Structurally designed trans-2-phenylcyclopropylamine derivatives potently inhibit histone demethylase LSD1/KDM1 .

@article{Mimasu2010StructurallyDT,
  title={Structurally designed trans-2-phenylcyclopropylamine derivatives potently inhibit histone demethylase LSD1/KDM1 .},
  author={Shinya Mimasu and Naoki Umezawa and Seichi Sato and Tsunehiko Higuchi and Takashi Umehara and Shigeyuki Yokoyama},
  journal={Biochemistry},
  year={2010},
  volume={49 30},
  pages={
          6494-503
        }
}
Lysine-specific demethylase 1 (LSD1/KDM1) demethylates histone H3, in addition to tumor suppressor p53 and DNA methyltransferase 1 (Dnmt1), thus regulating eukaryotic gene expression by altering chromatin structure. Specific inhibitors of LSD1 are desired as anticancer agents, because LSD1 aberrations are associated with several cancers, and LSD1 inhibition restores the expression of abnormally silenced genes in cancerous cells. In this study, we designed and synthesized several candidate… CONTINUE READING
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