Role of palmitoylation/depalmitoylation reactions in G-protein-coupled receptor function

Pharmacol Ther. 2003 Jan;97(1):1-33. doi: 10.1016/s0163-7258(02)00300-5.


G-protein-coupled receptors (GPCRs) constitute one of the largest protein families in the human genome. They are subject to numerous post-translational modifications, including palmitoylation. This review highlights the dynamic nature of palmitoylation and its role in GPCR expression and function. The palmitoylation of other proteins involved in GPCR signaling, such as G-proteins, regulators of G-protein signaling, and G-protein-coupled receptor kinases, is also discussed.

Publication types

  • Review

MeSH terms

  • Animals
  • Enzyme Activation
  • GTP-Binding Proteins / metabolism*
  • GTP-Binding Proteins / physiology
  • Humans
  • Models, Biological
  • Palmitates / metabolism*
  • Phosphorylation
  • Protein Processing, Post-Translational
  • Receptors, Cell Surface / metabolism*
  • Signal Transduction


  • Palmitates
  • Receptors, Cell Surface
  • GTP-Binding Proteins