Ontology highlight
ABSTRACT:
SUBMITTER: Basak S
PROVIDER: S-EPMC7655109 | biostudies-literature | 2020 Oct
REPOSITORIES: biostudies-literature
Basak Sandip S Kumar Arvind A Ramsey Steven S Gibbs Eric E Kapoor Abhijeet A Filizola Marta M Chakrapani Sudha S
eLife 20201016
Serotonin receptors (5-HT<sub>3A</sub>R) play a crucial role in regulating gut movement, and are the principal target of setrons, a class of high-affinity competitive antagonists, used in the management of nausea and vomiting associated with radiation and chemotherapies. Structural insights into setron-binding poses and their inhibitory mechanisms are just beginning to emerge. Here, we present high-resolution cryo-EM structures of full-length 5-HT<sub>3A</sub>R in complex with palonosetron, onda ...[more]