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Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
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The dual kinase complex FAK-Src as a promising therapeutic target in cancer

Victoria Bolós1, Joan Manuel Gasent, Sara López-Tarruella

  • 1Pfizer Oncology, Madrid, Spain;

Oncotargets and Therapy
|July 10, 2010
PubMed

Insights

The focal adhesion kinase (FAK) and steroid receptor coactivator (Src) complex drives cancer progression, metastasis, and treatment resistance. Inhibitors targeting FAK and Src show promise for overcoming these challenges in solid tumors.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cellular Signaling

Background:

  • Focal adhesion kinase (FAK) and steroid receptor coactivator (Src) are intracellular tyrosine kinases that interact to regulate cellular functions.
  • The FAK/Src complex is implicated in cancer, promoting tumor cell proliferation, anoikis resistance, angiogenesis, and epithelial-mesenchymal transition.
  • Increased FAK/Src expression and phosphorylation correlate with invasive phenotypes and resistance to anticancer therapies.

Purpose of the Study:

  • To review the normal cellular functions of the FAK/Src complex.
  • To consolidate data on the role of FAK/Src in cancer.
  • To summarize the clinical and preclinical development of FAK and Src inhibitors and their potential to overcome treatment resistance.

Main Methods:

  • Literature review of FAK/Src complex functions in normal and cancer cells.
  • Analysis of existing data on FAK/Src expression and phosphorylation in human tumors.
  • Compilation of information on FAK and Src inhibitors in clinical and preclinical development.
  • Review of FAK/Src association with chemotherapy and hormonal therapy resistance.

Main Results:

  • The FAK/Src complex is a key effector of integrin and tyrosine kinase receptor signaling.
  • FAK/Src activity is crucial for tumor growth, angiogenesis, invasion, and metastasis.
  • FAK/Src signaling contributes to resistance against current anticancer treatments.
  • Novel FAK and Src inhibitors are under development for various solid tumors.

Conclusions:

  • The FAK/Src complex plays a critical role in multiple facets of cancer progression and therapeutic resistance.
  • Targeting FAK and Src represents a promising strategy for novel cancer therapies.
  • Combined therapeutic approaches using FAK/Src inhibitors may overcome existing treatment resistances.
Keywords:
FAKFAK inhibitorsSRCSRC inhibitorscancertherapeutic target

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