histone deacetylase inhibitors


Summary: Compounds that inhibit HISTONE DEACETYLASES. This class of drugs may influence gene expression by increasing the level of acetylated HISTONES in specific CHROMATIN domains.

Top Publications

  1. Ogryzko V, Hirai T, Russanova V, Barbie D, Howard B. Human fibroblast commitment to a senescence-like state in response to histone deacetylase inhibitors is cell cycle dependent. Mol Cell Biol. 1996;16:5210-8 pubmed
    ..Two histone deacetylase inhibitors, sodium butyrate and trichostatin A, dramatically reduce the HDF proliferative life span in a manner ..
  2. Choi S, Braun T, Henig I, Gatza E, Magenau J, Parkin B, et al. Vorinostat plus tacrolimus/methotrexate to prevent GVHD after myeloablative conditioning, unrelated donor HCT. Blood. 2017;130:1760-1767 pubmed publisher
    ..Vorinostat for GVHD prevention is an effective strategy that should be confirmed in a randomized phase 3 study. This trial was registered at www.clinicaltrials.gov as #NCT01790568. ..
  3. Eichenauer D, Engert A. The evolving role of targeted drugs in the treatment of Hodgkin lymphoma. Expert Rev Hematol. 2017;10:775-782 pubmed publisher
    ..Expert commentary: A multitude of targeted drugs are investigated in HL. Promising data have particularly emerged from studies with BV and anti-PD-1 antibodies. However, mature data needed for final conclusions are still pending. ..
  4. Gao S, Zang J, Gao Q, Liang X, Ding Q, Li X, et al. Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. Bioorg Med Chem. 2017;25:2981-2994 pubmed publisher
    ..163, 0.396 and 0.605µM, respectively), compound 9n with IC50 values of 0.032, 0.256 and 0.311µM for HDAC1, 2 and 3 respectively, showed a moderate HDAC1 selectivity. ..
  5. Dong Q, Sharma S, Liu H, Chen L, Gu B, Sun X, et al. HDAC inhibitors reverse acquired radio resistance of KYSE-150R esophageal carcinoma cells by modulating Bmi-1 expression. Toxicol Lett. 2014;224:121-9 pubmed
    ..Although histone deacetylase inhibitors (HDIs) have been demonstrated to sensitize intrinsic radioresistant cancer cell lines to IR, little is ..
  6. Carlomagno Y, Chung D, Yue M, Castanedes Casey M, Madden B, Dunmore J, et al. An acetylation-phosphorylation switch that regulates tau aggregation propensity and function. J Biol Chem. 2017;292:15277-15286 pubmed publisher
  7. Dendoncker K, Timmermans S, Van Looveren K, De Cauwer L, De Bosscher K, Libert C. The nature of the GRE influences the screening for GR-activity enhancing modulators. PLoS ONE. 2017;12:e0181101 pubmed publisher
    ..b>Histone deacetylase inhibitors (HDACi) such as Vorinostat and Belinostat are two broad-spectrum HDACi that strongly increased the Dex-..
  8. Kovalev R, Stam T, Ibatulin F, Bondarev G, Filatov M. [Possibilities of epigenetic anti-tumor therapy in in-vitro models]. Vopr Onkol. 2012;58:800-7 pubmed
    ..b>Histone deacetylase inhibitors (HDACi) comprise structurally diverse compounds that are a group of targeted epigenetic anticancer ..
  9. Treppendahl M, Kristensen L, Grønbæk K. Predicting response to epigenetic therapy. J Clin Invest. 2014;124:47-55 pubmed publisher
    ..Here we provide an overview of markers that may predict the efficacy of FDA- and EMA-approved epigenetic drugs. ..

More Information


  1. Xie R, Yao Y, Tang P, Chen G, Liu X, Yun F, et al. Design, synthesis and biological evaluation of novel hydroxamates and 2-aminobenzamides as potent histone deacetylase inhibitors and antitumor agents. Eur J Med Chem. 2017;134:1-12 pubmed publisher
    ..Furthermore, 12a remarkably induced apoptosis and G2/M phase cell cycle arrest in A549 cancer cells. Those results indicated that compound 12a could be a promising candidate for treatment of cancer. ..
