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]
^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.
^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.
^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.
^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.
and 28 Related for: Histone deacetylase inhibitor information
Histonedeacetylases (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...
member of a larger class of compounds that inhibithistonedeacetylases (HDAC). Histonedeacetylaseinhibitors (HDI) have a broad spectrum of epigenetic...
is a histonedeacetylaseinhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a histonedeacetylase (HDAC)...
carried out by 1) covalent histone modifications by specific enzymes, e.g., histone acetyltransferases (HATs), deacetylases, methyltransferases, and kinases...
serves as an antifungal antibiotic and selectively inhibits the class I and II mammalian histonedeacetylase (HDAC) families of enzymes, but not class III...
butyrate treatment of cells results in histone hyperacetylation, and butyrate itself inhibits class I histonedeacetylase (HDAC) activity, specifically HDAC1...
Histonedeacetylase 2 (HDAC2) is an enzyme that in humans is encoded by the HDAC2 gene. It belongs to the histonedeacetylase class of enzymes responsible...
Histonedeacetylase 5 is an enzyme that in humans is encoded by the HDAC5 gene. Histones play a critical role in transcriptional regulation, cell cycle...
excretion of excess nitrogen. Sodium phenylbutyrate is also a histonedeacetylaseinhibitor and chemical chaperone, leading respectively to research into...
from Fujisawa and the University of Tokyo found it to be a histonedeacetylaseinhibitor with effects similar to those of trichostatin A. Phase I studies...
catalysed by enzymes with "histone acetyltransferase" (HAT) or "histonedeacetylase" (HDAC) activity. Acetylation is the process where an acetyl functional...
cancer as well. Abexinostat exerts its effect as a pan-histonedeacetylaseinhibitor and inhibits RAD51, which is involved in repairing DNA double strand...
Histonedeacetylase 3 is an enzyme encoded by the HDAC3 gene in both humans and mice. Histones are highly alkaline proteins that package and order DNA...
MS-275, is a benzamide histonedeacetylaseinhibitor undergoing clinical trials for treatment of various cancers. Entinostat inhibits class I HDAC1 and HDAC3...
Belinostat (trade name Beleodaq, previously known as PXD101) is a histonedeacetylaseinhibitor drug developed by TopoTarget for the treatment of hematological...
non-small-cell lung carcinoma. The idea being that etinostat, a histonedeacetylaseinhibitor, can prevent the silencing of genes by allowing them to be accessible...
new antidepressant treatments. Histonedeacetylases (HDACs) are a class of enzymes that remove acetyl groups from histones. Different HDACs play different...
It is also an HDAC inhibitor (specifically, HDAC1, HDAC2, HDAC3, and HDAC8), a drug that inhibits the function of histonedeacetylase enzymes, thereby favoring...
Hooker lab spanning seven years, wherein small molecule histonedeacetylase (HDAC) inhibitors were systematically screened and refined to resolve chemical...
Warnault V, Buttolo R, Naassila M, Vilpoux C (July 2015). "The histonedeacetylaseinhibitor sodium butyrate decreases excessive ethanol intake in dependent...
potential therapeutic mechanism. Valproate is a Histonedeacetylaseinhibitor. By inhibition of histonedeacetylase, it promotes more transcriptionally active...
Histonedeacetylase 1 (HDAC1) is an enzyme that in humans is encoded by the HDAC1 gene. Histone acetylation and deacetylation, catalyzed by multisubunit...
Apicidin is a fungal metabolite, as well as a histonedeacetylaseinhibitor. Han, J. W.; Ahn, S. H.; Park, S. H.; Wang, S. Y.; Bae, G. U.; Seo, D. W.;...
(4SC-201 or RAS2410) is an orally bioavailable inhibitor of histonedeacetylases (HDACs), of which inhibitors are antineoplastic agents. In 2011, the German...