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Regulation of SRC family kinases in human cancers

Banibrata Sen1, Faye M Johnson

  • 1Department of Thoracic/Head & Neck Medical Oncology, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA.

Journal of Signal Transduction
|July 22, 2011
PubMed

Insights

The protein tyrosine kinase Src regulates cell functions and is activated in cancers. Inhibitors targeting Src are being developed as a promising cancer therapy strategy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • The nonreceptor protein tyrosine kinase Src is vital for cell signaling in normal and cancerous cells.
  • Src family kinases (SFKs) activation is observed in many cancers, but their precise roles in tumor progression are not fully understood.
  • Src activation mechanisms involve domain interactions and structural changes influenced by activators, kinases, and phosphatases.

Purpose of the Study:

  • To summarize the regulatory mechanisms of Src kinase activity in normal and cancer cells.
  • To discuss the current status of Src inhibitor development for various cancer types.

Main Methods:

  • Review of literature on Src kinase regulation.
  • Analysis of mechanisms of Src activation in cancer.
  • Overview of clinical trials for Src inhibitors.

Main Results:

  • Src plays key roles in cancer invasion, tumor progression, epithelial-to-mesenchymal transition, angiogenesis, and metastasis.
  • Src is a validated therapeutic target in oncology.
  • Multiple small molecule Src inhibitors are under investigation in clinical trials.

Conclusions:

  • Understanding Src regulation is crucial for developing effective cancer therapies.
  • Src inhibitors represent a promising avenue for targeted cancer treatment.
  • Further research is needed to fully elucidate Src's role in diverse cancer types and optimize inhibitor strategies.

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