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

ABSTRACT:

SUBMITTER: Kevin Christopher Felt

PROVIDER: EMPIAR-12265 | biostudies-other |

REPOSITORIES: biostudies-other

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Structural basis for partial agonism in 5-HT3A 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-HT3R) 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]

PMID: 38177669

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