G protein-coupled receptors: heterologous regulation of homologous desensitization and its implications

Trends Pharmacol Sci. 1996 Nov;17(11):416-21. doi: 10.1016/s0165-6147(96)10048-1.


Two patterns of rapid desensitization have been characterized for G protein-coupled receptors: homologous desensitization, which mainly involves G protein-coupled receptor kinases and arrestins, and heterologous desensitization, which mainly involves protein kinases A (PKA) and C (PKC). In this review, Tsu Tshen Chuang and colleagues discuss evidence to show that PKA and PKC can modify the functional state of the G protein-coupled receptor kinases/arrestin homologous desensitization machinery, providing a novel level of cross-talk in signal transduction. Studies on regulation of G protein-coupled receptor kinases and arrestins confirm that the functional state of this machinery may have important consequences for cellular responsiveness and may represent new targets for therapeutic strategies.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • GTP-Binding Proteins / metabolism*
  • Humans
  • Phosphorylation
  • Receptors, Cell Surface / metabolism*
  • Sensitivity and Specificity


  • Receptors, Cell Surface
  • GTP-Binding Proteins