کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1355068 1500447 2016 25 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Inhibitors of histone deacetylase as antitumor agents: A critical review
ترجمه فارسی عنوان
مهار کننده های هیستون دیازتیلاز به عنوان مواد ضد تومور: یک بررسی بحرانی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی


• Histone deacetylase (HDAC) is an interesting target for several cancer types.
• The crystal structure and the biological effects of HDACs are described.
• The chemistry of two classes of HDAC inhibitors, for cancer, are covered in detail.
• Two classes of HDAC inhibitors are short chain fatty acids & hydroxamic acids.

Histone deacetylase (EC 3.5.1.98 – HDAC) is an amidohydrolase involved in deacetylating the histone lysine residues for chromatin remodeling and thus plays a vital role in the epigenetic regulation of gene expression. Due to its aberrant activity and over expression in several forms of cancer, HDAC is considered as a potential anticancer drug target. HDAC inhibitors alter the acetylation status of histone and non-histone proteins to regulate various cellular events such as cell survival, differentiation and apoptosis in tumor cells and thus exhibit anticancer activity. Till date, four drugs, namely Vorinostat (SAHA), Romidepsin (FK-228), Belinostat (PXD-101) and Panobinostat (LBH-589) have been granted FDA approval for cancer and several HDAC inhibitors are currently in various phases of clinical trials, either as monotherapy and/or in combination with existing/novel anticancer agents. Regardless of this, today scientific efforts have fortified the quest for newer and novel HDAC inhibitors that show isoform selectivity. This review focuses on the chemistry of the molecules of two classes of HDAC inhibitors, namely short chain fatty acids and hydroxamic acids, investigated so far as novel therapeutic agents for cancer.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic Chemistry - Volume 67, August 2016, Pages 18–42
نویسندگان
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