Histone Deacetylase Inhibitors as Anticancer Drugs
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چکیده
منابع مشابه
Histone Deacetylase Inhibitors as Anticancer Drugs
Carcinogenesis cannot be explained only by genetic alterations, but also involves epigenetic processes. Modification of histones by acetylation plays a key role in epigenetic regulation of gene expression and is controlled by the balance between histone deacetylases (HDAC) and histone acetyltransferases (HAT). HDAC inhibitors induce cancer cell cycle arrest, differentiation and cell death, redu...
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Histone deacetylase inhibitors represent a promising new class of compounds for the treatment of cancer. Inhibitors of this kind currently under clinical evaluation mainly target the classical (Rpd3/Hda1) family of histone deacetylases. Of particular note, the U.S. Food and Drug Administration recently approved the first histone deacetylase inhibitor (Zolinza: Merck and Co., Whitehouse Station,...
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Histone deacetylase (HDAC) inhibitors are an emerging class of therapeutics with potential as anticancer drugs. The rationale for developing HDAC inhibitors (and other chromatin-modifying agents) as anticancer therapies arose from the understanding that in addition to genetic mutations, epigenetic changes such as dysregulation of HDAC enzymes can alter phenotype and gene expression, disturb hom...
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During the past decade, a number of HDAC inhibitors have been identified that induce tumor cells in culture and in tumor-bearing animals to undergo growth arrest, differentiation, and/or apoptotic cell death (1). Acetylation and deacetylation of histones, part of the core proteins of nucleosomes, play an important role in the regulation of gene expression (2). There are two classes of enzymes i...
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In cancer cells, an imbalance often exists between histone acetyltransferase (HAT) and histone deacetylase (HDAC) activities, and various drug companies are actively seeking competitive HDAC inhibitors for chemotherapeutic intervention. Cancer cells appear to be more sensitive than nontransformed cells to HDAC inhibitors, which disrupt the cell cycle and induce apoptosis via derepression of gen...
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ژورنال
عنوان ژورنال: International Journal of Molecular Sciences
سال: 2017
ISSN: 1422-0067
DOI: 10.3390/ijms18071414