title: The anatomy of mammalian sweet taste receptors.
abstract: All sweet-tasting compounds are detected by a single G-protein coupled receptor (GPCR), the heterodimer T1R2-T1R3, for which no experimental structure is available. The sweet taste receptor is a class C GPCR, and the recently published crystallographic structures of metabotropic glutamate receptor (mGluR) 1 and 5 provide a significant step forward for understanding structure-function relationships within this family. In this article, we recapitulate more than 600 single point site-directed mutations and available structural data to obtain a critical alignment of the sweet taste receptor sequences with respect to other class C GPCRs. Using this alignment, a homology 3D-model of the human sweet taste receptor is built and analyzed to dissect out the role of key residues involved in ligand binding and those responsible for receptor activation. Proteins 2017; 85:332-341. © 2016 Wiley Periodicals, Inc.
authors.affiliation: Université Côte d'azur, CNRS, Institut de Chimie de Nice UMR7272, 06108 Nice, France.
authors.forename: Jean-Baptiste
authors.initials: JB
authors.lastname: Chéron
authors.affiliation: Université Côte d'azur, CNRS, Institut de Chimie de Nice UMR7272, 06108 Nice, France.|Department of Brain and Cognitive Science, DGIST (Daegu Gyeongbuk Institute of Science & Technology), Daegu, Korea.
authors.forename: Jérôme
authors.initials: J
authors.lastname: Golebiowski
authors.affiliation: Université Côte d'azur, CNRS, Institut de Chimie de Nice UMR7272, 06108 Nice, France.
authors.forename: Serge
authors.initials: S
authors.lastname: Antonczak
authors.affiliation: Université Côte d'azur, CNRS, Institut de Chimie de Nice UMR7272, 06108 Nice, France.
authors.forename: Sébastien
authors.identifier: http://orcid.org/0000-0003-2245-0478
authors.initials: S
authors.lastname: Fiorucci
mesh_terms: D000595:Amino Acid Sequence; D001665:Binding Sites; D015870:Gene Expression; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D017354:Point Mutation; D011485:Protein Binding; D054730:Protein Interaction Domains and Motifs; D055503:Protein Multimerization; D017433:Protein Structure, Secondary; D064529:Receptor, Metabotropic Glutamate 5 / Q000737:chemistry* / Q000235:genetics; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000235:genetics; D018094:Receptors, Metabotropic Glutamate / Q000737:chemistry* / Q000235:genetics; D016415:Sequence Alignment; D040681:Structural Homology, Protein; D013549:Sweetening Agents / Q000737:chemistry*; D013649:Taste / Q000502:physiology
chemical_list: C578935:GRM5 protein, human; D008024:Ligands; D064529:Receptor, Metabotropic Glutamate 5; D043562:Receptors, G-Protein-Coupled; D018094:Receptors, Metabotropic Glutamate; D013549:Sweetening Agents; C104077:metabotropic glutamate receptor type 1; C431926:taste receptors, type 1
keywords: GPCR; T1R; chemical senses; class C; structure-function relationships; sweet taste