Small GTPase regulation of GPCR anterograde trafficking

Trends Pharmacol Sci. 2012 Jan;33(1):28-34. doi: 10.1016/ Epub 2011 Oct 17.


The physiological functions of heterotrimeric G protein-coupled receptors (GPCRs) are dictated by their intracellular trafficking and precise targeting to the functional destinations. Over the past decades, most studies on the trafficking of GPCRs have focused on the events involved in endocytosis and recycling. By contrast, the molecular mechanisms underlying anterograde transport of newly synthesized GPCRs from the endoplasmic reticulum (ER) to the cell surface have only now begun to be revealed. In this review we discuss current advances in understanding the role of Ras-like GTPases, specifically the Rab and Sar1/ARF subfamilies, in regulating cell-surface transport of GPCRs en route from the ER and the Golgi.

Publication types

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

MeSH terms

  • Endoplasmic Reticulum / metabolism
  • Humans
  • Monomeric GTP-Binding Proteins / metabolism*
  • Protein Transport
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction


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