Epigenetic Therapy of Cancer

Avendaño, Carmen; Menéndez, J. Carlos

doi:10.1016/b978-0-444-62649-3.00008-9

Cited by 2 publications

(2 citation statements)

References 98 publications

(60 reference statements)

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“…Cancer development and progression is not only confined to genetic changes, but also involves epigenetic changes, leading to alterations in gene expression and cell phenotypes. Epigenetics is concerned with the heritable phenotypes based on changes in chromosome, as opposed to genetics, whose realm is on the basis of alterations in the primary DNA sequence (Avendaño and Menéndez, 2015, Berger et al, 2009). Alterations in the structure and modification status of chromatin represent powerful regulatory mechanisms for gene expression and genome stability (Avendaño and Menéndez, 2015).…”

Section: Introductionmentioning

confidence: 99%

“…Epigenetics is concerned with the heritable phenotypes based on changes in chromosome, as opposed to genetics, whose realm is on the basis of alterations in the primary DNA sequence (Avendaño and Menéndez, 2015, Berger et al, 2009). Alterations in the structure and modification status of chromatin represent powerful regulatory mechanisms for gene expression and genome stability (Avendaño and Menéndez, 2015). The major epigenetic modifications in mammals, and particularly in humans, are DNA methylation and post-translational histone modifications (acetylation, methylation, phosphorylation etc.)…”

Section: Introductionmentioning

confidence: 99%

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Pendant HDAC inhibitor SAHA derivatised polymer as a novel prodrug micellar carrier for anticancer drugs

Sun

Wang

et al. 2017

Journal of Drug Targeting

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Suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor (HDACi) approved by FDA for the treatment of cutaneous T cell lymphoma, is a promising anticancer drug for various cancers with a unique mode of action. However, it demonstrates limited clinical benefits in solid tumours as a single drug. In order to achieve enhanced and synergistic co-delivery of SAHA and doxorubicin (DOX), a cleavable SAHA-based prodrug polymer (POEG-b-PSAHA), consisting of hydrophilic poly(oligo(ethylene glycol) methacrylate) (POEG) blocks and hydrophobic SAHA segments, has been developed. POEG-b-PSAHA prodrug polymer was able to form spherical micelles with a diameter around 60 nm and well retained the pharmacological activity of SAHA in either inhibiting the proliferation of tumour cells or inducing histone acetylation. DOX formulated in POEG-b-PSAHA-based micelles showed a sustained release profile. DOX-loaded POEG-b-PSAHA exhibited more potent cytotoxicity towards tumour cells than free DOX and DOX loaded in a pharmacologically 'inert' nanocarrier, POEG-b-POM. Consistently, DOX/POEG-b-PSAHA formulation resulted in an improved therapeutic effect in vivo compared to free DOX, Doxil or DOX formulated in POEG-b-POM micelles. These results suggest that SAHA-based prodrug micelles may serve as a dual functional carrier for combination strategies in epigenetic-oriented anticancer therapy.

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Section: Introductionmentioning

confidence: 99%