Low signaling efficiency from receptor to effector in olfactory transduction: A quantified ligand-triggered GPCR pathway

Proc Natl Acad Sci U S A. 2022 Aug 9;119(32):e2121225119. doi: 10.1073/pnas.2121225119. Epub 2022 Aug 1.

Abstract

G protein-coupled receptor (GPCR) signaling is ubiquitous. As an archetype of this signaling motif, rod phototransduction has provided many fundamental, quantitative details, including a dogma that one active GPCR molecule activates a substantial number of downstream G protein/enzyme effector complexes. However, rod phototransduction is light-activated, whereas GPCR pathways are predominantly ligand-activated. Here, we report a detailed study of the ligand-triggered GPCR pathway in mammalian olfactory transduction, finding that an odorant-receptor molecule when (one-time) complexed with its most effective odorants produces on average much less than one downstream effector. Further experiments gave a nominal success probability of tentatively ∼10-4 (more conservatively, ∼10-2 to ∼10-5). This picture is potentially more generally representative of GPCR signaling than is rod phototransduction, constituting a paradigm shift.

Keywords: G protein; GPCR signaling; olfactory transduction; signal amplification.

Publication types

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

MeSH terms

  • Animals
  • Ligands*
  • Light Signal Transduction
  • Mammals / metabolism
  • Odorants*
  • Receptors, G-Protein-Coupled* / metabolism
  • Receptors, Odorant* / metabolism
  • Retinal Rod Photoreceptor Cells
  • Signal Transduction*
  • Smell*

Substances

  • Ligands
  • Receptors, G-Protein-Coupled
  • Receptors, Odorant