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Updated: Feb 14, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
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Published on: September 18, 2013

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Mechanisms of receptor tyrosine kinase activation in cancer

Zhenfang Du1, Christine M Lovly2,3

  • 1Department of Medicine, Division of Hematology and Oncology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.

Molecular Cancer
|February 20, 2018
PubMed

Insights

Receptor tyrosine kinases (RTKs) are crucial for cell functions but their dysregulation drives cancer. This review covers normal RTK signaling and aberrant activation mechanisms in cancer, aiding anti-cancer therapy selection.

Area of Science:

  • Molecular Biology
  • Cellular Biology
  • Oncology

Background:

  • Receptor tyrosine kinases (RTKs) regulate fundamental cellular processes like growth, motility, differentiation, and metabolism.
  • Dysregulation of RTK signaling is implicated in various human diseases, particularly cancers.
  • Genomic studies identify alterations in RTK genes (e.g., EGFR, HER2/ErbB2, MET) in cancer patients.

Purpose of the Study:

  • To review the normal physiological activation of RTKs.
  • To discuss the mechanisms of aberrant RTK activation in human cancers.
  • To highlight the implications of understanding these mechanisms for anti-cancer therapy selection.

Main Methods:

  • Literature review of RTK signaling pathways.
  • Analysis of genomic studies on RTK alterations in cancer.
  • Synthesis of information on normal and aberrant RTK activation.

Main Results:

  • RTKs are activated through well-defined signaling pathways under normal conditions.
  • Aberrant RTK activation in cancer occurs via gain-of-function mutations, genomic amplification, chromosomal rearrangements, and autocrine activation.
  • Specific RTKs like EGFR, HER2/ErbB2, and MET are frequently altered in various cancers.

Conclusions:

  • Understanding the mechanisms of RTK dysregulation is critical for developing targeted cancer therapies.
  • Knowledge of aberrant RTK activation pathways can guide the selection of effective anti-cancer treatments.
  • This review provides a comprehensive overview of RTK roles in cancer and therapeutic implications.
Keywords:
CancerChromosomal rearrangementMutationOncogeneReceptorTargeted therapyTyrosine kinaseTyrosine kinase inhibitor (TKI)

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