Activation state of the M3 muscarinic acetylcholine receptor modulates mammalian odorant receptor signaling

Sci Signal. 2011 Jan 11;4(155):ra1. doi: 10.1126/scisignal.2001230.

Abstract

A diverse repertoire of heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs) enables cells to sense their environment. Mammalian olfaction requires the activation of odorant receptors (ORs), the largest family of GPCRs; however, whether ORs functionally interact with other families of GPCRs is unclear. We show that the interaction of ORs with the type 3 muscarinic acetylcholine receptor (M3-R), which is found in olfactory sensory neurons (OSNs), modulated OR responses to cognate odorants. In human embryonic kidney-293T cells, ORs and the M3-R physically interacted, and the M3-R increased the potency and efficacy of odorant-elicited responses of several ORs. Selective M3-R antagonists attenuated odorant-dependent activation of OSNs, and, when the M3-R and ORs were expressed in transfected cells, OR activation was enhanced by muscarinic agonists and inhibited by muscarinic antagonists. Furthermore, M3-R-dependent potentiation of OR signaling synergized with that of receptor transporting protein 1S (RTP1S), an accessory factor required for the efficient membrane targeting of ORs. However, the M3-R did not enhance the abundance of ORs at the cell surface, suggesting that the M3-R acted through a distinct mechanism independent of RTP1S. Finally, the activation of ORs by cognate odorants transactivated the M3-R in the absence of its agonist. The crosstalk between ORs and the M3-R suggests that the functional coupling of ORs and the M3-R is required for robust OR activation.

Publication types

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

MeSH terms

  • Atropine / pharmacology
  • Benzofurans / pharmacology
  • Carbachol / pharmacology
  • Cholinergic Agonists / pharmacology
  • Colforsin / pharmacology
  • Cyclic AMP / metabolism
  • HEK293 Cells
  • Humans
  • Immunohistochemistry
  • Ionomycin / pharmacology
  • Ionophores / pharmacology
  • Membrane Transport Proteins / genetics
  • Membrane Transport Proteins / metabolism
  • Muscarinic Antagonists / pharmacology
  • Olfactory Receptor Neurons / drug effects
  • Olfactory Receptor Neurons / metabolism
  • Protein Binding / drug effects
  • Pyrrolidines / pharmacology
  • Receptor, Muscarinic M3 / genetics
  • Receptor, Muscarinic M3 / metabolism*
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism
  • Receptors, Odorant / genetics
  • Receptors, Odorant / metabolism*
  • Signal Transduction*
  • Transfection

Substances

  • Benzofurans
  • Cholinergic Agonists
  • Ionophores
  • Membrane Transport Proteins
  • Muscarinic Antagonists
  • Pyrrolidines
  • RTP1 protein, human
  • Receptor, Muscarinic M3
  • Receptors, G-Protein-Coupled
  • Receptors, Odorant
  • Colforsin
  • Ionomycin
  • Atropine
  • Carbachol
  • darifenacin
  • Cyclic AMP