Mapping the molecular motions of 5-HT₃ serotonin-gated channel by voltage-clamp fluorometry.

ABSTRACT: The serotonin-gated ion channel (5-HT₃R) mediates excitatory neuronal communication in the gut and the brain. It is the target for setrons, a class of competitive antagonists widely used as antiemetics, and is involved in several neurological diseases. Cryo-electron microscopy (cryo-EM) of the 5-HT₃R in complex with serotonin or setrons revealed that the protein has access to a wide conformational landscape. However, assigning known high-resolution structures to actual states contributing to the physiological response remains a challenge. In the present study, we used voltage-clamp fluorometry (VCF) to measure simultaneously, for 5-HT₃R expressed at a cell membrane, conformational changes by fluorescence and channel opening by electrophysiology. Four positi

SUBMITTER: Peverini L 

PROVIDER: S-EPMC11196107 | biostudies-literature | 2024 Jun

REPOSITORIES: biostudies-literature