Hydrazones as novel epigenetic modulators: Correlation between TET 1 protein inhibition activity and their iron(II) binding ability.
Bioorg Chem
; 88: 102809, 2019 07.
Article
en En
| MEDLINE
| ID: mdl-30999246
ABSTRACT
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).
Palabras clave
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Quelantes del Hierro
/
Dioxigenasas
/
Inhibidores Enzimáticos
/
Hidrazonas
Idioma:
En
Revista:
Bioorg Chem
Año:
2019
Tipo del documento:
Article