Receptor tyrosine kinases as targets for anticancer drugs

Trends Mol Med. 2002 Jan;8(1):17-23. doi: 10.1016/s1471-4914(01)02217-1.


Receptor tyrosine kinases (RTKs) are the primary mediators of the signaling network that transmit extracellular signals into the cell. Gene amplification and/or overexpression of RTK proteins or functional alterations caused by mutations in the corresponding genes or abnormal autocrine-paracrine growth factor loops contribute to constitutive RTK signaling, ultimately resulting in the manifestation of dysregulated cell growth and cancer. The mechanism of uncontrolled RTK signaling that leads to cancer has provided the rationale for anti-RTK drug development. Strategies towards the prevention and interception of RTK signaling include monoclonal antibodies, small-molecule inhibitors, immunotoxins and antisense oligonucleotides.

Publication types

  • Review

MeSH terms

  • Animals
  • Antibodies, Monoclonal / therapeutic use
  • Antineoplastic Agents / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Humans
  • Models, Genetic
  • Mutation
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Oligonucleotide Array Sequence Analysis
  • Receptor Protein-Tyrosine Kinases / antagonists & inhibitors
  • Receptor Protein-Tyrosine Kinases / metabolism*
  • Tumor Cells, Cultured


  • Antibodies, Monoclonal
  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Receptor Protein-Tyrosine Kinases