  2. Richardson P, Roy A, Acharyya S, Panneerselvam A, Mendelson E, Gunther A, et al. Treatment-free interval as a metric of patient experience and a health outcome of value for advanced multiple myeloma: the case for the histone deacetylase inhibitor panobinostat, a next-generation novel agent. Expert Rev Hematol. 2017;10:933-939 pubmed publisher
    ..TFI has not been traditionally measured in clinical trials, but should be assessed in prospective data collection given its value to payers, providers, and patients. ..
  3. She A, Kurtser I, Reis S, Hennig K, Lai J, Lang A, et al. Selectivity and Kinetic Requirements of HDAC Inhibitors as Progranulin Enhancers for Treating Frontotemporal Dementia. Cell Chem Biol. 2017;24:892-906.e5 pubmed publisher
    ..These findings have implications for epigenetic and cis-regulatory mechanisms controlling human GRN expression and may advance translational efforts to develop targeted therapeutics for treating PGRN-deficient FTD. ..
  4. Nagaraja S, Vitanza N, Woo P, Taylor K, Liu F, Zhang L, et al. Transcriptional Dependencies in Diffuse Intrinsic Pontine Glioma. Cancer Cell. 2017;31:635-652.e6 pubmed publisher
    ..The findings presented demonstrate transcriptional vulnerabilities and elucidate previously unknown mechanisms of DIPG pathobiology. ..
  5. Gardner E, Poirier J, Rudin C. Histone Code Aberrancies in Small Cell Lung Cancer. J Thorac Oncol. 2017;12:599-601 pubmed publisher
  6. Zhang Y, Ren J. Targeting autophagy for the therapeutic application of histone deacetylase inhibitors in ischemia/reperfusion heart injury. Circulation. 2014;129:1088-91 pubmed publisher
  7. Ahuja N, Easwaran H, Baylin S. Harnessing the potential of epigenetic therapy to target solid tumors. J Clin Invest. 2014;124:56-63 pubmed publisher
  8. Cosenza M, Civallero M, Marcheselli L, Sacchi S, Pozzi S. Ricolinostat, a selective HDAC6 inhibitor, shows anti-lymphoma cell activity alone and in combination with bendamustine. Apoptosis. 2017;22:827-840 pubmed publisher
    b>Histone deacetylase inhibitors (HDACis) have emerged as a new class of anticancer agents, targeting the biological process including cell cycle and apoptosis...
  9. Mishra V, Wegwitz F, Kosinsky R, Sen M, Baumgartner R, Wulff T, et al. Histone deacetylase class-I inhibition promotes epithelial gene expression in pancreatic cancer cells in a BRD4- and MYC-dependent manner. Nucleic Acids Res. 2017;45:6334-6349 pubmed publisher
    ..Taken together, our study uncovers a previously unknown role of BRD4 and MYC in eliciting the HDACi-mediated induction of a subset of genes and provides molecular insight into the mechanisms of HDACi action in PDAC. ..
  10. Burhenne J, Liu L, Heilig C, Meid A, Leisen M, Schmitt T, et al. Intracellular vorinostat accumulation and its relationship to histone deacetylase activity in soft tissue sarcoma patients. Cancer Chemother Pharmacol. 2017;80:433-439 pubmed publisher
    ..17 µM in PBMCs were necessary. HDAC inhibition closely followed intracellular vorinostat concentrations and was short-lasting, which may contribute to the limited efficacy seen with vorinostat in solid tumors so far. ..
