Heterogeneity amongst 5-HT3 receptor subunits

Is this significant?

Nor Syafinaz Yaakob, D. T. Malone, B. Exintaris, H. R. Irving

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

The serotonin 3 (5-HT3) receptor is a ligand gated ion channel unlike the other 5-HT receptors which are G protein coupled receptors. The functional 5-HT3 receptor forms a pentamer of five symmetrically arranged subunits surrounding a central pore. The 5-HT3A subunit was first identified at a molecular level and can form functional homomers or heteromers with the 5-HT3B subunit. Recently, three new 5-HT3 subunits have been discovered and these can also form functional heteromers with the 5-HT3A subunit. In addition, splice variants of the 5-HT3 subunits have also been reported. These findings have markedly increased the complexity of the 5-HT3 receptor and may form part of the explanation of unresolved differences between studies investigating 5-HT3 receptor function in cell lines compared with native tissues. In this review we discuss the properties of the different subunits and their distribution to determine if they contribute to functional changes in the 5-HT3 receptor. Several recent pharmacogenomic studies have revealed single nucleotide polymorphisms (SNPs) and other variations in the different 5-HT3 receptor subunits that are associated with various clinical conditions. We discuss the implications of these findings with respect to drug design and tailored pharmacogenomic therapies.

Original languageEnglish
Pages (from-to)57-68
Number of pages12
JournalCurrent Molecular Medicine
Volume11
Issue number1
DOIs
Publication statusPublished - 2011
Externally publishedYes

Fingerprint

Receptors, Serotonin, 5-HT3
Ligand-Gated Ion Channels
Serotonin Receptors
Drug Design
Pharmacogenetics
G-Protein-Coupled Receptors
Polymorphism
Single Nucleotide Polymorphism
Serotonin
Nucleotides
Cells
Tissue
Cell Line
Pharmaceutical Preparations

Keywords

  • 5-HT receptors
  • Chemotherapy induced emesis
  • Irritable bowel syndrome
  • Single nucleotide polymorphisms (SNPs)

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Molecular Medicine

Cite this

Heterogeneity amongst 5-HT3 receptor subunits : Is this significant? / Yaakob, Nor Syafinaz; Malone, D. T.; Exintaris, B.; Irving, H. R.

In: Current Molecular Medicine, Vol. 11, No. 1, 2011, p. 57-68.

Research output: Contribution to journalArticle

Yaakob, Nor Syafinaz ; Malone, D. T. ; Exintaris, B. ; Irving, H. R. / Heterogeneity amongst 5-HT3 receptor subunits : Is this significant?. In: Current Molecular Medicine. 2011 ; Vol. 11, No. 1. pp. 57-68.
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