Can Adding Constitutive Receptor Activity Redefine Biased Signaling Quantification?

Trends Pharmacol Sci. 2019 Mar;40(3):156-160. doi: 10.1016/j.tips.2019.01.002. Epub 2019 Feb 1.

Abstract

Biased signaling, the differential activation of distinct signaling pathways, is currently at the center of pharmacology. Reliable characterization of biased ligands requires robust scales applicable to all ligand classes: agonists, neutral antagonists, and inverse agonists. To this end, constitutive receptor activity should be included in the models.

Keywords: GPCR; biased signaling; constitutive receptor activity; inverse agonists.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Kinetics
  • Ligands
  • Models, Biological*
  • Receptors, G-Protein-Coupled / agonists*
  • Receptors, G-Protein-Coupled / antagonists & inhibitors*
  • Receptors, G-Protein-Coupled / metabolism
  • Signal Transduction*

Substances

  • Ligands
  • Receptors, G-Protein-Coupled