The identification of N-glycosylated residues of the human 5-HT3B receptor subunit: importance for cell membrane expression

J Neurochem. 2011 Mar;116(6):975-83. doi: 10.1111/j.1471-4159.2010.07129.x. Epub 2011 Jan 19.

Abstract

The 5-hydroxytryptamine 3 (5-HT(3)) receptor is a pentameric ligand-gated ion channel with potential molecular isoforms arising from different subunit combinations and/or different post-translational modifications of the individual subunits. Since N-glycosylation of the 5-HT3A subunit impacts cell surface trafficking, the presence of N-glycosylation of the human (h) 5-HT3B subunit and the influence upon cell membrane expression was investigated. Following transient expression of the h5-HT3B subunit by human embryonic kidney cells (HEK293 cells) stably expressing the h5-HT3A subunit, the N-glycosylation inhibitor tunicamycin reduced the size of the predominant h5-HT3B-immunoreactive protein (∼ 55 kDa reduced to ∼ 40 kDa). Disruption of each consensus N-glycosylation sequences in the h5-HT3B subunit (N31S, N75S, N117S, N147S and N182S) resulted in a reduced molecular weight (by ∼ 2-4 kDa) of each mutant when expressed by HEK293 cells stably expressing the h5-HT3A subunit. Immunocytochemical studies demonstrated that disruption of each of the N-glycosylation sequences (individually or combined) reduced the expression of the mutant h5-HT3B subunit protein in the cell membrane when co-expressed with the h5-HT3A subunit. The present study has identified utilised N-glycosylation sites of the h5-HT3B subunit and demonstrated that they promote subunit expression in the cell membrane; a prerequisite for 5-HT(3) receptor function.

MeSH terms

  • Cell Membrane / drug effects
  • Cell Membrane / metabolism*
  • Gene Expression Regulation*
  • Glycosylation / drug effects
  • HEK293 Cells / cytology
  • Humans
  • Mutagenesis, Site-Directed / methods
  • Mutation / genetics
  • Peptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine Amidase / pharmacology
  • Protein Subunits / genetics
  • Protein Subunits / metabolism*
  • Receptors, Serotonin, 5-HT3 / genetics
  • Receptors, Serotonin, 5-HT3 / metabolism*
  • Sequence Analysis, Protein / methods
  • Transfection / methods

Substances

  • Protein Subunits
  • Receptors, Serotonin, 5-HT3
  • Peptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine Amidase