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Kinome profiling of chondrosarcoma reveals SRC-pathway activity and dasatinib as option for treatment

Yvonne M Schrage1, Inge H Briaire-de Bruijn, Noel F C C de Miranda

  • 1Department of Pathology and Orthopedic Surgery, Leiden University Medical Center, Leiden, the Netherlands.

Cancer Research
|July 16, 2009
PubMed

Insights

Chondrosarcoma treatments are limited. Kinome profiling identified the Src pathway as active, and dasatinib, a Src inhibitor, showed potential therapeutic benefit in vitro for patients ineligible for surgery.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cancer Therapeutics

Background:

  • Chondrosarcomas exhibit resistance to conventional chemotherapy and radiotherapy.
  • Limited curative options exist for inoperable or metastatic chondrosarcoma.
  • Systemic treatment requires identification of novel molecular targets.

Purpose of the Study:

  • To identify molecular targets for systemic treatment of chondrosarcoma.
  • To investigate the activity of kinase pathways in chondrosarcoma.
  • To evaluate the efficacy of targeted inhibitors in chondrosarcoma cell lines.

Main Methods:

  • Kinome profiling using peptide arrays on chondrosarcoma cell lines and primary cultures.
  • Verification of kinase activity via immunoblotting.
  • In vitro evaluation of imatinib and dasatinib on chondrosarcoma cells.

Main Results:

  • Active AKT1/GSK3B, PDGFR, and Src kinase pathways were identified in chondrosarcoma.
  • Dasatinib demonstrated a decrease in chondrosarcoma cell viability at nanomolar concentrations in most cultures.
  • Imatinib showed no significant effect on chondrosarcoma cell viability.

Conclusions:

  • The Src pathway is active in chondrosarcoma, presenting a potential therapeutic target.
  • Dasatinib, a Src pathway inhibitor, may offer therapeutic benefits for surgically ineligible chondrosarcoma patients.
  • Further in vivo studies are warranted to confirm dasatinib's efficacy.

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