4.7 Article

Hydrazones as novel epigenetic modulators: Correlation between TET 1 protein inhibition activity and their iron(II) binding ability

期刊

BIOORGANIC CHEMISTRY
卷 88, 期 -, 页码 -

出版社

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2019.02.034

关键词

Epigenetic; Hydrazone; Inhibitor; Iron(II) affinity; TET 1 protein

资金

  1. Ministry of Education, Youth and Sports of the Czech Republic within the National Sustainability Program II [LQ1604]
  2. project BIOCEV [CZ.1.05/1.1.00/02.0109]
  3. Technology Agency of the Czech Republic [TE01020028]
  4. Ministry of Industry and Trade within project [FV20572]
  5. Ministry of Agriculture of the Czech Republic [QJ1610515]
  6. Charles University in Prague [UNCE 204064, SVV 260 364, PROGRES Q26/LF1]
  7. Operational Programme Prague - Competitiveness [CZ.07.1.02/0.0/0.0/16_040/0000376]
  8. National Programme of Sustainability I - NPU I [LO1601, MSMT-43760/2015]
  9. Ministry of Education, Youth and Sports of the Czech Republic [LM201564]
  10. Agency of the Czech Republic [17-02448S]

向作者/读者索取更多资源

Ten-eleven translocation protein (TET) 1 plays a key role in control of DNA demethylation and thereby of gene expression. Dysregulation of these processes leads to serious pathological states such as oncological and neurodegenerative ones and thus TET 1 targeting is highly requested. Therefore, in this work, we examined the ability of hydrazones (acyl-, aroyl- and heterocyclic hydrazones) to inhibit the TET 1 protein and its mechanism of action. Inhibitory activity of hydrazones 1-7 towards TET 1 was measured. The results showed a high affinity of the tested chelators for iron(II). The study clearly showed a significant correlation between the chelator's affinity for iron(II) ions (represented by the binding constant) and TET 1 protein inhibitory activity (represented by IC50 values).

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