NOVEL CELL-BASED ASSAYS FOR IDENTIFYING ENHANCERS OR INHIBITORS OF T1R TASTE RECEPTORS (T1R2/T1R3 SWEET) AND UMAMI (T1R1/T1R3 UMAMI) TASTE RECEPTORS

摘要

This invention relates to improved assays for identifying modulators (enhancers or inhibitors) of sweet (T1R2/T1R3) and umami (T1R1/T1R3) taste receptors. These receptors may comprise the endogenous T1Rs e.g., from humans or rodents, or may comprise functional variants such as 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. The subject assays preferably use endogenous taste or gastrointestinal cells which express T1R taste receptors or recombinant cell which express such T1Rs, for example mammalian cells or Xenopus oocytes. The modulators (enhancers or inhibitors) identified according to the subject assays are useful as taste modulators (which is confirmed in taste tests) and/or as therapeutics for treating conditions such as diabetes, obesity, weight control, fat metabolism, glucose metabolism, insulin metabolism, satiety and/or the release of satiety peptides such as GLP-1.