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US 8,524,465 B2Granted
Agonists of bitter taste receptors and uses thereof
AssigneeDeutsches Institut Fuer Ernaehrungsforschung Potsdam-Rehbruecke
InventorsMaik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
Life of this patent
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Abstract
The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.
Claims11
A method for identifying an antagonist of hTAS2R14 bitter taste receptor activity,
- wherein said hTAS2R14 bitter taste receptor activity is mediated by a hTAS2R14 bitter taste receptor comprising:
- (a) a polypeptide comprising the amino acid sequence according to SEQ ID NO:
- 2;
- or
- (b) a polypeptide comprising not more than fifteen (15) amino acid residues that are conservatively substituted compared to SEQ ID NO:
- 2 and has at least 20% hTAS2R14 bitter taste receptor activity;
- or
- (c) a polypeptide having hTAS2R14 bitter taste receptor activity and where said polypeptide is at least 95% identical to a polypeptide having the amino acid sequence according to SEQ ID NO:
- 2;
- comprising the steps:
- (1) contacting a hTAS2R14 bitter taste receptor or a host cell expressing said hTAS2R14 bitter taste receptor with a potential antagonist, and
- (2) determining whether the potential antagonist inhibits the hTAS2R14 bitter taste receptor activity;
- wherein prior, concomitantly and/or after step (1) said bitter taste receptor or said host cell is contacted with chlorhexidine.
10 more elements
A method for identifying an agonist of hTAS2R14 bitter taste receptor activity,
- wherein said hTAS2R14 bitter taste receptor activity is mediated by a hTAS2R14 bitter taste receptor comprising:
- (a) a polypeptide comprising the amino acid sequence according to SEQ ID NO:
- 2;
- or
- (b) a polypeptide comprising not more than fifteen (15) amino acid residues that are conservatively substituted compared to SEQ ID NO:
- 2 and has at least 20% hTAS2R14 bitter taste receptor activity;
- or
- (c) a polypeptide having hTAS2R14 bitter taste receptor activity and where said polypeptide is at least 95% identical to a polypeptide having the amino acid sequence according to SEQ ID NO:
- 2;
- comprising the steps:
- (1) contacting a hTAS2R14 bitter taste receptor or a host cell expressing said hTAS2R14 bitter taste receptor with a potential agonist, and
- (2) determining whether the potential agonist induces the hTAS2R14 bitter taste receptor activity;
- wherein prior, concomitantly and/or after step (1) said bitter taste receptor or said host cell is contacted with chlorhexidine.
10 more elements
Dependencies are inferred from the claim text.