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Review
. 2019 May 16;11(1):81.
doi: 10.1186/s13148-019-0675-4.

Epigenetics in cancer therapy and nanomedicine

Annalisa Roberti  1 , Adolfo F Valdes  2 , Ramón Torrecillas  2 , Mario F Fraga  3 , Agustin F Fernandez  4
Affiliations
Review

Epigenetics in cancer therapy and nanomedicine

Annalisa Roberti et al. Clin Epigenetics. .

Abstract

The emergence of nanotechnology applied to medicine has revolutionized the treatment of human cancer. As in the case of classic drugs for the treatment of cancer, epigenetic drugs have evolved in terms of their specificity and efficiency, especially because of the possibility of using more effective transport and delivery systems. The use of nanoparticles (NPs) in oncology management offers promising advantages in terms of the efficacy of cancer treatments, but it is still unclear how these NPs may be affecting the epigenome such that safe routine use is ensured. In this work, we summarize the importance of the epigenetic alterations identified in human cancer, which have led to the appearance of biomarkers or epigenetic drugs in precision medicine, and we describe the transport and release systems of the epigenetic drugs that have been developed to date.

Keywords: DNMT inhibitors; Epigenetics; HDCA inhibitors; Nanocarriers; Nanomedicine; Nanoparticles.

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Conflict of interest statement

The authors declare that they have no competing interests.

Figures

Fig. 1
Fig. 1
Epigenetic mechanisms contributing to gene regulation. DNA methylation, histone modifications, and noncoding RNAs (ncRNAs)
Fig. 2
Fig. 2
Examples of epigenetic alterations in cancer cells. Hypermethylation of promoters of tumor suppressor genes, global loss of H4K20me3 and H4K16ac, and up- or downregulation of miRNAs that target oncogenes and tumor suppressor genes, respectively
Fig. 3
Fig. 3
Examples of epigenetic drugs and their general mechanisms of action. Some of these drugs are approved by USFDA, and others are currently in clinical trials
Fig. 4
Fig. 4
External factors that affect the epigenome. Although the associations between exposure to various external factors and alterations in the human epigenome, with consequent risk to health, have been demonstrated, in the case of nanoparticles, these associations have not been well studied
Fig. 5
Fig. 5
Schematic representation of the different types of nanocarriers for epigenetic therapy in cancer. a Vehicles for transport and delivery of iDNMTs in poly(lactic-co-glycolic acid) (PLGA)- and poly(ethylene glycol) (PEG)-based nanomicelles, in gelatinase with PEG and poly-ε-caprolactone (PCL), and in alendronate-PEG-2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE). b Vehicles for transport and delivery of iHDACs in hyaluronic acid (HA)-coated cationic solid lipid (SL) nanoparticles (didecyldimethyl ammonium bromide (DDAB) is used as cationic lipid), in micelles based on SAHA-based prodrug polymer (POEG-b-PSAHA) (POEG: poly(oligo(ethylene glycol) methacrylate)), and in a PLGA-lecithin-PEG core-shell system (DSPE: 1,2-dioctadecanoyl-sn-glycero-3-phosphoethanolamine). c Vehicles for transport and delivery of siRNA in cationic cyclodextrin-based polymer (CDP) modified with a terminal adamantane group (AD-PEG) and some AD-PEG conjugated to human transferrin (Th), in PEGylated liposomes, in single-walled nanotubes (SWNTs) functionalized with PEG-DSPE and polymer poly(allylamine hydrochloride) (PAH), and in exosome-based systems
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References

    1. Alabert C, Barth TK, Reveron-Gomez N, Sidoli S, Schmidt A, Jensen ON, Imhof A, Groth A. Two distinct modes for propagation of histone PTMs across the cell cycle. Genes Dev. 2015;29(6):585–590. doi: 10.1101/gad.256354.114. - DOI - PMC - PubMed
    1. Bernstein BE, Meissner A, Lander ES. The mammalian epigenome. Cell. 2007;128(4):669–681. doi: 10.1016/j.cell.2007.01.033. - DOI - PubMed
    1. Budhavarapu VN, Chavez M, Tyler JK. How is epigenetic information maintained through DNA replication? Epigenetics Chromatin. 2013;6(1):32. doi: 10.1186/1756-8935-6-32. - DOI - PMC - PubMed
    1. Hathaway NA, Bell O, Hodges C, Miller EL, Neel DS, Crabtree GR. Dynamics and memory of heterochromatin in living cells. Cell. 2012;149(7):1447–1460. doi: 10.1016/j.cell.2012.03.052. - DOI - PMC - PubMed
    1. Zhu B, Reinberg D. Epigenetic inheritance: uncontested? Cell Res. 2011;21(3):435–441. doi: 10.1038/cr.2011.26. - DOI - PMC - PubMed

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