EGFR Signaling in Cancer

Ligands

  • EGFR (ERBB1) has seven known ligands: epidermal growth factor (EGF), TGFA, heparin-binding EGF-like growth factor (HBEGF), amphiregulin (AREG), betacellulin (BTC), epiregulin (EREG), and epigen (EPGN). EGF and TGFα are the most common and most characterized.
  • Interestingly, ERBB2 (HER2) does not have a ligand. ERBB2 can heterodimerize with EGFR, ERBB3, and ERBB4, functioning through activation of other receptor family members.
  • Neuregulin 1 and 2 bind ERBB3 to activate it, whereas EGF, BTC, and neuregulins (1–4) bind ERBB4.

EGFR Signaling in Cancer

  • Dysregulation of EGFR signaling is seen in cancer.
  • EGFR kinase are commonly seen in lung cancer. These result in constitutive activation of the EGF receptor.
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