A novel small molecule hybrid of vorinostat and DACA displays anticancer activity against human hormone-refractory metastatic prostate cancer through dual inhibition of histone deacetylase and topoisomerase I.

@article{Yu2014ANS,
  title={A novel small molecule hybrid of vorinostat and DACA displays anticancer activity against human hormone-refractory metastatic prostate cancer through dual inhibition of histone deacetylase and topoisomerase I.},
  author={Chia-Chun Yu and Shiow-Lin Pan and Shi-Wei Chao and S. Liu and J. Hsu and Yu-Chen S. H. Yang and Tsia-Kun Li and W. Huang and J. Guh},
  journal={Biochemical pharmacology},
  year={2014},
  volume={90 3},
  pages={
          320-30
        }
}
  • Chia-Chun Yu, Shiow-Lin Pan, +6 authors J. Guh
  • Published 2014
  • Biology, Medicine
  • Biochemical pharmacology
  • Vorinostat, which is an extensively studied inhibitor against histone deacetylase (HDAC), shows limited clinical activity to solid tumors. WJ35435, a new hybrid of vorinostat and DACA (a topoisomerase inhibitor) potently inhibited HDAC activity (in particular HDAC1 and HDAC6) in kinase assay and cell-based examination. The anti-HDAC effect was confirmed by the induction of histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation. WJ35435 showed better potency than… CONTINUE READING
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