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Histone deacetylase inhibitor information


Histone deacetylase inhibitors (HDAC inhibitors, HDACi, HDIs) are chemical compounds that inhibit histone deacetylases. Since deacetylation of histones produces transcriptionally silenced heterochromatin, HDIs can render chromatin more transcriptionally active and induce epigenomic changes.

HDIs have a long history of use in psychiatry and neurology as mood stabilizers and anti-epileptics, such as valproic acid. Since at least 2003 they have been investigated as possible treatments for cancers,[1][2] parasitic[3] and inflammatory diseases.[4]

  1. ^ Miller TA, Witter DJ, Belvedere S (November 2003). "Histone deacetylase inhibitors". Journal of Medicinal Chemistry. 46 (24): 5097–116. doi:10.1021/jm0303094. PMID 14613312.
  2. ^ Mwakwari SC, Patil V, Guerrant W, Oyelere AK (2010). "Macrocyclic histone deacetylase inhibitors". Current Topics in Medicinal Chemistry. 10 (14): 1423–40. doi:10.2174/156802610792232079. PMC 3144151. PMID 20536416.
  3. ^ Patil V, Guerrant W, Chen PC, Gryder B, Benicewicz DB, Khan SI, et al. (January 2010). "Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group". Bioorganic & Medicinal Chemistry. 18 (1): 415–25. doi:10.1016/j.bmc.2009.10.042. PMC 2818366. PMID 19914074.
  4. ^ Blanchard F, Chipoy C (February 2005). "Histone deacetylase inhibitors: new drugs for the treatment of inflammatory diseases?". Drug Discovery Today. 10 (3): 197–204. doi:10.1016/S1359-6446(04)03309-4. PMID 15708534.

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Histone deacetylase inhibitor

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Histone deacetylase inhibitors (HDAC inhibitors, HDACi, HDIs) are chemical compounds that inhibit histone deacetylases. Since deacetylation of histones...

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Histone deacetylases (EC 3.5.1.98, HDAC) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on both histone...

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Vorinostat

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member of a larger class of compounds that inhibit histone deacetylases (HDAC). Histone deacetylase inhibitors (HDI) have a broad spectrum of epigenetic...

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Panobinostat

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is a hydroxamic acid and acts as a non-selective histone deacetylase inhibitor (pan-HDAC inhibitor). Panobinostat was approved for medical use in the...

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Givinostat

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is a histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a histone deacetylase (HDAC)...

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carried out by 1) covalent histone modifications by specific enzymes, e.g., histone acetyltransferases (HATs), deacetylases, methyltransferases, and kinases...

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Trichostatin A

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serves as an antifungal antibiotic and selectively inhibits the class I and II mammalian histone deacetylase (HDAC) families of enzymes, but not class III...

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Sodium butyrate

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butyrate treatment of cells results in histone hyperacetylation, and butyrate itself inhibits class I histone deacetylase (HDAC) activity, specifically HDAC1...

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Histone deacetylase 2 (HDAC2) is an enzyme that in humans is encoded by the HDAC2 gene. It belongs to the histone deacetylase class of enzymes responsible...

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Histone deacetylase 5 is an enzyme that in humans is encoded by the HDAC5 gene. Histones play a critical role in transcriptional regulation, cell cycle...

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excretion of excess nitrogen. Sodium phenylbutyrate is also a histone deacetylase inhibitor and chemical chaperone, leading respectively to research into...

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Romidepsin

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from Fujisawa and the University of Tokyo found it to be a histone deacetylase inhibitor with effects similar to those of trichostatin A. Phase I studies...

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Histone acetylation and deacetylation

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catalysed by enzymes with "histone acetyltransferase" (HAT) or "histone deacetylase" (HDAC) activity. Acetylation is the process where an acetyl functional...

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Abexinostat

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cancer as well. Abexinostat exerts its effect as a pan-histone deacetylase inhibitor and inhibits RAD51, which is involved in repairing DNA double strand...

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HDAC3

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Histone deacetylase 3 is an enzyme encoded by the HDAC3 gene in both humans and mice. Histones are highly alkaline proteins that package and order DNA...

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Entinostat

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MS-275, is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers. Entinostat inhibits class I HDAC1 and HDAC3...

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Belinostat

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Belinostat (trade name Beleodaq, previously known as PXD101) is a histone deacetylase inhibitor drug developed by TopoTarget for the treatment of hematological...

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non-small-cell lung carcinoma. The idea being that etinostat, a histone deacetylase inhibitor, can prevent the silencing of genes by allowing them to be accessible...

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Tucidinostat

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Hiyasta) is a histone deacetylase inhibitor (HDI) developed in China. It was also known as HBI-8000. It is a benzamide HDI and inhibits Class I HDAC1...

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new antidepressant treatments. Histone deacetylases (HDACs) are a class of enzymes that remove acetyl groups from histones. Different HDACs play different...

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Butyric acid

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It is also an HDAC inhibitor (specifically, HDAC1, HDAC2, HDAC3, and HDAC8), a drug that inhibits the function of histone deacetylase enzymes, thereby favoring...

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Mocetinostat

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Mocetinostat (MGCD0103) is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers including follicular...

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Hooker lab spanning seven years, wherein small molecule histone deacetylase (HDAC) inhibitors were systematically screened and refined to resolve chemical...

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Addiction

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Warnault V, Buttolo R, Naassila M, Vilpoux C (July 2015). "The histone deacetylase inhibitor sodium butyrate decreases excessive ethanol intake in dependent...

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Valproate

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potential therapeutic mechanism. Valproate is a Histone deacetylase inhibitor. By inhibition of histone deacetylase, it promotes more transcriptionally active...

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HDAC1

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Histone deacetylase 1 (HDAC1) is an enzyme that in humans is encoded by the HDAC1 gene. Histone acetylation and deacetylation, catalyzed by multisubunit...

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Apicidin

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Apicidin is a fungal metabolite, as well as a histone deacetylase inhibitor. Han, J. W.; Ahn, S. H.; Park, S. H.; Wang, S. Y.; Bae, G. U.; Seo, D. W.;...

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Resminostat

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(4SC-201 or RAS2410) is an orally bioavailable inhibitor of histone deacetylases (HDACs), of which inhibitors are antineoplastic agents. In 2011, the German...

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