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Insights into novel emerging epigenetic drugs in myeloid malignancies

Epigenetics has been defined as ‘a stably heritable phenotype resulting from changes in a chromosome without alterations in the DNA sequence’ and several epigenetic regulators are recurrently mutated in hematological malignancies. Epigenetic modifications include changes such as DNA methylation, his...

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Detalles Bibliográficos
Autores principales: Chandhok, Namrata S., Prebet, Thomas
Formato: Online Artículo Texto
Lenguaje:English
Publicado: SAGE Publications 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6685116/
https://www.ncbi.nlm.nih.gov/pubmed/31431820
http://dx.doi.org/10.1177/2040620719866081
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author Chandhok, Namrata S.
Prebet, Thomas
author_facet Chandhok, Namrata S.
Prebet, Thomas
author_sort Chandhok, Namrata S.
collection PubMed
description Epigenetics has been defined as ‘a stably heritable phenotype resulting from changes in a chromosome without alterations in the DNA sequence’ and several epigenetic regulators are recurrently mutated in hematological malignancies. Epigenetic modifications include changes such as DNA methylation, histone modifications and RNA associated gene silencing. Transcriptional regulation, chromosome stability, DNA replication and DNA repair are all controlled by these modifications. Mutations in genes encoding epigenetic modifiers are a frequent occurrence in hematologic malignancies and important in both the initiation and progression of cancer. Epigenetic modifications are also frequently reversible, allowing excellent opportunities for therapeutic intervention. The goal of epigenetic therapies is to reverse epigenetic dysregulation, restore the epigenetic balance, and revert malignant cells to a more normal condition. The role of epigenetic therapies thus far is most established in hematologic malignancies, with several agents already approved by the US Food and Drug Administration. In this review, we discuss pharmacological agents targeting epigenetic regulators.
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spelling pubmed-66851162019-08-20 Insights into novel emerging epigenetic drugs in myeloid malignancies Chandhok, Namrata S. Prebet, Thomas Ther Adv Hematol Review Epigenetics has been defined as ‘a stably heritable phenotype resulting from changes in a chromosome without alterations in the DNA sequence’ and several epigenetic regulators are recurrently mutated in hematological malignancies. Epigenetic modifications include changes such as DNA methylation, histone modifications and RNA associated gene silencing. Transcriptional regulation, chromosome stability, DNA replication and DNA repair are all controlled by these modifications. Mutations in genes encoding epigenetic modifiers are a frequent occurrence in hematologic malignancies and important in both the initiation and progression of cancer. Epigenetic modifications are also frequently reversible, allowing excellent opportunities for therapeutic intervention. The goal of epigenetic therapies is to reverse epigenetic dysregulation, restore the epigenetic balance, and revert malignant cells to a more normal condition. The role of epigenetic therapies thus far is most established in hematologic malignancies, with several agents already approved by the US Food and Drug Administration. In this review, we discuss pharmacological agents targeting epigenetic regulators. SAGE Publications 2019-08-06 /pmc/articles/PMC6685116/ /pubmed/31431820 http://dx.doi.org/10.1177/2040620719866081 Text en © The Author(s), 2019 http://www.creativecommons.org/licenses/by-nc/4.0/ This article is distributed under the terms of the Creative Commons Attribution-NonCommercial 4.0 License (http://www.creativecommons.org/licenses/by-nc/4.0/) which permits non-commercial use, reproduction and distribution of the work without further permission provided the original work is attributed as specified on the SAGE and Open Access pages (https://us.sagepub.com/en-us/nam/open-access-at-sage).
spellingShingle Review
Chandhok, Namrata S.
Prebet, Thomas
Insights into novel emerging epigenetic drugs in myeloid malignancies
title Insights into novel emerging epigenetic drugs in myeloid malignancies
title_full Insights into novel emerging epigenetic drugs in myeloid malignancies
title_fullStr Insights into novel emerging epigenetic drugs in myeloid malignancies
title_full_unstemmed Insights into novel emerging epigenetic drugs in myeloid malignancies
title_short Insights into novel emerging epigenetic drugs in myeloid malignancies
title_sort insights into novel emerging epigenetic drugs in myeloid malignancies
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6685116/
https://www.ncbi.nlm.nih.gov/pubmed/31431820
http://dx.doi.org/10.1177/2040620719866081
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