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Updated: Jan 27, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors
Antonella Di Pizio1, Maik Behrens2, Dietmar Krautwurst3
1Leibniz-Institute for Food Systems Biology at the Technical University of Munich, Freising, 85354, Germany. a.dipizio.leibniz-lsb@tum.de.
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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