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Statins do not directly inhibit the activity of major epigenetic modifying enzymes


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Bridgeman, S, Northrop, W, Ellison, G, Sabapathy, T, Melton, PE ORCID: 0000-0003-4026-2964, Newsholme, P and Mamotte, CDS 2019 , 'Statins do not directly inhibit the activity of major epigenetic modifying enzymes' , Cancers, vol. 11, no. 4 , pp. 1-14 , doi: 10.3390/cancers11040516.

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The potential anticancer effects of statins—a widely used class of cholesterol loweringdrugs—has generated significant interest, as has the use of epigenetic modifying drugs such asHDAC and DNMT inhibitors. We set out to investigate the effect of statin drugs on epigeneticmodifications in multiple cell lines, including hepatocellular carcinoma, breast carcinoma, leukemicmacrophages, cervical adenocarcinoma, and insulin-secreting cells, as well as liver extracts fromstatin-treated C57B1/6J mice. Cells or cell extracts were treated with statins and with establishedepigenetic modulators, and HDAC, HAT, and DNMT activities were quantified. We also examinedhistone acetylation by immunoblotting. Statins altered neither HDAC nor HAT activity. Accordingly,acetylation of histones H3 and H4 was unchanged with statin treatment. However, statins tended toincrease DNMT activity. These results indicate that direct inhibition of the major classes of epigeneticmodifying enzymes, as previously reported elsewhere, is unlikely to contribute to any anticancereffects of statins. This study concerned global effects on epigenetic enzyme activities and histoneacetylation; whether statins influence epigenetic modifications in certain genomic regions, cannot beruled out and remains to be investigated.

Item Type: Article
Authors/Creators:Bridgeman, S and Northrop, W and Ellison, G and Sabapathy, T and Melton, PE and Newsholme, P and Mamotte, CDS
Keywords: DNA methylation D,NMT inhibitors, HDAC inhibitors, HMG-CoA reductase inhibitors, epigenetics, histone acetylation
Journal or Publication Title: Cancers
Publisher: MDPI
ISSN: 2072-6694
DOI / ID Number: 10.3390/cancers11040516
Copyright Information:

Copyright 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution(CC BY) license (

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