Molecular mechanism of setron-mediated inhibition of full-length 5-HT3A receptor

Serotonin receptors (5-HT3R) belong to the pentameric ligand-gated ion channel superfamily and mediate excitatory postsynaptic signaling. Here the authors present the high-resolution cryo-EM structure of 5-HT3AR bound with the competitive antagonist granisetron and further validate the granisetron-b...

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Autores principales: Sandip Basak, Yvonne Gicheru, Abhijeet Kapoor, Megan L. Mayer, Marta Filizola, Sudha Chakrapani
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2019
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Acceso en línea:https://doaj.org/article/b766ed4a222d442488eb15a659c8ec8c
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Sumario:Serotonin receptors (5-HT3R) belong to the pentameric ligand-gated ion channel superfamily and mediate excitatory postsynaptic signaling. Here the authors present the high-resolution cryo-EM structure of 5-HT3AR bound with the competitive antagonist granisetron and further validate the granisetron-binding mode with electrophysiology measurements and MD simulations.