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    T1R HETERO-OLIGOMERIC TASTE RECEPTORS AND CELL LINES THAT EXPRESS SAID RECEPTORS AND USE THEREOF FOR IDENTIFICATION OF TASTE COMPOUNDS
    2.
    发明申请
    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：US20190086393A1

    公开(公告)日：2019-03-21

    申请号：US16130319

    申请日：2018-09-13

    Applicant: Senomyx, Inc.

    Inventor： Mark ZOLLER ,  Xiaodong LI ,  Lena Staszewski ,  Shawn O'Connell ,  Sergey Zozulya ,  Jon Elliot Adler ,  Hong Xu ,  Fernando Echeverri

    IPC: G01N33/50 ,  C12Q1/6876 ,  G01N33/566 ,  C07K14/705

    Abstract: 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.

    Methods of using TIR hetero-oligomeric receptors for screening compounds that modulate sweet or umami taste
    4.
    发明授权
    Methods of using TIR hetero-oligomeric receptors for screening compounds that modulate sweet or umami taste 有权

    公开(公告)号：US10088472B2

    公开(公告)日：2018-10-02

    申请号：US15264785

    申请日：2016-09-14

    Applicant: SENOMYX, INC.

    Inventor： Jon E. Adler ,  Xiaodong Li ,  Lena Luukkonen ,  Hong Xu ,  Fernando Echeverri

    IPC: G01N33/50 ,  G01N33/74 ,  C07K14/72

    Abstract: Newly identified mammalian taste-cell-specific G protein-coupled receptors which function as hetero-oligomeric complexes in the sweet taste transduction pathway, and the genes and cDNA encoding said receptors are described. Specifically, T1R G protein-coupled receptors active in sweet taste signaling as hetero-oligomeric complexes, 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 identifying putative taste modulating compounds using such hetero-oligomeric complexes also described, as is a novel surface expression facilitating peptide useful for targeting integral plasma membrane proteins to the surface of a cell.

    Identification of bitter ligands that specifically activate human T2R receptors and related assays for identifying human bitter taste modulators
    10.
    发明授权
    Identification of bitter ligands that specifically activate human T2R receptors and related assays for identifying human bitter taste modulators 有权
    识别特异性激活人T2R受体的苦配体和相关测定法，用于鉴定人类苦味调节剂

    公开(公告)号：US09170254B2

    公开(公告)日：2015-10-27

    申请号：US14243380

    申请日：2014-04-02

    Applicant: SENOMYX, INC.

    Inventor： Xiaodong Li ,  Hong Xu ,  Qing Li ,  Huixian Tang ,  Alexey Pronin

    IPC: G01N33/50 ,  G01N33/566

    CPC classification number: G01N33/566 ,  G01N33/5008 ,  G01N33/5023 ,  G01N2500/00 ,  G01N2500/10

    Abstract: 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 disease, celiac disease, et al.

    Abstract translation: 本发明涉及T2R味觉受体家族中的特定人味受体对特定苦味化合物的反应的发现。 此外，本发明涉及特异性hT2R9等位基因的发现及其在具有相同配体配体的功能测定中的不同活性。 本发明还涉及这些T2R受体在用于鉴定通过特定的苦配体和相关化合物调节这些味觉受体的活化的配体的测定中的用途。 这些化合物可以用作添加剂和/或从食品，饮料，化妆品和药物中去除，以便改变（阻断）T2R相关的苦味。 也可以使用T2R配体作为治疗和调节T2R相关胃肠道和代谢功能以及治疗胃肠道和代谢疾病如饮食失调，食物感觉，食物吸收，肥胖，糖尿病，克罗恩病，乳糜泻等的治疗剂。

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