  11. Bohnsack J, Patel V, Morrow A. Ethanol Exposure Regulates Gabra1 Expression via Histone Deacetylation at the Promoter in Cultured Cortical Neurons. J Pharmacol Exp Ther. 2017;363:1-11 pubmed publisher
  12. Lu J, Chatain G, Bugarini A, Wang X, Maric D, Walbridge S, et al. Histone Deacetylase Inhibitor SAHA Is a Promising Treatment of Cushing Disease. J Clin Endocrinol Metab. 2017;102:2825-2835 pubmed publisher
    ..b>Histone deacetylase inhibitors (HDACis) are antitumor drugs approved for clinical use, with the potential to affect ..
  13. Lubbert M, Kuendgen A. Combining DNA methyltransferase and histone deacetylase inhibition to treat acute myeloid leukemia/myelodysplastic syndrome: achievements and challenges. Cancer. 2015;121:498-501 pubmed publisher
  14. Igarashi K, Kawaguchi K, Kiyuna T, Murakami T, Miwa S, Nelson S, et al. Efficacy In Vitro of Caffeine and Valproic Acid on Patient-Derived Undifferentiated Pleomorphic Sarcoma and Rhabdomyosarcoma Cell Lines. Anticancer Res. 2017;37:4081-4084 pubmed
    ..13 ± 0.20 mM. Synergistic efficacy of combination treatment of CAF and VPA was also observed for both cell lines. The results of the present study suggest that CAF and VPA may be useful in the treatment of recalcitrant sarcoma. ..
  15. Prince H. Pioneering studies of histone deacetylase inhibitors in myeloma: signals of activity set the stage for combination therapy trials. Leuk Lymphoma. 2012;53:1658-9 pubmed publisher
  16. Layman W, Zuo J. Preventing ototoxic hearing loss by inhibiting histone deacetylases. Cell Death Dis. 2015;6:e1882 pubmed publisher
  17. De Vreese R, D Hooghe M. Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. Eur J Med Chem. 2017;135:174-195 pubmed publisher
    ..of the synthesis and biological activity of the most representative benzohydroxamic acid-based histone deacetylase inhibitors published to date...
  18. Smolewski P, Robak T. The discovery and development of romidepsin for the treatment of T-cell lymphoma. Expert Opin Drug Discov. 2017;12:859-873 pubmed publisher
    ..Combinations of romidepsin with other antineoplastic agents may also further improve drug response and outcomes in T-cell lymphoma. ..
  19. West A, Johnstone R. New and emerging HDAC inhibitors for cancer treatment. J Clin Invest. 2014;124:30-9 pubmed publisher
    ..We examine HDAC inhibitors (HDACis) targeting class I, II, and IV HDACs that are currently under development for use as anticancer agents following the FDA approval of two HDACis, vorinostat and romidepsin. ..
  20. McClure J, Inks E, Zhang C, Peterson Y, Li J, Chundru K, et al. Comparison of the Deacylase and Deacetylase Activity of Zinc-Dependent HDACs. ACS Chem Biol. 2017;12:1644-1655 pubmed publisher
    ..Additionally, this selective HDAC3 inhibition allows for control of HMGB-1 secretion from activated macrophages without altering the acetylation status of histones or tubulin. ..
  21. Bastian L, Einsiedel H, Henze G, Seeger K, Shalapour S. The sequence of application of methotrexate and histone deacetylase inhibitors determines either a synergistic or an antagonistic response in childhood acute lymphoblastic leukemia cells. Leukemia. 2011;25:359-61 pubmed publisher
  22. Bassi S, Tripathi T, Monziani A, Di Leva F, Biagioli M. Epigenetics of Huntington's Disease. Adv Exp Med Biol. 2017;978:277-299 pubmed publisher
    ..Thus, the overarching goal of this chapter is to discuss the current status of the literature, reviewing how an aberrant epigenetic landscape can contribute to altered gene expression and neuronal dysfunction in HD. ..
  23. Lai J, Leman L, Ku S, Vickers C, Olsen C, Montero A, et al. Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells. Bioorg Med Chem Lett. 2017;27:3289-3293 pubmed publisher
    ..Multiple studies have reported the efficacy of histone deacetylase inhibitors (HDACi) in this regard...
