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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...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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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. |
format | Online Article Text |
id | pubmed-6471708 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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