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The Histone Deacetylase Inhibitor JAHA Down-Regulates pERK and Global DNA Methylation in MDA-MB231 Breast Cancer Cells

1
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), Edificio 16, Università di Palermo, Viale delle Scienze, Palermo 90128, Italy
2
Department of Chemistry, School of Life Sciences, University of Sussex, Falmer, Brighton BN1 9QJ, UK
*
Author to whom correspondence should be addressed.
Academic Editor: Łukasz John
Materials 2015, 8(10), 7041-7047; https://doi.org/10.3390/ma8105358
Received: 29 August 2015 / Revised: 7 October 2015 / Accepted: 9 October 2015 / Published: 16 October 2015
(This article belongs to the Special Issue Organometallic Compounds 2015)
The histone deacetylase inhibitor N1-(ferrocenyl)-N8-hydroxyoctanediamide (JAHA) down-regulates extracellular-signal-regulated kinase (ERK) and its activated form in triple-negative MDA-MB231 breast cancer cells after 18 h and up to 30 h of treatment, and to a lesser extent AKT and phospho-AKT after 30 h and up to 48 h of treatment. Also, DNA methyltransferase 1 (DNMT1), 3b and, to a lesser extent, 3a, downstream ERK targets, were down-regulated already at 18 h with an increase up to 48 h of exposure. Methylation-sensitive restriction arbitrarily-primed (MeSAP) polymerase chain reaction (PCR) analysis confirmed the ability of JAHA to induce genome-wide DNA hypomethylation at 48 h of exposure. Collective data suggest that JAHA, by down-regulating phospho-ERK, impairs DNMT1 and 3b expression and ultimately DNA methylation extent, which may be related to its cytotoxic effect on this cancer cytotype. View Full-Text
Keywords: histone deacetylase inhibitor; extracellular-signal-regulated kinase (ERK); AKT; DNA methyltransferase (DNMT) histone deacetylase inhibitor; extracellular-signal-regulated kinase (ERK); AKT; DNA methyltransferase (DNMT)
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Librizzi, M.; Chiarelli, R.; Bosco, L.; Sansook, S.; Gascon, J.M.; Spencer, J.; Caradonna, F.; Luparello, C. The Histone Deacetylase Inhibitor JAHA Down-Regulates pERK and Global DNA Methylation in MDA-MB231 Breast Cancer Cells. Materials 2015, 8, 7041-7047.

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