Beyond the flavour: The potential druggability of chemosensory G protein-coupled receptors

Antonella Di Pizio; Maik Behrens; Dietmar Krautwurst

doi:10.3390/ijms20061402

Beyond the flavour: The potential druggability of chemosensory G protein-coupled receptors

Antonella Di Pizio^* (First Author), Maik Behrens (Co-Author), Dietmar Krautwurst (Last Author)

^*Corresponding author for this work

Research output: Contribution to journal › Review article / Perspectives › peer-review

62 Scopus citations

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.

Original language	English
Article number	1402
Journal	International Journal of Molecular Sciences
Volume	20
Issue number	6
DOIs	https://doi.org/10.3390/ijms20061402
State	Published - 2 Mar 2019

Keywords

Chemosensory receptors
Drugs
Ecnomotopic expression
Flavour molecules
Smell
Taste

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10.3390/ijms20061402

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title = "Beyond the flavour: The potential druggability of chemosensory G protein-coupled receptors",

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.",

keywords = "Chemosensory receptors, Drugs, Ecnomotopic expression, Flavour molecules, Smell, Taste",

author = "\{Di Pizio\}, Antonella and Maik Behrens and Dietmar Krautwurst",

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T2 - The potential druggability of chemosensory G protein-coupled receptors

AU - Di Pizio, Antonella

AU - Behrens, Maik

AU - Krautwurst, Dietmar

PY - 2019/3/2

Y1 - 2019/3/2

N2 - 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.

AB - 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.

KW - Chemosensory receptors

KW - Drugs

KW - Ecnomotopic expression

KW - Flavour molecules

KW - Smell

KW - Taste

UR - https://www.scopus.com/pages/publications/85063679828

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DO - 10.3390/ijms20061402

M3 - Review article / Perspectives

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AN - SCOPUS:85063679828

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JO - International Journal of Molecular Sciences

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ER -

Beyond the flavour: The potential druggability of chemosensory G protein-coupled receptors

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Keywords

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