  24. Qu K, Zaba L, Satpathy A, Giresi P, Li R, Jin Y, et al. Chromatin Accessibility Landscape of Cutaneous T Cell Lymphoma and Dynamic Response to HDAC Inhibitors. Cancer Cell. 2017;32:27-41.e4 pubmed publisher
    ..Clinical response to histone deacetylase inhibitors (HDACi) is strongly associated with a concurrent gain in chromatin accessibility...
  25. Ye J. Improving insulin sensitivity with HDAC inhibitor. Diabetes. 2013;62:685-7 pubmed publisher
  26. Rajasekharan S, Ramesh S, Bakkiyaraj D. Synergy of flavonoids with HDAC inhibitor: new approach to target Candida tropicalis biofilms. J Chemother. 2015;27:246-9 pubmed publisher
    ..In conclusion, this is the first report to our knowledge on implementing a combination therapy using flavonoids and histone deacetylase (HDAC) inhibitor. ..
  27. Warlick E, Cao Q, Miller J. Bortezomib and vorinostat in refractory acute myelogenous leukemia and high-risk myelodysplastic syndromes: produces stable disease but at the cost of high toxicity. Leukemia. 2013;27:1789-91 pubmed publisher
  28. Li X, Zhang Y, Jiang Y, Wu J, Inks E, Chou C, et al. Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study. Eur J Med Chem. 2017;134:185-206 pubmed publisher
  29. Falahi F, van Kruchten M, Martinet N, Hospers G, Rots M. Current and upcoming approaches to exploit the reversibility of epigenetic mutations in breast cancer. Breast Cancer Res. 2014;16:412 pubmed publisher
    ..Finally, we describe epigenetic editing as a promising new approach for possible applications towards more targeted breast cancer treatment. ..
  30. Kawada Y, Asahara S, Sugiura Y, Sato A, Furubayashi A, Kawamura M, et al. Histone deacetylase regulates insulin signaling via two pathways in pancreatic ? cells. PLoS ONE. 2017;12:e0184435 pubmed publisher
    ..Treatment of MIN6 cells with histone deacetylase inhibitors led to increased IRS2 expression, but this occurred in concert with low insulin signaling...
  31. Collins C, Ellis J, Holaska J. MAPK signaling pathways and HDAC3 activity are disrupted during differentiation of emerin-null myogenic progenitor cells. Dis Model Mech. 2017;10:385-397 pubmed publisher
    ..Thus, pharmacological targeting of multiple pathways acting at specific differentiation stages may be a better therapeutic approach in the future to rescue muscle regeneration in vivo. ..
  32. Yoshida M, Kijima M, Akita M, Beppu T. Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A. J Biol Chem. 1990;265:17174-9 pubmed
    ..These results clearly indicate that TSA is a potent and specific inhibitor of the histone deacetylase and that the in vivo effect of TSA on cell proliferation and differentiation can be attributed to the inhibition of the enzyme. ..
  33. Lam H, Cloonan S, Bhashyam A, Haspel J, Singh A, Sathirapongsasuti J, et al. Histone deacetylase 6-mediated selective autophagy regulates COPD-associated cilia dysfunction. J Clin Invest. 2013;123:5212-30 pubmed publisher
    ..We conclude that an autophagy-dependent pathway regulates cilia length during CS exposure and has potential as a therapeutic target for COPD. ..
  34. Yanda M, Liu Q, Cebotaru L. An inhibitor of histone deacetylase 6 activity, ACY-1215, reduces cAMP and cyst growth in polycystic kidney disease. Am J Physiol Renal Physiol. 2017;313:F997-F1004 pubmed publisher
    ..We found that ACY-1215 lowered cAMP levels and protein expression of adenylyl cyclase 6. Our results suggest that HDAC6 could potentially serve as a therapeutic target in ADPKD. ..
  35. Moreau P, de Wit E. Recent progress in relapsed multiple myeloma therapy: implications for treatment decisions. Br J Haematol. 2017;179:198-218 pubmed publisher
    ..While acknowledging the lack of head-to-head data on which to base comparisons between the numerous regimens, we collate the latest data in order to provide a basis on which to make clinical decisions in this rapidly advancing field...
