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Characterization of the beta-D-glucopyranoside binding site of the human bitter taste receptor hTAS2R16.


ABSTRACT: G-protein-coupled receptors mediate the senses of taste, smell, and vision in mammals. Humans recognize thousands of compounds as bitter, and this response is mediated by the hTAS2R family, which is one of the G-protein-coupled receptors composed of only 25 receptors. However, structural information on these receptors is limited. To address the molecular basis of bitter tastant discrimination by the hTAS2Rs, we performed ligand docking simulation and functional analysis using a series of point mutants of hTAS2R16 to identify its binding sites. The docking simulation predicted two candidate binding structures for a salicin-hTAS2R16 complex, and at least seven amino acid residues in transmembrane 3 (TM3), TM5, and TM6 were shown to be involved in ligand recognition. We also identified the probable salicin-hTAS2R16 binding mode using a mutated receptor experiment. This study characterizes the molecular interaction between hTAS2R16 and beta-D-glucopyranoside and will also facilitate rational design of bitter blockers.

SUBMITTER: Sakurai T 

PROVIDER: S-EPMC2934701 | biostudies-literature | 2010 Sep

REPOSITORIES: biostudies-literature

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Characterization of the beta-D-glucopyranoside binding site of the human bitter taste receptor hTAS2R16.

Sakurai Takanobu T   Misaka Takumi T   Ishiguro Masaji M   Masuda Katsuyoshi K   Sugawara Taishi T   Ito Keisuke K   Kobayashi Takuya T   Matsuo Shinji S   Ishimaru Yoshiro Y   Asakura Tomiko T   Abe Keiko K  

The Journal of biological chemistry 20100706 36


G-protein-coupled receptors mediate the senses of taste, smell, and vision in mammals. Humans recognize thousands of compounds as bitter, and this response is mediated by the hTAS2R family, which is one of the G-protein-coupled receptors composed of only 25 receptors. However, structural information on these receptors is limited. To address the molecular basis of bitter tastant discrimination by the hTAS2Rs, we performed ligand docking simulation and functional analysis using a series of point m  ...[more]

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