Histone deacetylase inhibitors (HDAC inhibitors, HDACi, HDIs) are chemical compounds that inhibit histone deacetylases. HDIs ... "The Bromodomain Inhibitor JQ1 and the Histone Deacetylase Inhibitor Panobinostat Synergistically Reduce N-Myc Expression and ... The histone deacetylase inhibitors are a new class of cytostatic agents that inhibit the proliferation of tumor cells in ... Histone deacetylase inhibitors exert their anti-tumour effects via the induction of expression changes of oncogenes or tumour ...

Histone acetyltransferase (HAT) Histone deacetylase inhibitor Histone methyltransferase (HMT) Histone-modifying enzymes RNA ... These are just some examples of constantly emerging non-histone, non-chromatin roles for HDACs. Histone deacetylase inhibitors ... "Histone Deacetylases and Mechanisms of Regulation of Gene Expression (Histone deacetylases in cancer)". Crit Rev Oncog. 20 (1-2 ... the histone deacetylases form an ancient protein superfamily known as the histone deacetylase superfamily. HDACs, are ...

... is a drug which acts as a histone deacetylase inhibitor, and was one of the first compounds discovered via high- ... Su GH, Sohn TA, Ryu B, Kern SE (June 2000). "A novel histone deacetylase inhibitor identified by high-throughput ... January 2013). "Scriptaid, a novel histone deacetylase inhibitor, protects against traumatic brain injury via modulation of ... Monneret C (January 2005). "Histone deacetylase inhibitors". European Journal of Medicinal Chemistry. 40 (1): 1-13. doi:10.1016 ...

Bolden, Jessica E.; Peart, Melissa J.; Johnstone, Ricky W. (2006). "Anticancer activities of histone deacetylase inhibitors". ... These modifications are effected by enzymes called histone acetyltransferases (HATs) and histone deacetylases (HDACs). Two ... The Histone Deacetylase Enzymes". Cold Spring Harbor Perspectives in Biology. 6 (4): a018713. doi:10.1101/cshperspect.a018713. ... Another family of deacetylases require NAD+, which transfers an ribosyl group to the acetyl oxygen. Acetate esters and ...

Xu X, Kozikowski AP, Pozzo-Miller L (2014). "A selective histone deacetylase-6 inhibitor improves BDNF trafficking in ... Histone deacetylases (HDACs) are a class of enzymes that remove acetyl groups from histones. Different HDACs play different ... September 2009). "Antidepressant actions of histone deacetylase inhibitors". The Journal of Neuroscience. 29 (37): 11451-60. ... "The potential use of histone deacetylase inhibitors in the treatment of depression". Progress in Neuro-psychopharmacology & ...

Vigushin DM, Coombes RC (January 2002). "Histone deacetylase inhibitors in cancer treatment". Anti-Cancer Drugs. 13 (1): 1-13. ... Cyclin D1 also binds to histone acetylases and histone deacetylases to regulate cell proliferation and cell differentiation ... "Cyclin D1 inhibits peroxisome proliferator-activated receptor gamma-mediated adipogenesis through histone deacetylase ... "Cyclin D1 inhibits peroxisome proliferator-activated receptor gamma-mediated adipogenesis through histone deacetylase ...

It is an inhibitor in vitro of SIRT1, but can be a stimulator in cells. Biological immortality Histone deacetylases or HDACs ... Marks PA, Xu WS (July 2009). "Histone deacetylase inhibitors: Potential in cancer therapy". Journal of Cellular Biochemistry. ... Sirtuins that deacetylate histones are structurally and mechanistically distinct from other classes of histone deacetylases ( ... Yeast Sir2 and some, but not all, sirtuins are protein deacetylases. Unlike other known protein deacetylases, which simply ...

April 2014). "Histone deacetylase inhibitor romidepsin induces HIV expression in CD4 T cells from patients on suppressive ... The trial also compared the effect of romidepsin to another histone deacetylase inhibitor, Vorinostat A study involving ... Masuoka Y, Shindoh N, Inamura N (2008). "Histone deacetylase inhibitors from microorganisms: the Astellas experience". In ... is a novel histone deacetylase inhibitor". Experimental Cell Research. 241 (1): 126-133. doi:10.1006/excr.1998.4027. PMID ...

"DEMETHYLATING AGENTS AND HISTONE DEACETYLASE INHIBITORS AS NEW... by Joana Margarida Jorge". library.ehaweb.org. Retrieved 2022 ... Demethylating Agents and Histone Deacetylase Inhibitors as New Therapeutic Strategies in Chronic Lymphocytic Leukemia". ... Both of these drugs are inhibitors of DNA Methyltransferases (DNMT) which are enzymes that are responsible for methylating DNA ...

