Advancements in G protein-coupled receptor biosensors to study GPCR-G protein coupling

Br J Pharmacol. 2023 Jun;180(11):1433-1443. doi: 10.1111/bph.15962. Epub 2022 Oct 17.

Abstract

Enzymatic and cellular signalling biosensors are used to decipher the activities of complex biological systems. Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in the human body, are plentiful and vary in utility, form and function. Their applications have continually expanded our understanding of this important protein class. Here, we briefly summarize a subset of this field with accelerating importance: transducer biosensors measuring receptor-coupling and selectivity, with an emphasis on sensors measuring receptor association and activation of heterotrimeric signalling complexes.

Keywords: BERKY; BRET; FRET; G protein coupled receptors; G proteins; GEMTA; GPCR; SPASM; TRUPATH; biosensor; functional selectivity; signalling bias; transducerome.

Publication types

  • Review
  • Research Support, N.I.H., Extramural

MeSH terms

  • Biosensing Techniques*
  • GTP-Binding Proteins / metabolism
  • Humans
  • Receptors, G-Protein-Coupled* / metabolism
  • Signal Transduction

Substances

  • Receptors, G-Protein-Coupled
  • GTP-Binding Proteins