کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1984332 | 1539973 | 2007 | 18 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
MS-275, a potent orally available inhibitor of histone deacetylases-The development of an anticancer agent
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کلمات کلیدی
SAHAAMLFDAMS-275CTCLCLLDLTMTDPBMCsMDSTSAEGFRHDACsCRACPACyproterone acetate - استات سایپروترونGene expression - بیان ژنTrichostatin A - تریکوستاتین AMaximum tolerated dose - حداکثر دوز قابل تحملdose limiting toxicity - دوز محدودیت سمیتCancer - سرطانperipheral blood mononuclear cells - سلول های تک هسته ای خون محیطیTRAIL - قطارCutaneous T-cell lymphoma - لنفوم پوستی Tacute myeloid leukemia - لوسمی حاد میلوئیدی یا به اختصار AMLChronic lymphocytic leukemia - لوسمی مزمن لنفوئیدیhistone deacetylase inhibitors - مهار کننده های هیستون داستیلازhistone deacetylases - هیستون deacetylaseshistone acetyltransferases - هیستون استیل ترانسفرازChromatin - کروماتینHATs - کلاه
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
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چکیده انگلیسی
In the last few years it was found that beside genetic aberrations, epigenetic changes also play an important role in tumorigenesis. Acetylation and deacetylation of histones have been found to contribute to a significant extent to epigenetic regulation of gene expression. Analyses of various tumor models and patient samples revealed that the enzyme class of histone deacetylases is associated with many types of cancer and that, for example, over-expression of these enzymes leads to a disturbed balance between acetylation and deacetylation of histones, resulting in differences in the gene expression patterns between normal and cancer cells. Consequently, this class of enzymes has been considered as a potential target for cancer therapy. Numerous inhibitors have been identified and several are in clinical development. Although, with SAHA, one inhibitor has been approved by the FDA for a tumor indication, many open questions remain regarding the mode of action of these inhibitors. In this review, various aspects of preclinical and clinical research of the HDAC inhibitor MS-275 are described, to provide insight into the development of such a compound.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: The International Journal of Biochemistry & Cell Biology - Volume 39, Issues 7â8, JulyâAugust 2007, Pages 1388-1405
Journal: The International Journal of Biochemistry & Cell Biology - Volume 39, Issues 7â8, JulyâAugust 2007, Pages 1388-1405
نویسندگان
Holger Hess-Stumpp, Tomke Ute Bracker, David Henderson, Oliver Politz,