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Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors

Overview
Journal Int J Mol Sci
Publisher MDPI
Date 2019 Mar 23
PMID 30897734
Citations 26
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Abstract

G protein-coupled receptors (GPCRs) belong to the largest class of drug targets. Approximately half of the members of the human GPCR superfamily are chemosensory receptors, including odorant receptors (ORs), trace amine-associated receptors (TAARs), bitter taste receptors (TAS2Rs), sweet and umami taste receptors (TAS1Rs). Interestingly, these chemosensory GPCRs (csGPCRs) are expressed in several tissues of the body where they are supposed to play a role in biological functions other than chemosensation. Despite their abundance and physiological/pathological relevance, the druggability of csGPCRs has been suggested but not fully characterized. Here, we aim to explore the potential of targeting csGPCRs to treat diseases by reviewing the current knowledge of csGPCRs expressed throughout the body and by analysing the chemical space and the drug-likeness of flavour molecules.

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References
1.
Santa-Cruz Calvo S, Egan J . The endocrinology of taste receptors. Nat Rev Endocrinol. 2015; 11(4):213-27. PMC: 5220401. DOI: 10.1038/nrendo.2015.7. View

2.
Galindo M, Voigt N, Stein J, van Lengerich J, Raguse J, Hofmann T . G protein-coupled receptors in human fat taste perception. Chem Senses. 2011; 37(2):123-39. DOI: 10.1093/chemse/bjr069. View

3.
Dang Y, Hao L, Cao J, Sun Y, Zeng X, Wu Z . Molecular docking and simulation of the synergistic effect between umami peptides, monosodium glutamate and taste receptor T1R1/T1R3. Food Chem. 2018; 271:697-706. DOI: 10.1016/j.foodchem.2018.08.001. View

4.
Nelson G, Hoon M, Chandrashekar J, Zhang Y, Ryba N, Zuker C . Mammalian sweet taste receptors. Cell. 2001; 106(3):381-90. DOI: 10.1016/s0092-8674(01)00451-2. View

5.
Lu P, Zhang C, Lifshitz L, Zhuge R . Extraoral bitter taste receptors in health and disease. J Gen Physiol. 2017; 149(2):181-197. PMC: 5299619. DOI: 10.1085/jgp.201611637. View