Patent ID: 8043823
Filing Date: 2011-10-25
Classification: A23L,A61P,C07D,G01N

Abstract:
1. A method for identifying an antagonist of hTAS2R46, hTAS2R47, or hTAS2R50 bitter taste receptor activity, wherein the bitter taste receptor is encoded by a polynucleotide selected from the group consisting of: (a) polynucleotide encoding at least the mature form of the polypeptide having the amino acid sequence as shown in SEQ ID NO: 2, 4, or 6; (b) polynucleotide having the coding nucleotide sequence as shown in SEQ ID NO: 1, 3, or 5 encoding at least the mature form of the polypeptide; (c) polynucleotide encoding a derivative of a polypeptide encoded by a polynucleotide of (a) or (b), wherein: (d) polynucleotide which encodes a polypeptide having hTAS2R46, hTAS2R47, or hTAS2R50 bitter taste receptor activity, and where said polypeptide is at least 95% identical to a polypeptide as shown in SEQ ID NO: 2, 4, and 6, respectively;  comprising the steps: wherein amarogentin, or structurally related agonists thereof, have a structure according to formula (VIII) wherein R R R R R R R A″ is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkoxyalkyl, heterocycloalkyl, an alicyclic system, aryl and heteroaryl; optionally substituted; s is an integer from 0 to 3; and the bond indicated by the dashed line may be present or not.