Activated human Orai1 channel in lipid biolayer may exist as a pentamer

Biochem Biophys Res Commun. 2024 Nov 12:733:150723. doi: 10.1016/j.bbrc.2024.150723. Epub 2024 Sep 21.

Abstract

The human Orai1 (hOrai1) channel plays a crucial role in extracellular Ca2+ influx and has emerged as an attractive drug target for various diseases. However, the activated structure of the hOrai1 channel assembly within a lipid bilayer remains unknown. In this study, we expressed and purified the hOrai1 channel covalently linked to two SOAR tandems (HOSS). Patch-clamp experiments in whole-cell configuration showed that HOSS is constitutively active. Biochemical characterization confirmed that the purified HOSS channels were successfully incorporated into MSP1E3D1 nanodiscs. Negative staining revealed that the HOSS channels resemble a mushroom, with the body representing the hOrai1 channel and the leg representing the SOAR domain. Surprisingly, 2D analysis of cryo-EM data demonstrated a pentameric assembly of HOSS in a lipid bilayer. Our findings suggest that the hOrai1 channel may assemble into different oligomeric states in response to varying membrane environments.

Keywords: Lipid biolayer; Nanodisc; Oligomer; Orai1; SOAR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcium / metabolism
  • Cryoelectron Microscopy
  • HEK293 Cells
  • Humans
  • Lipid Bilayers* / chemistry
  • Lipid Bilayers* / metabolism
  • ORAI1 Protein* / chemistry
  • ORAI1 Protein* / genetics
  • ORAI1 Protein* / metabolism
  • Patch-Clamp Techniques
  • Protein Multimerization

Substances

  • Lipid Bilayers
  • ORAI1 Protein
  • ORAI1 protein, human
  • Calcium