Targeting the cancer kinome through polypharmacology

Nat Rev Cancer. 2010 Feb;10(2):130-7. doi: 10.1038/nrc2787.


Kinase inhibitors are the largest class of new cancer drugs. However, it is already apparent that most tumours can escape from the inhibition of any single kinase. If it is necessary to inhibit multiple kinases, how do we choose which ones? In this Opinion article, we discuss some of the strategies that are currently being used to identify new therapeutic combinations of kinase targets.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Drug Delivery Systems*
  • Drug Discovery*
  • Drug Resistance, Neoplasm*
  • Humans
  • Mutation
  • Neoplasms / drug therapy*
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein Kinases / genetics
  • RNA, Small Interfering / pharmacology
  • Technology, Pharmaceutical


  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • RNA, Small Interfering
  • Protein Kinases