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

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 t...

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Detalles Bibliográficos
Autores principales: Di Pizio, Antonella, Behrens, Maik, Krautwurst, Dietmar
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6471708/
https://www.ncbi.nlm.nih.gov/pubmed/30897734
http://dx.doi.org/10.3390/ijms20061402
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author Di Pizio, Antonella
Behrens, Maik
Krautwurst, Dietmar
author_facet Di Pizio, Antonella
Behrens, Maik
Krautwurst, Dietmar
author_sort Di Pizio, Antonella
collection PubMed
description 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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spelling pubmed-64717082019-04-26 Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors Di Pizio, Antonella Behrens, Maik Krautwurst, Dietmar Int J Mol Sci Review 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. MDPI 2019-03-20 /pmc/articles/PMC6471708/ /pubmed/30897734 http://dx.doi.org/10.3390/ijms20061402 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Di Pizio, Antonella
Behrens, Maik
Krautwurst, Dietmar
Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors
title Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors
title_full Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors
title_fullStr Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors
title_full_unstemmed Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors
title_short Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors
title_sort beyond the flavour: the potential druggability of chemosensory g protein-coupled receptors
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6471708/
https://www.ncbi.nlm.nih.gov/pubmed/30897734
http://dx.doi.org/10.3390/ijms20061402
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