Trafficking of G protein-coupled receptors

Matthew T. Drake, Sudha K. Shenoy, Robert J. Lefkowitz

Research output: Contribution to journalReview articlepeer-review

240 Scopus citations


G protein-coupled receptors (GPCRs) play an integral role in the signal transduction of an enormous array of biological phenomena, thereby serving to modulate at a molecular level almost all components of human biology. This role is nowhere more evident than in cardiovascular biology, where GPCRs regulate such core measures of cardiovascular function as heart rate, contractility, and vascular tone. GPCR/ligand interaction initiates signal transduction cascades, and requires the presence of the receptor at the plasma membrane. Plasma membrane localization is in turn a function of the delivery of a receptor to and removal from the cell surface, a concept defined most broadly as receptor trafficking. This review illuminates our current view of GPCR trafficking, particularly within the cardiovascular system, as well as highlights the recent and provocative finding that components of the GPCR trafficking machinery can facilitate GPCR signaling independent of G protein activation.

Original languageEnglish (US)
Pages (from-to)570-582
Number of pages13
JournalCirculation research
Issue number6
StatePublished - Sep 2006


  • 7-transmembrane receptors
  • GPCR
  • GPCR kinase (GRK)
  • Trafficking
  • β-arrestin

ASJC Scopus subject areas

  • Physiology
  • Cardiology and Cardiovascular Medicine


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