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    Screening assays to identify compounds which modulate T1R associated taste modalities which eliminate false positives
    1.
    发明授权
    Screening assays to identify compounds which modulate T1R associated taste modalities which eliminate false positives 有权

    公开(公告)号：US10281467B2

    公开(公告)日：2019-05-07

    申请号：US15724407

    申请日：2017-10-04

    Applicant: SENOMYX, INC.

    Inventor： Guy Servant ,  Nicole Servant

    IPC: G01N33/566

    Abstract: This invention relates to assays which screen for compounds that modulate taste elicited by the T1R2/T1R3 sweet taste receptor which include a novel counter screen to eliminate false positives. In addition, the invention contemplates assays which screen for compounds that modulate taste elicited by the T1R1/T1R3 umami taste receptor which include a novel counter screen to eliminate false positives. Preferably the assays are conducted in high throughput format thereby enabling the screening of many hundreds of different compounds whereby the counter screen significantly improves assay efficiency. Further, the invention relates to the use of the compounds identified in the subject screening assays to modulate T1R associated taste perception.

    Electrophysiological assays using oocytes that express human ENaC and the use of phenamil to improve the effect of ENaC enhancers in assays using membrane potential reporting dyes
    2.
    发明授权
    Electrophysiological assays using oocytes that express human ENaC and the use of phenamil to improve the effect of ENaC enhancers in assays using membrane potential reporting dyes 有权

    公开(公告)号：US10215759B2

    公开(公告)日：2019-02-26

    申请号：US15257517

    申请日：2016-09-06

    Applicant: SENOMYX, INC.

    Inventor： Guy Servant ,  Hong Chang ,  Cyril Redcrow ,  Sumita Ray ,  Imran Clark ,  Bryan Moyer

    IPC: C12Q1/02 ,  C12N15/85 ,  G01N33/50 ,  G01N33/68

    Abstract: In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should thereby modulate salty taste in humans.

    SCREENING ASSAYS TO IDENTIFY COMPOUNDS WHICH MODULATE T1R ASSOCIATED TASTE MODALITIES WHICH ELIMINATE FALSE POSITIVES
    9.
    发明申请
    SCREENING ASSAYS TO IDENTIFY COMPOUNDS WHICH MODULATE T1R ASSOCIATED TASTE MODALITIES WHICH ELIMINATE FALSE POSITIVES 审中-公开

    公开(公告)号：US20190277845A1

    公开(公告)日：2019-09-12

    申请号：US16363106

    申请日：2019-03-25

    Applicant: Senomyx, Inc.

    Inventor： Guy Servant ,  Nicole Servant

    IPC: G01N33/566

    Abstract: This invention relates to assays which screen for compounds that modulate taste elicited by the T1R2/T1R3 sweet taste receptor which include a novel counter screen to eliminate false positives. In addition, the invention contemplates assays which screen for compounds that modulate taste elicited by the T1R1/T1R3 umami taste receptor which include a novel counter screen to eliminate false positives. Preferably the assays are conducted in high throughput format thereby enabling the screening of many hundreds of different compounds whereby the counter screen significantly improves assay efficiency. Further, the invention relates to the use of the compounds identified in the subject screening assays to modulate T1R associated taste perception.

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