Journal
INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY
Volume 77, Issue -, Pages 184-196Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.biocel.2016.03.005
Keywords
G protein-coupled receptor (GPCR); Bitter taste receptors (T2Rs); Bitter blockers; Ligand bias; Constitutive active mutants; Cholesterol; Structural water molecules
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Funding
- Natural Sciences and Engineering Research Council of Canada (NSERC)
- Alberta Livestock and Meat Agency (ALMA)
- Manitoba Medical Services Foundation Allen Rouse Career Award
- University of Manitoba
- Research Manitoba
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Bitter taste receptors (T2Rs) belong to the super family of G protein-coupled receptors (GPCRs). There are 25 T2Rs expressed in humans, and these interact with a large and diverse group of bitter ligands. T2Rs are expressed in many extra-oral tissues and can perform diverse physiological roles. Structure function studies led to the identification of similarities and dissimilarities between T2Rs and Class A GPCRs including amino acid conservation and novel motifs. However, the efficacy of most of the T2R ligands is not yet elucidated and the biochemical pharmacology of T2Rs is poorly understood. Recent studies on T2Rs characterized novel ligands including blockers for these receptors that include inverse agonist and antagonists. In this review we discuss the techniques used for elucidating bitter blockers, concept of ligand bias, generic amino acid numbering, the role of cholesterol, and conserved water molecules in the biochemistry and pharmacology of T2Rs. (C) 2016 Elsevier Ltd. All rights reserved.
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