Overexpression of thymidylate synthase mediates desensitization for 5-fluorouracil of tumor cells

Int J Cancer. 2003 Sep 1;106(3):324-6. doi: 10.1002/ijc.11221.

Abstract

The prognosis of cancers of various organs overexpressing thymidylate synthase (TS) has been reported to be poor. It has been suggested that the poor prognosis is partly due to a low sensitivity of TS-overexpressing tumors to TS-targeting 5-fluorouracil (5-FU). To investigate the relationship between TS expression and sensitivity to 5-FU, we used the TS-overexpressing cervical cancer cell line SKG-II/TS and SKG-I/TS that had been established by TS gene transfer. The 50% growth inhibitory concentration (IC(50)) of 5-FU for SKG-II/TS was 24 +/- 6.0 microM, which was 6 times as high as that for the control (4.0 +/- 1.1 microM), showing significantly decreased sensitivity to 5-FU (p < 0.01). The IC(50) of 5-FU for SKG-I/TS was 90 +/- 15 microM, which was over 2 times as high as that for the control (40 +/- 0.6 microM), showing significantly decreased sensitivity to 5-FU (p < 0.05). Thus, TS-overexpressing tumors have decreased sensitivity to 5-FU, which may be one of the factors that determine the prognosis of these tumors.

MeSH terms

  • Antimetabolites, Antineoplastic / pharmacology*
  • Cell Survival / drug effects
  • Drug Resistance, Neoplasm*
  • Female
  • Fluorouracil / pharmacology*
  • Gene Expression Regulation, Enzymologic / drug effects
  • Gene Expression Regulation, Neoplastic / drug effects*
  • Humans
  • Thymidylate Synthase / metabolism*
  • Transfection
  • Tumor Cells, Cultured
  • Uterine Cervical Neoplasms / drug therapy
  • Uterine Cervical Neoplasms / enzymology*
  • Uterine Cervical Neoplasms / pathology*

Substances

  • Antimetabolites, Antineoplastic
  • Thymidylate Synthase
  • Fluorouracil