EGF-dependent induction of BCL-xL and p21CIP1/WAF1 is highly variable in HNSCC cells--implications for EGFR-targeted therapies

Anticancer Res. 2010 Nov;30(11):4579-85.

Abstract

The anti-apoptotic protein BCL-x(L) and the cell cycle inhibitor p21(CIP1/WAF1) were previously implicated in head and neck cancer. Several reports point to a role of the epidermal growth factor receptor (EGFR, ErbB-1, HER1) in regulating their expression. In the present study, we investigated the influence of EGFR on these tumor-associated factors. HNSCC cell lines were incubated with EGF or with the EGFR-specific kinase inhibitor AG1478. Western blot analysis and quantitative reverse transcription-polymerase chain reaction (qRT-PCR) were deployed to measure BCL-x(L) and p21(CIP1/WAF1) protein and mRNA levels. A dose-dependent rise of BCL-x(L) as well as p21(CIP1/WAF1) protein was noted after incubation with EGF, whereas inhibition with AG1478 reduced basal expression levels. No influence on BCL-2 was seen. Interestingly, qRT-PCR revealed that p21(CIP1/WAF1) but not BCL-x(L) transcript levels were induced after EGF treatment. Taken together, it can be stated that p21(CIP1/WAF1) and BCL-x(L) but not BCL-2 levels are tightly regulated by EGFR in HNSCC cell lines. BCL-x(L) induction appears to be due to protein stabilization rather than transcriptional activation, which is the likely cause of p21(CIP1/WAF1) induction. The noted variability in EGF response of HNSCC cells could reflect frequently observed variations in clinical response rates after implementation of anti-EGFR therapies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Blotting, Western
  • Carcinoma, Squamous Cell / drug therapy*
  • Carcinoma, Squamous Cell / genetics
  • Carcinoma, Squamous Cell / metabolism
  • Cell Proliferation / drug effects
  • Cyclin-Dependent Kinase Inhibitor p21 / genetics*
  • Cyclin-Dependent Kinase Inhibitor p21 / metabolism
  • Enzyme Inhibitors / pharmacology
  • Epidermal Growth Factor / therapeutic use*
  • ErbB Receptors / antagonists & inhibitors
  • Head and Neck Neoplasms / drug therapy*
  • Head and Neck Neoplasms / genetics
  • Head and Neck Neoplasms / metabolism
  • Humans
  • Phosphorylation / drug effects
  • Quinazolines
  • RNA, Messenger / genetics
  • Reverse Transcriptase Polymerase Chain Reaction
  • Tumor Cells, Cultured
  • Tyrphostins / pharmacology
  • bcl-X Protein / genetics*
  • bcl-X Protein / metabolism

Substances

  • BCL2L1 protein, human
  • CDKN1A protein, human
  • Cyclin-Dependent Kinase Inhibitor p21
  • Enzyme Inhibitors
  • Quinazolines
  • RNA, Messenger
  • Tyrphostins
  • bcl-X Protein
  • RTKI cpd
  • Epidermal Growth Factor
  • EGFR protein, human
  • ErbB Receptors