  36. Nikolova T, Kiweler N, Krämer O. Interstrand Crosslink Repair as a Target for HDAC Inhibition. Trends Pharmacol Sci. 2017;38:822-836 pubmed publisher
    ..Accordingly, histone deacetylase inhibitors (HDACi) are small, pharmacologically and clinically relevant molecules that sensitize cancer cells to ..
  37. Ronnekleiv Kelly S, Sharma A, Ahuja N. Epigenetic therapy and chemosensitization in solid malignancy. Cancer Treat Rev. 2017;55:200-208 pubmed publisher
    ..have evaluated the clinical potential of the various epigenetic therapies, currently only histone deacetylase inhibitors and DNA methyltransferase inhibitors are approved for use in specific hematologic malignancies...
  38. Kim B, Ratnayake R, Lee H, Shi G, Zeller S, Li C, et al. Synthesis and biological evaluation of largazole zinc-binding group analogs. Bioorg Med Chem. 2017;25:3077-3086 pubmed publisher
  39. Arhoma A, Chantry A, Haywood Small S, Cross N. SAHA-induced TRAIL-sensitisation of Multiple Myeloma cells is enhanced in 3D cell culture. Exp Cell Res. 2017;360:226-235 pubmed publisher
  40. Kwon W, Rha S, Jeung H, Kim T, Chung H. Modulation of HAT activity by the BRCA2 N372H variation is a novel mechanism of paclitaxel resistance in breast cancer cell lines. Biochem Pharmacol. 2017;138:163-173 pubmed publisher
    ..Restoration of wild BRCA2 from variant type improved paclitaxel sensitivity (p<0.001). Modulation of HAT activity by BRCA2 N372H variation is a new mechanism of paclitaxel resistance in breast cancer. ..
  41. Perri F, Longo F, Giuliano M, Sabbatino F, Favia G, Ionna F, et al. Epigenetic control of gene expression: Potential implications for cancer treatment. Crit Rev Oncol Hematol. 2017;111:166-172 pubmed publisher
    ..Recently, methyltransferase and histone deacetylase inhibitors have attracted the attention of researchers and clinicians as they potentially provide alternative ..
  42. Tang F, Choy E, Tu C, Hornicek F, Duan Z. Therapeutic applications of histone deacetylase inhibitors in sarcoma. Cancer Treat Rev. 2017;59:33-45 pubmed publisher
    ..Therefore, better drugs to treat sarcomas are needed. Histone deacetylase inhibitors (HDAC inhibitors, HDACi, HDIs) are epigenetic modifying agents that can inhibit sarcoma growth in ..
  43. Hanigan T, Taha T, Aboukhatwa S, Frasor J, Petukhov P. Scaffold dependent histone deacetylase (HDAC) inhibitor induced re-equilibration of the subcellular localization and post-translational modification state of class I HDACs. PLoS ONE. 2017;12:e0186620 pubmed publisher
    The mechanism of action of histone deacetylase inhibitors (HDACi) is mainly attributed to the inhibition of the deacetylase catalytic activity for their histone substrates...
  44. Krieger V, Hamacher A, Gertzen C, Senger J, Zwinderman M, Marek M, et al. Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups. J Med Chem. 2017;60:5493-5506 pubmed publisher
    ..Furthermore, 4j almost completely reversed the cisplatin resistance in Cal27CisR. This effect is related to a synergistic induction of apoptosis as seen in the combination of 4j with cisplatin. ..
  45. Baylin S. Resistance, epigenetics and the cancer ecosystem. Nat Med. 2011;17:288-9 pubmed publisher
  46. Vaiserman A, Koliada A, Koshel N, Simonenko A, Pasiukova E. [Effect of the histone deacetylase inhibitor sodium butyrate on the viability and life span in Drosophila melanogaster]. Adv Gerontol. 2012;25:126-31 pubmed
    ..Since SB is an efficient inducer of epigenetic changes, it can be assumed that its use as a life-extending agent (geroprotector) can be quite promising. ..
