5-Fluorouracil targets thymidylate synthase in the selective suppression of TH17 cell differentiation

Oncotarget. 2016 Apr 12;7(15):19312-26. doi: 10.18632/oncotarget.8344.

Abstract

While it is well established that treatment of cancer patients with 5-Fluorouracil (5-FU) can result in immune suppression, the exact function of 5-FU in the modulation of immune cells has not been fully established. We found that low dose 5-FU selectively suppresses TH17 and TH1 cell differentiation without apparent effect on Treg, TH2, and significantly suppresses thymidylate synthase (TS) expression in TH17 and TH1 cells but has a lesser effect in tumor cells and macrophages. Interestingly, the basal expression of TS varies significantly between T helper phenotypes and knockdown of TS significantly impairs TH17 and TH1 cell differentiation without affecting the differentiation of either Treg or TH2 cells. Finally, low dose 5-FU is effective in ameliorating colitis development by suppressing TH17 and TH1 cell development in a T cell transfer colitis model. Taken together, the results highlight the importance of the anti-inflammatory functions of low dose 5-FU by selectively suppressing TH17 and TH1 immune responses.

Keywords: 5-FU; Immune response; Immunity; Immunology and Microbiology Section; TH17; TS.

MeSH terms

  • Animals
  • Antimetabolites, Antineoplastic / pharmacology
  • Blotting, Western
  • Cell Differentiation / drug effects*
  • Cell Line, Tumor
  • Colitis / metabolism
  • Colitis / prevention & control
  • Cytokines / genetics
  • Cytokines / metabolism
  • Dose-Response Relationship, Drug
  • Fluorouracil / pharmacology*
  • Mice, Inbred C57BL
  • Mice, Knockout
  • RNA Interference
  • Reverse Transcriptase Polymerase Chain Reaction
  • Th1 Cells / drug effects
  • Th1 Cells / metabolism
  • Th17 Cells / drug effects*
  • Th17 Cells / metabolism
  • Thymidylate Synthase / antagonists & inhibitors*
  • Thymidylate Synthase / genetics
  • Thymidylate Synthase / metabolism

Substances

  • Antimetabolites, Antineoplastic
  • Cytokines
  • Thymidylate Synthase
  • Fluorouracil