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    Methods of screening heteromeric T1R2/T1R3 receptors which modulate sweet taste signaling
    3.
    发明授权
    Methods of screening heteromeric T1R2/T1R3 receptors which modulate sweet taste signaling 有权
    筛选调节甜味信号的异源性T1R2 / T1R3受体的方法

    公开(公告)号：US08323912B2

    公开(公告)日：2012-12-04

    申请号：US13023502

    申请日：2011-02-08

    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： G01N33/567 ,  C07K1/00 ,  C07K14/00 ,  C07K17/00

    CPC分类号： G01N33/5008 ,  C12N2503/00 ,  C12N2510/00 ,  C40B30/04 ,  G01N33/6872 ,  G01N2333/726 ,  G01N2500/10

    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。

    In vitro methods of detecting cells sensitive to sweet tastants by detecting expression of hetero-oligomeric T1R2/T1R3 taste receptors
    10.
    发明授权
    In vitro methods of detecting cells sensitive to sweet tastants by detecting expression of hetero-oligomeric T1R2/T1R3 taste receptors 有权
    通过检测异低聚T1R2 / T1R3味觉受体的表达来检测对甜味滋味物敏感的细胞的体外方法

    公开(公告)号：US08206938B2

    公开(公告)日：2012-06-26

    申请号：US13099327

    申请日：2011-05-02

    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 ,  C12Q1/68

    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。