  47. Yoo D, Kim D, Kim M, Choi J, Jung H, Nam S, et al. Sodium butyrate, a histone deacetylase Inhibitor, ameliorates SIRT2-induced memory impairment, reduction of cell proliferation, and neuroblast differentiation in the dentate gyrus. Neurol Res. 2015;37:69-76 pubmed publisher
    ..This result suggests that histone acetylation and deacetylation are key factors modulating hippocampal functions such as memory formation, cell proliferation, and neuroblast differentiation in the dentate gyrus. ..
  48. Crozatier B, Ventura Clapier R. Inhibition of hypertrophy, per se, may not be a good therapeutic strategy in ventricular pressure overload: other approaches could be more beneficial. Circulation. 2015;131:1448-57 pubmed publisher
  49. Xie R, Li Y, Tang P, Yuan Q. Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity. Bioorg Med Chem Lett. 2017;27:4415-4420 pubmed publisher
    ..Vorambucil could be a promising candidate and a useful tool to elucidate the role of those DNA/HDAC dual-targeting inhibitors for cancer therapy. ..
  50. Cheng M, Wong Y, Chang C, Yang C, Chen S, Yuan C, et al. B1, a novel HDAC inhibitor, induces apoptosis through the regulation of STAT3 and NF-?B. Int J Mol Med. 2017;39:1137-1148 pubmed publisher
    ..The inhibition of the intricate crosstalk between STAT3 and NF-?B may be a major factor in the molecular action mechanism of B1. The multiple targeting effects of B1 render it a potential new drug for lung cancer therapy. ..
  51. Benito E, Urbanke H, Ramachandran B, Barth J, Halder R, Awasthi A, et al. HDAC inhibitor-dependent transcriptome and memory reinstatement in cognitive decline models. J Clin Invest. 2015;125:3572-84 pubmed publisher
    ..of transcriptome plasticity in the hippocampal CA1 region in aging and AD models and suggests that histone deacetylase inhibitors should be further explored as a cost-effective therapeutic strategy against age-associated cognitive ..
  52. Wei Z, Shan Y, Tao L, Liu Y, Zhu Z, Liu Z, et al. Diallyl trisulfides, a natural histone deacetylase inhibitor, attenuate HIF-1? synthesis, and decreases breast cancer metastasis. Mol Carcinog. 2017;56:2317-2331 pubmed publisher
    ..It reduced the protein expression of HIF-1?, which did not involve inhibition of HIF-1? mRNA expression or ubiquitin proteasome degradation. Efficient inhibition of HIF-1? expression was required for DATS to resist breast cancer. ..
  53. Kumar P, Gogulamudi V, Periasamy R, Raghavaraju G, Subramanian U, Pandey K. Inhibition of HDAC enhances STAT acetylation, blocks NF-?B, and suppresses the renal inflammation and fibrosis in Npr1 haplotype male mice. Am J Physiol Renal Physiol. 2017;313:F781-F795 pubmed publisher
    ..The current findings will help in developing the molecular therapeutic targets and new treatment strategies for hypertension and renal dysfunction in humans. ..
  54. Nakayama T, Akagawa K. Transcription regulation mechanism of the syntaxin 1A gene via protein kinase A. Biochem J. 2017;474:2465-2473 pubmed publisher
    ..The results of the current study suggest that forskolin phosphorylates HDAC8-Ser39 via the PKA pathway and increases histone H3 acetylation in cells expressing HDAC8, resulting in the induction of the Stx1a gene. ..
  55. Trapani D, Esposito A, Criscitiello C, Mazzarella L, Locatelli M, Minchella I, et al. Entinostat for the treatment of breast cancer. Expert Opin Investig Drugs. 2017;26:965-971 pubmed publisher
    ..This offers the rationale for combining HDAC inhibitors with immunotherapy, including therapeutic cancer vaccines. ..