Liang D, Kong X, Sang N (November 2006). "Effects of histone deacetylase inhibitors on HIF-1". Cell Cycle. 5 (21): 2430-5. doi: ... scientists found that the continued up-regulation of HIF1A via PHD inhibitors regenerates lost or damaged tissue in mammals ...

... (4SC-201 or RAS2410) is an orally bioavailable inhibitor of histone deacetylases (HDACs), of which inhibitors are ... Tsilimigras, D. I.; Ntanasis-Stathopoulos, I.; Moris, D.; Spartalis, E.; Pawlik, T. M. (2018). "Histone deacetylase inhibitors ... an oral histone deacetylase inhibitor, in patients with advanced solid tumors". Clin Cancer Res. 19 (19): 5494-504. doi:10.1158 ... Histone deacetylase inhibitors, Sulfonamides, Hydroxamic acids, Experimental drugs, Pyrroles, All stub articles, Antineoplastic ...

Methylation inhibitors and histone deacetylase inhibitors, such as valproic acid, increase reelin mRNA levels, while L- ... One study indicated the upregulation of histone deacetylase HDAC1 in the hippocampi of patients. Histone deacetylases suppress ... Valproic acid, a histone deacetylase inhibitor, when taken in combination with antipsychotics, is proposed to have some ... Mitchell CP, Chen Y, Kundakovic M, Costa E, Grayson DR (April 2005). "Histone deacetylase inhibitors decrease reelin promoter ...

"Histone deacetylase inhibitors: mechanisms and clinical significance in cancer: HDAC inhibitor-induced apoptosis". Adv Exp Med ... It is a member of a larger class of histone deacetylase inhibitors (HDIs or HDACIs) that have a broad spectrum of epigenetic ... Drummond DC, Noble CO, Kirpotin DB, Guo Z, Scott GK, Benz CC (2005). "Clinical development of histone deacetylase inhibitors as ... TSA can be used to alter gene expression by interfering with the removal of acetyl groups from histones (histone deacetylases, ...

October 2001). "Histone deacetylase inhibitors arrest polyglutamine-dependent neurodegeneration in Drosophila". Nature. 413 ( ... survival in the presence of mutant huntingtin are correction of transcriptional regulation using histone deacetylase inhibitors ... including protein homeostasis and histone deacetylase inhibition); and strategies to replace lost neurons. In addition, novel ... Selective serotonin reuptake inhibitors and mirtazapine have been recommended for depression, while atypical antipsychotics are ...

... process has been demonstrated to be similar to histone hyperacetylation and it was found that histone de-acetylase inhibitors ... "Histone deacetylase inhibitors promote the tumoricidal effect of HAMLET". Cancer Res. 67 (23): 11327-34. doi:10.1158/0008-5472. ... Hamlet has been shown to bind with high affinity to individual histone proteins, to be specific H2a, H2b, H3, and H4, as well ... Cells also showed decreased levels of mTOR, a known inhibitor of macroautophagy. HAMLET cells and cells under conditions of ...

... is a member of a larger class of compounds that inhibit histone deacetylases (HDAC). Histone deacetylase inhibitors (HDI) have ... Marks PA, Breslow R (January 2007). "Dimethyl sulfoxide to vorinostat: development of this histone deacetylase inhibitor as an ... September 2013). "Development of a histone deacetylase 6 inhibitor and its biological effects". Proceedings of the National ... Bouchecareilh M, Hutt DM, Szajner P, Flotte TR, Balch WE (November 2012). "Histone deacetylase inhibitor (HDACi) ...

The histone deacetylase inhibitor PXD101 synergises with 5-fluorouracil to inhibit colon cancer cell growth in vitro and in ... Belinostat is a histone deacetylase inhibitor (HDACi). TopoTarget expects to launch an initial regulatory study using ... "Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors". Biochemical Journal. ... and commercialization of a group of small molecules that inhibit histone deacetylase (HDAC) enzymes. One of these drugs- ...

"Selectively targeting prostate cancer with antiandrogen equipped histone deacetylase inhibitors". ACS Chem. Biol. 8 (11): 2550- ...

... the Bcl inhibitor produce overall and complete response rates of 33% and 14%, respectively; histone deacetylase inhibitors ... BCL inhibitor venetoclax to block Bcl2's action in promoting B-cell survival and proliferation; 5) histone deacetylase ... encodes histone-lysine N-methyltransferase 2D, a histone methyltransferase which regulates the expression of various genes). ... Phosphoionsitide 3-kinase inhibitors produced overall response rates of 10-12.5 months in 42-59%; tisagenlecleuce cells ...

Histone deacetylases can be regulated by endogenous factors, dietary components, synthetic inhibitors and bacteria-derived ... Mahlknecht U, Will J, Varin A, Hoelzer D, Herbein G (September 2004). "Histone deacetylase 3, a class I histone deacetylase, ... Dashwood RH, Ho E (2007). "Dietary histone deacetylase inhibitors: from cells to mice to man". Semin. Cancer Biol. 17 (5): 363- ... Histone deacetylase 3 is an enzyme encoded by the HDAC3 gene in both humans and mice. Histones are highly alkaline proteins ...

"Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents". J. Hematol. Oncol. 3 (1): 5. doi:10.1186/1756- ... Due to their histone deacetylase (HDAC) inhibitory activity, tremendous effort has been thrust into the synthesis of these ... HDAC inhibitors are therefore thought to increase the expression of tumor suppressor genes, and they are an emerging compound ...

Therefore, histone deacetylase inhibitors may be applied to increase histone acetylation and suppress H3K9 dimethylation, ... June 2007). "Histone deacetylase inhibitors enhance memory and synaptic plasticity via CREB:CBP-dependent transcriptional ... Kazantsev AG, Thompson LM (October 2008). "Therapeutic application of histone deacetylase inhibitors for central nervous system ... this is dependent on rate of transcription HDAC inhibitors do not affect NMDA-R Histone deacetylases (HDAC) remove acetyl ...

2005). "The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic ... Tan J, Cang S, Ma Y, Petrillo RL, Liu D (February 2010). "Novel histone deacetylase inhibitors in clinical trials as anti- ... April 2008). "The histone deacetylase inhibitor ITF2357 selectively targets cells bearing mutated JAK2(V617F)". Leukemia. 22 (4 ... Givinostat (INN) or gavinostat (originally ITF2357) is a histone deacetylase inhibitor with potential anti-inflammatory, anti- ...

Marks PA, Richon VM, Rifkind RA (August 2000). "Histone deacetylase inhibitors: inducers of differentiation or apoptosis of ... HDAC9 histone deacetylase 9". Cai Y, Huang D, Ma W, Wang M, Qin Q, Jiang Z, Liu M (August 2021). "Histone deacetylase 9 ... Histone deacetylase 9 is an enzyme that in humans is encoded by the HDAC9 gene. Histones play a critical role in ... "Association of class II histone deacetylases with heterochromatin protein 1: potential role for histone methylation in control ...

Marks PA, Richon VM, Rifkind RA (August 2000). "Histone deacetylase inhibitors: inducers of differentiation or apoptosis of ... Histone deacetylase 7 is an enzyme that in humans is encoded by the HDAC7 gene. Histones play a critical role in ... "Isolation of a novel histone deacetylase reveals that class I and class II deacetylases promote SMRT-mediated repression". ... "Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity". The Journal ...

"Histone deacetylase inhibitors induce growth arrest and differentiation in uveal melanoma". Clinical Cancer Research. 18 (2): ... Ismail IH, Andrin C, McDonald D, Hendzel MJ (Oct 2010). "BMI1-mediated histone ubiquitylation promotes DNA double-strand break ... "Histone H2A deubiquitinase activity of the Polycomb repressive complex PR-DUB". Nature. 465 (7295): 243-7. Bibcode:2010Natur. ... which controls homeobox genes by regulating the amount of ubiquitinated Histone H2A in Nucleosomes bound to their promoters. In ...

Furthermore, histone deacetylase inhibitors, such as sodium butyrate, strongly upregulate its expression in some cultured cells ... Bordin M, D'Atri F, Guillemot L, Citi S (December 2004). "Histone deacetylase inhibitors up-regulate the expression of tight ...

Histone deacetylase inhibitors and DNA methyltransferase inhibitors are commonly used in the treatment of bipolar disorder. ... Histone deacetylase proteins reverse the acetylation of histone proteins, suppressing DNA expression. Thus, HDAC1 inhibitors ... Lithium is also known as a histone deacetylase inhibitor. In general, selective serotonin reuptake inhibitors are associated ... Acetyl groups on histone proteins can act as binding sites for bromodomain-containing proteins and other chromatin-remodeling ...

Grayson DR, Kundakovic M, Sharma RP (February 2010). "Is there a future for histone deacetylase inhibitors in the ... Histone acetyltransferase Histone deacetylase Histone methylation Acetylation Phosphorylation Nucleosome Watson JD, Baker TA, ... These reactions are typically catalysed by enzymes with "histone acetyltransferase" (HAT) or "histone deacetylase" (HDAC) ... "Histone deacetylase (HDAC) inhibitors attenuate cardiac hypertrophy by suppressing autophagy". Proceedings of the National ...

Using Histone deacetylase (HDAC) inhibitors allows for genes to remain transcriptionally active. HDACi's have been used in ... The idea being that etinostat, a histone deacetylase inhibitor, can prevent the silencing of genes by allowing them to be ... and histone acetylation. Several studies have shown that histone acetyltransferase (HAT) inhibitors are useful in re-inducing ... HDAC inhibitors are also being used, due to the changes in histone acetylation and the increased HDACs observed. While the ...