Senomyx, Inc.

Other

Firmenich Incorporated

Alexey Pronin

Hong Xu

Xiaodong Li

Huixian Tang

Qing Li

Jon Elliot Adler

Guy Servant

Paul Brust

Shawn O'Connell

Walter Keung

Judy Connor

Wen Zhao

Lena Staszewski

Donald Karanewsky

Mark Zoller

Catherine Tachdjian

Vincent Darmohusodo

Andrew P Patron

Lan Zhang

Chad Priest

Bryan Moyer

Victor Selchau

Thomas P Brady

Melissa Arellano

Brett Weylan Ching

Jing Ling

Nicholas Callamaras

Hubdan Tang

Donald S Karanewsky

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.

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.

The present invention relates to isolated nucleic acid sequences that encode human olfactory cyclic nucleotide gated (CNG) channel subunits, and the corresponding polypeptides. The invention further relates to the use of human CNG channels to profile, screen for, and identify compounds that modulate the human olfactory CNG channel. More specifically, the invention relates to the expression of the human olfactory CNG channel in cells, preferably mammalian cells, and the use of these cells in high throughput cell-based assays to identify compounds that enhance or block human olfactory CNG function. Compounds that activate the olfactory CNG channel will enhance smell and can be used to make foods more palatable for individuals with attenuated olfactory function. Conversely, compounds that inhibit the olfactory CNG channel will inhibit smell and can be use to block malodors. Additionally, the invention relates to the use of cell-based olfactory CNG channel assays to identify modulates of G-protein coupled receptor (GPCRs) and other proteins that regulate cyclic nucleotide levels.

Expression of functional human olfactory cyclic nucleotide gated (CNG) channel in recombinant host cells and use thereof in cell based assays to identify smell modulators

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 of a novel haplotype of the human taste receptor hT2R50 in the T2R taste receptor family that responds to particular bitter ligands, i.e., 2-acetylpyrazine and ethylpyrazine. The present invention also relates to the use of this novel haplotype in assays for identifying ligands that modulate the activation of the hT250 taste receptor. These compounds potentially may be used as additives in foods, beverages and medicinals for modifying (blocking) hT2R50-associated bitter taste.

Methods of identifying modulators of bitter taste using hT2R50 receptors

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

Compounds that inhibit (block) bitter taste in composition and methods of making same

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

Compounds that inhibit (block) bitter taste in composition and use thereof

The present invention relates to the discovery of a novel haplotype of the human taste receptor hT2R50 in the T2R taste receptor family that responds to particular bitter ligands, i.e., 2-acetylpyrazine and ethylpyrazine. The present invention also relates to the use of this novel haplotype in assays for identifying ligands that modulate the activation of the hT2R50 taste receptor. These compounds potentially may be used as additives in foods, beverages and medicinals for modifying (blocking) hT2R50-associated bitter taste.

Nucleic acid encoding a haplotype of human T2R receptor hT2R50

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

Alexey Pronin