Identifying resistance mechanisms against five tyrosine kinase inhibitors targeting the ERBB/RAS pathway in 45 cancer cell lines

PLoS One. 2013;8(3):e59503. doi: 10.1371/journal.pone.0059503. Epub 2013 Mar 29.

Abstract

Because of the low overall response rates of 10-47% to targeted cancer therapeutics, there is an increasing need for predictive biomarkers. We aimed to identify genes predicting response to five already approved tyrosine kinase inhibitors. We tested 45 cancer cell lines for sensitivity to sunitinib, erlotinib, lapatinib, sorafenib and gefitinib at the clinically administered doses. A resistance matrix was determined, and gene expression profiles of the subsets of resistant vs. sensitive cell lines were compared. Triplicate gene expression signatures were obtained from the caArray project. Significance analysis of microarrays and rank products were applied for feature selection. Ninety-five genes were also measured by RT-PCR. In case of four sunitinib resistance associated genes, the results were validated in clinical samples by immunohistochemistry. A list of 63 top genes associated with resistance against the five tyrosine kinase inhibitors was identified. Quantitative RT-PCR analysis confirmed 45 of 63 genes identified by microarray analysis. Only two genes (ANXA3 and RAB25) were related to sensitivity against more than three inhibitors. The immunohistochemical analysis of sunitinib-treated metastatic renal cell carcinomas confirmed the correlation between RAB17, LGALS8, and EPCAM and overall survival. In summary, we determined predictive biomarkers for five tyrosine kinase inhibitors, and validated sunitinib resistance biomarkers by immunohistochemistry in an independent patient cohort.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Carcinoma, Renal Cell / drug therapy
  • Carcinoma, Renal Cell / genetics
  • Carcinoma, Renal Cell / pathology
  • Cell Line, Tumor
  • Computational Biology*
  • Drug Resistance, Neoplasm / genetics*
  • ErbB Receptors / metabolism*
  • Female
  • Humans
  • Indoles / pharmacology
  • Indoles / therapeutic use
  • Kidney Neoplasms / drug therapy
  • Kidney Neoplasms / genetics
  • Kidney Neoplasms / pathology
  • Male
  • Middle Aged
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Pyrroles / pharmacology
  • Pyrroles / therapeutic use
  • Signal Transduction / drug effects*
  • Signal Transduction / genetics
  • Sunitinib
  • Transcriptome / drug effects
  • ras Proteins / metabolism*

Substances

  • Indoles
  • Protein Kinase Inhibitors
  • Pyrroles
  • EGFR protein, human
  • ErbB Receptors
  • Protein-Tyrosine Kinases
  • ras Proteins
  • Sunitinib

Grants and funding

The study was supported by the OTKA PD 83154, by the Predict project (grant no. 259303 of the Health.2010.2.4.1.-8 call), by the TAMOP-4.2.1.B-09/1/KMR-2010-0001 and by the Alexander von Humboldt Stiftung. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.