Bitter taste receptors: Novel insights into the biochemistry and pharmacology |
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| Institution: | 1. Department of Pharmacology, School of Basic Medical Sciences, Xi''an Jiaotong University Health Science Center, Xi''an 710061, China;2. Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, Xi''an Jiaotong University Health Science Center, Xi''an 710061, China;3. Department of Surgical Oncology, The First Affiliated Hospital of Xi''an Jiaotong University, Xi''an 710061, China;4. Department of Pharmacy, The Second Affiliated Hospital of Xi''an Jiaotong University, Xi''an 710004, China;1. Institute of Biochemistry, Food Science and Nutrition, The Robert H. Smith Faculty of Agriculture, Food and Environment, The Hebrew University, Rehovot, Israel;4. Department of Pharmaceutical Chemistry, University of California – San Francisco, San Francisco, CA, USA;5. Department of Molecular Genetics, German Institute of Human Nutrition Potsdam-Rehbruecke, Nuthetal, Germany |
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| Abstract: | 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. |
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| 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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