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Demethylating Agents in the Treatment of Cancer

Gene silencing resulting from aberrant DNA methylation can lead to tumorigenesis. Therefore, drugs that inhibit or interfere with DNA methylation have been used to reactivate and induce silenced gene re-expression in malignancies. Two demethylating agents, azacitidine and decitabine, are approved fo...

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Detalles Bibliográficos
Autores principales: Howell, Paul M., Liu, Zixing, Khong, Hung T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2010
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4036667/
https://www.ncbi.nlm.nih.gov/pubmed/27713340
http://dx.doi.org/10.3390/ph3072022
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author Howell, Paul M.
Liu, Zixing
Khong, Hung T.
author_facet Howell, Paul M.
Liu, Zixing
Khong, Hung T.
author_sort Howell, Paul M.
collection PubMed
description Gene silencing resulting from aberrant DNA methylation can lead to tumorigenesis. Therefore, drugs that inhibit or interfere with DNA methylation have been used to reactivate and induce silenced gene re-expression in malignancies. Two demethylating agents, azacitidine and decitabine, are approved for the treatment of myelodysplastic syndromes (MDS) by the U.S. Food and Drug Administration (FDA), and are now considered the standard of care in MDS. In this review, we discuss clinical data, including clinical benefits and toxicities, which led to the approval of azacitidine and decitabine. We also summarize findings from clinical trials that used these two demethylating agents in the treatment of solid tumors. Lastly, we discuss some limitations in the use of azacitidine and decitabine in cancer therapy.
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spelling pubmed-40366672014-05-28 Demethylating Agents in the Treatment of Cancer Howell, Paul M. Liu, Zixing Khong, Hung T. Pharmaceuticals (Basel) Review Gene silencing resulting from aberrant DNA methylation can lead to tumorigenesis. Therefore, drugs that inhibit or interfere with DNA methylation have been used to reactivate and induce silenced gene re-expression in malignancies. Two demethylating agents, azacitidine and decitabine, are approved for the treatment of myelodysplastic syndromes (MDS) by the U.S. Food and Drug Administration (FDA), and are now considered the standard of care in MDS. In this review, we discuss clinical data, including clinical benefits and toxicities, which led to the approval of azacitidine and decitabine. We also summarize findings from clinical trials that used these two demethylating agents in the treatment of solid tumors. Lastly, we discuss some limitations in the use of azacitidine and decitabine in cancer therapy. MDPI 2010-07-02 /pmc/articles/PMC4036667/ /pubmed/27713340 http://dx.doi.org/10.3390/ph3072022 Text en © 2010 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an Open Access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Review
Howell, Paul M.
Liu, Zixing
Khong, Hung T.
Demethylating Agents in the Treatment of Cancer
title Demethylating Agents in the Treatment of Cancer
title_full Demethylating Agents in the Treatment of Cancer
title_fullStr Demethylating Agents in the Treatment of Cancer
title_full_unstemmed Demethylating Agents in the Treatment of Cancer
title_short Demethylating Agents in the Treatment of Cancer
title_sort demethylating agents in the treatment of cancer
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4036667/
https://www.ncbi.nlm.nih.gov/pubmed/27713340
http://dx.doi.org/10.3390/ph3072022
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