Functional selectivity of EGF family peptide growth factors: Implications for cancer

Kristy J. Wilson, Jennifer L. Gilmore, John Foley, Mark A. Lemmon, David J. Riese

Research output: Contribution to journalReview article

125 Scopus citations


Breast, prostate, pancreatic, colorectal, lung, and head and neck cancers exploit deregulated signaling by ErbB family receptors and their ligands, EGF family peptide growth factors. EGF family members that bind the same receptor are able to stimulate divergent biological responses both in cell culture and in vivo. This is analogous to the functional selectivity exhibited by ligands for G-protein coupled receptors. Here we review this literature and propose that this functional selectivity of EGF family members is due to distinctions in the conformation of the liganded receptor and subsequent differences in the sites of receptor tyrosine phosphorylation and receptor coupling to signaling effectors. We also discuss the roles of divergent ligand activity in establishing and maintaining malignant phenotypes. Finally, we discuss the potential of mutant EGF family ligands as cancer chemotherapeutics targeted to ErbB receptors.

Original languageEnglish (US)
Pages (from-to)1-8
Number of pages8
JournalPharmacology and Therapeutics
Issue number1
StatePublished - Apr 1 2009


  • Amphiregulin
  • EGF
  • Epidermal growth factor receptor
  • ErbB receptors
  • ErbB4
  • Neuregulins
  • Signal transduction
  • Transforming growth factor alpha

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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