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    CHIMERIC HUMAN SWEET-UMAMI AND UMAMI-SWEET TASTE RECEPTORS
    4.
    发明授权
    CHIMERIC HUMAN SWEET-UMAMI AND UMAMI-SWEET TASTE RECEPTORS 有权
    嵌合体人类甜味剂 - UMAMI和UMAMI-SWEET味觉受体

    公开(公告)号：EP1937718B1

    公开(公告)日：2017-12-06

    申请号：EP06826406.8

    申请日：2006-10-19

    申请人： Senomyx, Inc.

    发明人： LI, Xiaodong ,  ZHANG, Feng ,  XU, Hong ,  LI, Qing

    IPC分类号： C07K14/705 ,  C12P21/02 ,  C12N15/62 ,  G01N33/68

    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 T1R or a variant or fragment thereof, either T1R1 or T1R2, and the transmembrane portion of another T1R or a variant or fragment thereof, either T1R1 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.

    IMPROVED PROCESS FOR THE SYNTHESIS OF SUBSTITUTED 1-BENZYL-3-(1-(ISOXAZOL-4-YLMETHYL)-1H-PYRAZOL-4-YL)IMIDAZOLIDINE-2,4-DIONES
    5.
    发明公开
    IMPROVED PROCESS FOR THE SYNTHESIS OF SUBSTITUTED 1-BENZYL-3-(1-(ISOXAZOL-4-YLMETHYL)-1H-PYRAZOL-4-YL)IMIDAZOLIDINE-2,4-DIONES 审中-公开
    改进方法合成取代的1-苄基-3-（1-（异恶唑-4-基甲基）-1H-吡唑-4-基）咪唑烷-2,4-二酮

    公开(公告)号：EP3104712A1

    公开(公告)日：2016-12-21

    申请号：EP15748635.8

    申请日：2015-02-11

    申请人： Senomyx, Inc.

    发明人： FOTSING, Joseph, R.

    IPC分类号： A23F5/40 ,  A23L27/20 ,  A61K31/422

    摘要： The present invention relates to processes and intermediates for the preparation of compounds of formula (I): or a salt or oxide thereof, wherein Alk, M1, M2, R1, R2, R3, R4, R5, R6, R7, and n are as described herein. The present invention also relates to compounds of formula (I) and composition comprising a compound of formula (I). Also disclosed is a method of altering or improving the taste of a composition that includes adding to the composition at least one compound of formula (I), in an amount effective to obtain a modified composition having altered or improved taste relative to an otherwise identical composition lacking said compound.

    T1R Hetero-oligomeric taste receptors and cell lines that express said receptors and use thereof for identification of taste compounds
    7.
    发明公开
    T1R Hetero-oligomeric taste receptors and cell lines that express said receptors and use thereof for identification of taste compounds 有权
    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。