c-Kit-dependent growth of uveal melanoma cells: a potential therapeutic target?

Invest Ophthalmol Vis Sci. 2004 Jul;45(7):2075-82. doi: 10.1167/iovs.03-1196.

Abstract

Purpose: This study was conducted to investigate the expression and functional impact of the proto-oncogene c-kit in uveal melanoma.

Methods: Based on immunohistochemical (IHC) study of paraffin-embedded specimens from 134 uveal melanomas and Western blot analysis on eight fresh-frozen samples the expression of c-kit in uveal melanoma was studied. Furthermore, the phosphorylation of c-kit and the impact of the tyrosine kinase inhibitor STI571 was examined in the three uveal melanoma cell lines OCM-1, OCM-3, and 92-1.

Results: Eighty-four of 134 paraffin-embedded samples and six of eight fresh-frozen samples expressed c-kit. c-Kit was strongly expressed and tyrosine phosphorylated in cultured uveal melanoma cells compared with cutaneous melanoma cells. Moreover, in contrast to cutaneous melanoma cell lines c-kit maintained a high phosphorylation level in serum-depleted uveal melanoma cells. No activation-related mutations in exon 11 of the KIT gene were found. On the contrary, expression of the stem cell growth factor (c-kit ligand) was detected in all three uveal melanoma cell lines, suggesting the presence of autocrine (paracrine) stimulation pathways. Treatment of uveal melanoma cell lines with STI571, which blocks c-kit autophosphorylation, resulted in cell death. The IC(50) of the inhibitory effects on c-kit phosphorylation and cell proliferation was of equal size and less than 2.5 microM.

Conclusions: The results confirm that c-kit is vastly expressed in uveal melanoma, suggest that the c-kit molecular pathway may be important in uveal melanoma growth, and point to its use as a target for therapy with STI571.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Benzamides
  • Blotting, Western
  • Cell Division
  • Female
  • Humans
  • Imatinib Mesylate
  • Immunoenzyme Techniques
  • Male
  • Melanoma / metabolism*
  • Melanoma / pathology*
  • Middle Aged
  • Paraffin Embedding
  • Phosphorylation / drug effects
  • Piperazines
  • Polymerase Chain Reaction
  • Proto-Oncogene Mas
  • Proto-Oncogene Proteins c-kit / genetics
  • Proto-Oncogene Proteins c-kit / metabolism*
  • Pyrimidines / pharmacology
  • RNA, Messenger / metabolism
  • Skin Neoplasms / metabolism
  • Skin Neoplasms / pathology
  • Tumor Cells, Cultured
  • Tyrosine / metabolism
  • Uveal Neoplasms / metabolism*
  • Uveal Neoplasms / pathology*

Substances

  • Benzamides
  • MAS1 protein, human
  • Piperazines
  • Proto-Oncogene Mas
  • Pyrimidines
  • RNA, Messenger
  • Tyrosine
  • Imatinib Mesylate
  • Proto-Oncogene Proteins c-kit