Initiation of high frequency multi-drug resistance following kinase targeting by siRNAs

Cell Cycle. 2007 Aug 15;6(16):2001-4. doi: 10.4161/cc.6.16.4538. Epub 2007 Jun 4.

Abstract

The sequential use of non cross-resistant cytotoxic agents is the standard of care for advanced solid tumors in order to enhance survival and optimise quality of life. Nevertheless, drug resistance to non cross-resistant agents is commonly witnessed, with clinical response rates to non cross-resistant regimens declining as the disease advances. Expression of ABC transporters is unlikely to fully explain this phenomenon, and a clear molecular explanation for this process remains uncertain. A statistical analysis of a recently published RNA interference screen targeting 779 kinases in three cell lines deriving from different tumor types reveals a significant correlation between resistance to paclitaxel and a non cross-resistant cytotoxic agent. Furthermore, 20% of kinases that promote resistance to paclitaxel when targeted by RNAi also promote resistance to a non cross-resistant agent within that same cell line, consistent with a tissue-type dependence of multi-drug resistance. Conversely, paclitaxel-specific resistance and sensitising kinases occur less frequently than expected. This indicates that several cell line specific kinases may regulate multi-drug resistance and provide a potential explanation for the phenomenon of drug resistance to non cross-resistant agents witnessed in oncology practice. Furthermore, this work supports efforts to identify common pathways of drug response for future drug discovery programmes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cisplatin / pharmacology
  • Doxorubicin / pharmacology
  • Drug Resistance, Multiple / genetics*
  • Drug Resistance, Neoplasm / genetics
  • Fluorouracil / pharmacology
  • HCT116 Cells
  • Humans
  • Paclitaxel / pharmacology
  • Phosphotransferases / genetics*
  • Phosphotransferases / metabolism
  • RNA, Small Interfering / genetics*
  • Transfection

Substances

  • Antineoplastic Agents
  • RNA, Small Interfering
  • Doxorubicin
  • Phosphotransferases
  • Paclitaxel
  • Cisplatin
  • Fluorouracil