Histone deacetylase (
HDAC) inhibitors have been shown to enhance the effects of
5-fluorouracil (5-FU) against various
cancer cells; however, no report has shown that an
HDAC inhibitor may enhance the effects of
5-FU with radiation. Therefore, we investigated whether the novel
HDAC inhibitor OBP-801/YM753 could enhance the effects of
5-FU with radiation on esophageal
squamous carcinoma KYSE170 cells. The inhibition of the cell growth was significantly stronger with the combination of OBP-801/YM753 with
5-FU than with the
5-FU treatment only. Furthermore, inhibition of the colony formation was the most effective with the combined treatment of OBP-801/YM753,
5-FU, and radiation. Western blot analysis showed that OBP-801/YM753 suppressed the expression of
thymidylate synthase induced by
5-FU. Therefore, this three-combined
therapy is promising for patients with esophageal
squamous carcinoma.