Cryo-EM structure of 5-HT3A receptor in its resting conformation

Nat Commun. 2018 Feb 6;9(1):514. doi: 10.1038/s41467-018-02997-4.

Abstract

Serotonin receptors (5-HT3AR) directly regulate gut movement, and drugs that inhibit 5-HT3AR function are used to control emetic reflexes associated with gastrointestinal pathologies and cancer therapies. The 5-HT3AR function involves a finely tuned orchestration of three domain movements that include the ligand-binding domain, the pore domain, and the intracellular domain. Here, we present the structure from the full-length 5-HT3AR channel in the apo-state determined by single-particle cryo-electron microscopy at a nominal resolution of 4.3 Å. In this conformation, the ligand-binding domain adopts a conformation reminiscent of the unliganded state with the pore domain captured in a closed conformation. In comparison to the 5-HT3AR crystal structure, the full-length channel in the apo-conformation adopts a more expanded conformation of all the three domains with a characteristic twist that is implicated in gating.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cloning, Molecular
  • Cryoelectron Microscopy*
  • Electrophysiology
  • Female
  • Ions
  • Ligands
  • Mice
  • Oocytes / chemistry
  • Protein Conformation
  • Protein Domains
  • Receptors, Serotonin, 5-HT3 / ultrastructure*
  • Recombinant Proteins / chemistry
  • Serotonin / chemistry
  • Xenopus laevis

Substances

  • Ions
  • Ligands
  • Receptors, Serotonin, 5-HT3
  • Recombinant Proteins
  • Serotonin