  56. Wilcox R. Cutaneous T-cell lymphoma: 2017 update on diagnosis, risk-stratification, and management. Am J Hematol. 2017;92:1085-1102 pubmed publisher
    ..nodal, visceral or blood involvement are generally approached with biologic-response modifiers or histone deacetylase inhibitors prior to escalating therapy to include systemic, single-agent chemotherapy...
  57. Shackleton M. Moving targets that drive cancer progression. N Engl J Med. 2010;363:885-6 pubmed publisher
  58. Xu Z, Tong Q, Zhang Z, Wang S, Zheng Y, Liu Q, et al. Inhibition of HDAC3 prevents diabetic cardiomyopathy in OVE26 mice via epigenetic regulation of DUSP5-ERK1/2 pathway. Clin Sci (Lond). 2017;131:1841-1857 pubmed publisher
    ..The present study indicates the potential application of HDAC3 inhibitor for the prevention of DCM. ..
  59. Nelson P. Molecular states underlying androgen receptor activation: a framework for therapeutics targeting androgen signaling in prostate cancer. J Clin Oncol. 2012;30:644-6 pubmed publisher
  60. Fairlie D, Sweet M. HDACs and their inhibitors in immunology: teaching anticancer drugs new tricks. Immunol Cell Biol. 2012;90:3-5 pubmed publisher
  61. Janaki Ramaiah M, Naushad S, Lavanya A, Srinivas C, Anjana Devi T, Sampathkumar S, et al. Scriptaid cause histone deacetylase inhibition and cell cycle arrest in HeLa cancer cells: A study on structural and functional aspects. Gene. 2017;627:379-386 pubmed publisher
    ..This observation was further strengthened by an artificial neuronal network (ANN) model. ..
  62. Sancho Pelluz J, Paquet Durand F. HDAC inhibition prevents Rd1 mouse photoreceptor degeneration. Adv Exp Med Biol. 2012;723:107-13 pubmed publisher
  63. Yao C, Zhang G, Walker A, Zhao K, Li Y, Lyu L, et al. Potent induction of apoptosis by givinostat in BCR-ABL1-positive and BCR-ABL1-negative precursor B-cell acute lymphoblastic leukemia cell lines. Leuk Res. 2017;60:129-134 pubmed publisher
    ..These data further enrich our understanding of the mechanisms of the antineoplastic effects of givinostat in B-ALL and provide a preclinical rationale for the inclusion of givinostat or similar agent in leukemia therapy. ..
  64. Killick Cole C, Singleton W, Bienemann A, Asby D, Wyatt M, Boulter L, et al. Repurposing the anti-epileptic drug sodium valproate as an adjuvant treatment for diffuse intrinsic pontine glioma. PLoS ONE. 2017;12:e0176855 pubmed publisher
    ..These findings support the use of sodium valproate as an adjuvant treatment for DIPG. ..
  65. Zhang Q, Lu B, Li J. Design, synthesis and biological evaluation of 4-piperazinyl-containing Chidamide derivatives as HDACs inhibitors. Bioorg Med Chem Lett. 2017;27:3162-3166 pubmed publisher
    ..Compound 9g, proved to be the most potent and efficacious derivative in this series, was orally active in an HCT116 xenograft model in vivo. ..
  66. Tian Y, Lv W, Li X, Wang C, Wang D, Wang P, et al. Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. Bioorg Med Chem Lett. 2017;27:2943-2945 pubmed publisher
    ..This work highlighted an optimized strategy to assay slow-binding inhibitors of unstable proteins with known fast-binding inhibitors. It should be especially useful in a hit-discovery stage to find moderate potent compounds. ..
  67. Atlante S, Chegaev K, Cencioni C, Guglielmo S, Marini E, Borretto E, et al. Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors. Eur J Med Chem. 2018;144:612-625 pubmed publisher
    ..Thanks to their unique biological features, these compounds may represent new therapeutic tools for cardiovascular, neuromuscular and inflammatory diseases. ..
