Structure of the human histamine H1 receptor complex with doxepin

@article{Shimamura2011StructureOT,
  title={Structure of the human histamine H1 receptor complex with doxepin},
  author={Tatsuro Shimamura and Mitsunori Shiroishi and Simone Weyand and Hirokazu Tsujimoto and Graeme Winter and Vsevolod Katritch and Ruben Abagyan and Vadim Cherezov and Wei Liu and Gye Won Han and Takuya Kobayashi and Raymond C. Stevens and So Iwata},
  journal={Nature},
  year={2011},
  volume={475},
  pages={65-70}
}
The biogenic amine histamine is an important pharmacological mediator involved in pathophysiological processes such as allergies and inflammations. Histamine H1 receptor (H1R) antagonists are very effective drugs alleviating the symptoms of allergic reactions. Here we show the crystal structure of the H1R complex with doxepin, a first-generation H1R antagonist. Doxepin sits deep in the ligand-binding pocket and directly interacts with Trp 4286.48, a highly conserved key residue in G-protein… Expand

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