding assays that use human T1R2 to identify potential taste modulators 有权
标题翻译：使用人类T1R2鉴定潜在味觉调节剂的结合分析
公开(公告)号：US20050032158A1
公开(公告)日：2005-02-10
申请号：US10725284
申请日：2003-12-02
申请人： Jon Adler , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya
发明人： Jon Adler , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya
IPC分类号： G01N33/50 , A23L1/305 , C07K14/705 , C07K16/28 , C07K19/00 , C12M1/00 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/12 , C12Q1/02 , G01N33/15 , G01N33/53 , G01N37/00 , C12Q1/68 , C07H21/04
CPC分类号： C07K14/723 , C07K14/705 , C07K2319/00 , C12Q1/6883 , G01N33/5041 , G01N33/6872 , G01N33/74 , G01N2333/726 , G06F19/12
摘要： Binding assays for identifying compounds that modulate human T1R2 polypeptide associated taste are disclosed. These assays detect the specific binding of compounds to a human T1R2 polypeptide or the modulation of the specific binding of a compound that specifically binds to a human T1R2 polypeptide. The binding assays may include the use of detectable labels, e.g., radionuclides, enxymes, fluorophases, and the like. Compounds identified in these binding assays have putative application as T1R2 taste modulators, particularly sweet taste, and potentially are useful additives in compositions for human or animal consumption.
摘要翻译：公开了用于鉴定调节人类T1R2多肽相关味道的化合物的结合测定法。这些测定法检测化合物与人T1R2多肽的特异性结合，或调节与人T1R2多肽特异性结合的化合物的特异性结合。结合测定可以包括使用可检测的标记，例如放射性核素，核酸，氟化酶等。在这些结合测定中鉴定的化合物具有T1R2味道调节剂，特别是甜味的推定应用，并且潜在地是用于人或动物消费的组合物中有用的添加剂。

7. 发明申请

US20060160176A1 Functional assays for identifying compounds that modulate T1R1/T1R3 (umami) taste 有权
标题翻译：用于鉴定调节T1R1 / T1R3（鲜味）味道的化合物的功能测定
公开(公告)号：US20060160176A1
公开(公告)日：2006-07-20
申请号：US10725488
申请日：2003-12-03
申请人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
发明人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Adler , Hong Xu , Fernando Echeverri
IPC分类号： A61K38/17 , C07H21/04 , C12P21/06 , C07K14/705
CPC分类号： G01N33/5041 , A01K2217/05 , C07K14/705 , C07K2319/00 , C12Q1/6876 , C12Q2600/124 , C12Q2600/158 , G01N33/5008 , G01N33/566 , G01N2333/4719 , G01N2333/705 , G01N2333/726 , G01N2500/04
摘要： Functional assays for identifying compounds that activate or modulate the activation of the T1R1/T1R3 (umami) taste receptor are provided. These assays detect the effect of one or more compounds on the activation of T1R1/T1R3 (umami) taste receptor or on the activation of T1R1/T1R3 umami taste receptor by another compound e.g., monosodium glutamate, lactisole, or another unami taste modulator. These assays preferably are cell-based functional assays and typically use cells, e.g., HEK-293 cells that express a G protein such as Gα15, Gα16 or gustducin. Compounds identified in the disclosed functional assays are potentially useful as flavor additives in compositions for human or animal consumption.
摘要翻译：提供用于鉴定激活或调节T1R1 / T1R3（鲜味）味觉受体的活化的化合物的功能测定。这些测定法检测一种或多种化合物对T1R1 / T1R3（鲜味）味觉受体活化的影响，或通过另一种化合物如谷氨酸钠，乳清酸或另一种非口味调节剂对T1R1 / T1R3鲜味受体的活化。这些测定优选是基于细胞的功能测定，并且通常使用细胞，例如表达G蛋白例如Gα，αα16或Gustducin的HEK-293细胞。在公开的功能测定中鉴定的化合物在用于人类或动物消费的组合物中可用作风味添加剂。

8. 发明申请

US20080038741A1 T1R taste receptors and genes encoding same 有权
标题翻译： T1R味觉受体和编码相同的基因
公开(公告)号：US20080038741A1
公开(公告)日：2008-02-14
申请号：US11797156
申请日：2007-05-01
申请人： Jon Adler , Sergey Zozulya , Xiadong Li , Shawn O'Connell , Lena Staszewski
发明人： Jon Adler , Sergey Zozulya , Xiadong Li , Shawn O'Connell , Lena Staszewski
IPC分类号： C12N15/12 , C07H21/00 , C07K14/705 , C12Q1/68 , G01N33/566 , G01N33/53 , C12N15/63 , C07K16/28
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 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。具体地说，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促味剂的味觉的方法，以及用于产生在哺乳动物中引发预定味觉的新颖分子或分子组合的方法，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。

9. 发明申请

US20080026404A1 Chimeric human T1R3 taste receptor polyptides and compositions containing same 有权
标题翻译：嵌合人类T1R3味道受体多肽及其组合物
公开(公告)号：US20080026404A1
公开(公告)日：2008-01-31
申请号：US11797155
申请日：2007-05-01
申请人： Jon Adler , Sergey Zozulya , Xiadong Li , Shawn O'Connell , Lena Staszewski
发明人： Jon Adler , Sergey Zozulya , Xiadong Li , Shawn O'Connell , Lena Staszewski
IPC分类号： G01N33/53 , C07K14/00 , G01N33/68
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 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。具体地说，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促味剂的味觉的方法，以及用于产生在哺乳动物中引发预定味觉的新颖分子或分子组合的方法，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。

10. 发明授权

US08759015B2 Methods of screening T1R1/T1R3 receptors for compounds that modulate umami taste signaling 有权
标题翻译：筛选调节鲜味信号的化合物的T1R1 / T1R3受体的方法
公开(公告)号：US08759015B2
公开(公告)日：2014-06-24
申请号：US13549833
申请日：2012-07-16
申请人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Elliot Adler , Hong Xu , Fernando Echeverri
发明人： Mark Zoller , Xiaodong Li , Lena Staszewski , Shawn O'Connell , Sergey Zozulya , Jon Elliot Adler , Hong Xu , Fernando Echeverri
IPC分类号： G01N33/53 , G01N33/567
CPC分类号： G01N33/5041 , A01K2217/05 , C07K14/705 , C07K2319/00 , C12Q1/6876 , C12Q2600/124 , C12Q2600/158 , G01N33/5008 , G01N33/566 , G01N2333/4719 , G01N2333/705 , G01N2333/726 , G01N2500/04
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. 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。特别地，已经发现，T1R1和T1R3的共表达导致对鲜味刺激（包括谷氨酸钠）起反应的味觉感受器。此外，已经发现，T1R2和T1R3受体的共表达导致对包括天然存在的和人造甜味剂的甜味刺激有反应的味觉受体。最后，本发明涉及一些发现，一些化合物，例如乳酸，抑制人T1R2 / T1R3和T1R1 / T1R3受体的活性，因此抑制甜味和鲜味，这表明这些受体可能是唯一的甜味和鲜味受体。

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