Hydrazones as novel epigenetic modulators: Correlation between TET 1 protein inhibition activity and their iron(II) binding ability
Jazyk angličtina Země Spojené státy americké Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
30999246
DOI
10.1016/j.bioorg.2019.02.034
PII: S0045-2068(18)31169-6
Knihovny.cz E-zdroje
- Klíčová slova
- Epigenetic, Hydrazone, Inhibitor, Iron(II) affinity, TET 1 protein,
- MeSH
- chelátory železa chemická syntéza chemie toxicita MeSH
- dioxygenasy antagonisté a inhibitory chemie MeSH
- enzymatické testy MeSH
- epigeneze genetická účinky léků MeSH
- hydrazony chemická syntéza chemie toxicita MeSH
- inhibitory enzymů chemická syntéza chemie toxicita MeSH
- železo chemie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- chelátory železa MeSH
- dioxygenasy MeSH
- hydrazony MeSH
- inhibitory enzymů MeSH
- železo MeSH
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).
Research and Development Center C2P s r o Jungmannova 101 503 51 Chlumec nad Cidlinou Czech Republic
Citace poskytuje Crossref.org
Targeting of the Mitochondrial TET1 Protein by Pyrrolo[3,2-b]pyrrole Chelators
