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Structural basis for recognition of antihistamine drug by human histamine receptor
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Structural basis for recognition of antihistamine drug by human histamine receptor
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Journal Article
Structural basis for recognition of antihistamine drug by human histamine receptor
2022
Overview
The histamine receptors belong to the G protein-coupled receptor (GPCR) superfamily, and play important roles in the regulation of histamine and other neurotransmitters in the central nervous system, as potential targets for the treatment of neurologic and psychiatric disorders. Here we report the crystal structure of human histamine receptor H
3
R bound to an antagonist PF-03654746 at 2.6 Å resolution. Combined with the computational and functional assays, our structure reveals binding modes of the antagonist and allosteric cholesterol. Molecular dynamic simulations and molecular docking of different antihistamines further elucidate the conserved ligand-binding modes. These findings are therefore expected to facilitate the structure-based design of novel antihistamines.
Crystal structure of human histamine receptor H3R bound to an antagonist PF-03654746 reveals the unexpected binding modes of the antagonist and allosteric cholesterol, which could facilitate the structure-based design of novel antihistamines.
Publisher
Nature Publishing Group UK,Nature Publishing Group,Nature Portfolio
