G protein-coupled receptor kinases: Past, present and future

Cell Signal. 2018 Jan;41:17-24. doi: 10.1016/j.cellsig.2017.07.004. Epub 2017 Jul 12.


This review is provided in recognition of the extensive contributions of Dr. Robert J. Lefkowitz to the G protein-coupled receptor (GPCR) field and to celebrate his 75th birthday. Since one of the authors trained with Bob in the 80s, we provide a history of work done in the Lefkowitz lab during the 80s that focused on dissecting the mechanisms that regulate GPCR signaling, with a particular emphasis on the GPCR kinases (GRKs). In addition, we highlight structure/function characteristics of GRK interaction with GPCRs as well as a review of two recent reports that provide a molecular model for GRK-GPCR interaction. Finally, we offer our perspective on some future studies that we believe will drive this field.

Keywords: Arrestins; GPCR; GRK; Phosphorylation; Signaling; X-ray crystallography.

Publication types

  • Historical Article
  • Research Support, N.I.H., Extramural

MeSH terms

  • Arrestins / history
  • Crystallography, X-Ray
  • G-Protein-Coupled Receptor Kinases / history*
  • GTP-Binding Proteins / metabolism
  • History, 20th Century
  • Humans
  • Molecular Conformation
  • Phosphorylation
  • Receptors, G-Protein-Coupled / history*
  • Signal Transduction


  • Arrestins
  • Receptors, G-Protein-Coupled
  • G-Protein-Coupled Receptor Kinases
  • GTP-Binding Proteins