Heteromeric α7β2 Nicotinic Acetylcholine Receptors in the Brain

Jie Wu, Qiang Liu, Pei Tang, Jens D. Mikkelsen, Jianxin Shen, Paul Whiteaker, Jerrel L. Yakel

Research output: Contribution to journalReview articlepeer-review

49 Scopus citations

Abstract

The α7 nicotinic acetylcholine receptor (α7 nAChR) is highly expressed in the brain, where it maintains various neuronal functions including (but not limited to) learning and memory. In addition, the protein expression levels of α7 nAChRs are altered in various brain disorders. The classic rule governing α7 nAChR assembly in the mammalian brain was that it was assembled from five α7 subunits to form a homomeric receptor pentamer. However, emerging evidence demonstrates the presence of heteromeric α7 nAChRs in heterologously expressed systems and naturally in brain neurons, where α7 subunits are co-assembled with β2 subunits to form a novel type of α7β2 nAChR. Interestingly, the α7β2 nAChR exhibits distinctive function and pharmacology from traditional homomeric α7 nAChRs. We review recent advances in probing the distribution, function, pharmacology, pathophysiology, and stoichiometry of the heteromeric α7β2 nAChR, which have provided new insights into the understanding of a novel target of cholinergic signaling.

Original languageEnglish (US)
Pages (from-to)562-574
Number of pages13
JournalTrends in Pharmacological Sciences
Volume37
Issue number7
DOIs
StatePublished - Jul 1 2016
Externally publishedYes

Keywords

  • acetylcholine
  • alpha 7 nicotinic acetylcholine receptor
  • choline
  • nicotine
  • nicotinic acetylcholine receptor

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology

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