Senomyx, Inc.

Other

Firmenich Incorporated

Huixian Tang

Alexey Pronin

Qing Li

Xiaodong Li

Hong Xu

Jon Elliot Adler

Shawn O'Connell

Guy Servant

Paul Brust

Walter Keung

Judy Connor

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, fod absorption, obesity, diabetes, Crohn's disease, celiac disease, et al.

Identification of bitter ligands that specifically activate human T2R receptors and related assays for identifying human bitter taste modulators

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 bitter 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.

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.

Isolated nucleic acids encoding T2R76 polypeptides, recombinantly expressed T2R76 polypeptides, heterologous expression systems for recombinant expression of T2R76 polypeptides, assay methods employing the same, and methods for altering taste perception via administration of a T2R76 modulator. These T22R76 polypeptides can be expressed alone or co-expressed with another T2R polypeptide, preferably a different human T2R polypeptide.

Assays for detecting T2R76 taste modulatory compounds

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds, i.e., chlorogenic lactone compounds that contribute at least partially to the bitter taste of many coffee beverages. The present invention further relates to the use of these receptors in assays for identifying ligands that modulate the activation of these taste receptors by chlorogenic lactones and related compounds and which may be used as additives and/or removed from foods, beverages and medicinals in order to modify (block) T2R-associated bitter taste. A preferred embodiment is the use of the identified compounds as additives in coffee and coffee-flavored foods, beverages and medicinals.

Use of bitter taste receptor to screen for compounds that offset the bitter taste of chlorogenic lactone containing coffee compositions

Assays for identifying compounds that modulate, preferably inhibit bitter taste associated with the activation of hT2R4, hT2R44 and/or hT2R61 are provided. The compounds identified according to these assays should modulate, e.g., inhibit bitter taste associated with bitter tasting compounds including quinine, 6-nitrosaccharin, saccharin and/or denatonium. These compounds are useful additives for foods, beverages or medicinal preparations having a bitter taste.

Use of specific T2R taste receptors to identify compounds that block bitter taste

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds. The invention further relates to the use of these receptors in assays for identifying ligands that modulate the activation of these taste receptors by these bitter ligands and related compounds and which may be used as additives and/or removed from foods, beverages, cosmetics and medicinals in order to modify (block) T2R-associated bitter taste.

Assays which screen for compounds that modulate bitter taste of chlorogenic lactone compounds

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter ligands, i.e., acetaminophen, ranitidine, strychnine and denatonium. The present invention further relates to the use of these receptors in assays for identifying ligands that modulate the activation of these taste receptors and which may be used as additives in foods, beverages and medicinals for modifying (blocking) T2R-associated bitter taste.

Human T2R receptors for ranitidine, strychnine and denatonium and related assays for identifying human bitter taste modulators

Assays for identifying compounds that modulate, preferably inhibit bitter taste associated with the activation of hT2R4, hT2R44 and/or hT2R61 are provided. The compounds identified according to these assays should modulate, e.g., inhibit bitter taste associated with bitter tasting compounds including quinine, 6-nitrosaccharin, saccharin and/or denatonium. These compounds are useful additives for foods, beverages or medicinal preparationshaving a bitter taste.

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San Diego, CA, United States of America

Huixian Tang