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Full-length mouse 5-HT3A receptor in complex with SMP100, pre-activated and open-like


ABSTRACT:

SUBMITTER: Kevin Christopher Felt 

PROVIDER: EMPIAR-12199 | biostudies-other |

REPOSITORIES: biostudies-other

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Publications

Structural basis for partial agonism in 5-HT<sub>3A</sub> receptors.

Felt Kevin K   Stauffer Madeleine M   Salas-Estrada Leslie L   Guzzo Peter R PR   Xie Dejian D   Huang Jinkun J   Filizola Marta M   Chakrapani Sudha S  

Nature structural & molecular biology 20240104 4


Hyperactivity of serotonin 3 receptors (5-HT<sub>3</sub>R) underlies pathologies associated with irritable bowel syndrome and chemotherapy-induced nausea and vomiting. Setrons, a class of high-affinity competitive antagonists, are used in the treatment of these conditions. Although generally effective for chemotherapy-induced nausea and vomiting, the use of setrons for treating irritable bowel syndrome has been impaired by adverse side effects. Partial agonists are now being considered as an alt  ...[more]

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