  68. Kienzler A, Rizzi M, Reith M, Nutt S, Eibel H. Inhibition of human B-cell development into plasmablasts by histone deacetylase inhibitor valproic acid. J Allergy Clin Immunol. 2013;131:1695-9 pubmed publisher
  69. Cohen J. Understanding HIV latency to undo it. Science. 2011;332:786 pubmed publisher
  70. Amemiya S, Yamaguchi T, Hashimoto Y, Noguchi Yachide T. Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. Bioorg Med Chem. 2017;25:3677-3684 pubmed publisher
    ..Interestingly, it also showed growth-inhibitory activity towards BRD4 inhibitor-resistant cells. ..
  71. Dong G, Chen W, Wang X, Yang X, Xu T, Wang P, et al. Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors. J Med Chem. 2017;60:7965-7983 pubmed publisher
    ..This proof-of-concept study demonstrates the feasibility of discovering an inhibitor targeting cancer metabolism and epigenetics and provides an efficient strategy for multitarget antitumor drug discovery. ..
  72. Yuan Z, Sun Q, Li D, Miao S, Chen S, Song L, et al. Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors. Eur J Med Chem. 2017;134:281-292 pubmed publisher
    ..In summary, our study provided a practical drug design strategy targeting multiple enzymes, and 15a represents a novel and promising lead compound for the development of novel epigenetic inhibitors as antitumor agents. ..
  73. Russo R, Cimmino F, Pezone L, Manna F, Avitabile M, Langella C, et al. Kinome expression profiling of human neuroblastoma tumors identifies potential drug targets for ultra high-risk patients. Carcinogenesis. 2017;38:1011-1020 pubmed publisher
    ..Preclinical in vivo studies are needed to consolidate the SAHA and Radicicol treatment in ultra-HR NBL patients...
  74. Guha M. HDAC inhibitors still need a home run, despite recent approval. Nat Rev Drug Discov. 2015;14:225-6 pubmed publisher
  75. Durham B, Grigg R, Wood I. Inhibition of histone deacetylase 1 or 2 reduces induced cytokine expression in microglia through a protein synthesis independent mechanism. J Neurochem. 2017;143:214-224 pubmed publisher
    ..Taken together, this study supports the idea that inhibitors selective towards HDAC1 or HDAC2, may be therapeutically useful for targeting neuroinflammation in brain injuries and neurodegenerative disease. ..
  76. Garmpis N, Damaskos C, Garmpi A, Dimitroulis D, Spartalis E, Margonis G, et al. Targeting Histone Deacetylases in Malignant Melanoma: A Future Therapeutic Agent or Just Great Expectations?. Anticancer Res. 2017;37:5355-5362 pubmed
    ..Histone deacetylases (HDAC) are associated with different types of cancer. Histone deacetylase inhibitors (HDACI) are enzymes that inhibit the action of HDAC, resulting in block of tumor cell proliferation...
  77. Xu Z, Yang Y, Mai X, Liu B, Xiong Y, Feng L, et al. Syntheses and Biological Evaluation of Novel Hydroxamic Acid Derivatives Containing Purine Moiety as Histone Deacetylase Inhibitors. Chem Pharm Bull (Tokyo). 2018;66:439-451 pubmed publisher
  78. Gurgul A, Opiela J, Pawlina K, Szmatoła T, Bochenek M, Bugno Poniewierska M. The effect of histone deacetylase inhibitor trichostatin A on porcine mesenchymal stem cell transcriptome. Biochimie. 2017;139:56-73 pubmed publisher
    The use of histone deacetylase inhibitors such as trichostatin A (TSA) for epigenetic transformation of mesenchymal stem cells (MSCs), whose nuclei will be transferred into enucleated oocytes, is a novel approach in research involving ..
  79. Thomas E. Histone Posttranslational Modifications in Schizophrenia. Adv Exp Med Biol. 2017;978:237-254 pubmed publisher
    ..This chapter will review the current information regarding histone modifications in schizophrenia and the potential therapeutic relevance of such marks. ..
  80. Korzus E. Rubinstein-Taybi Syndrome and Epigenetic Alterations. Adv Exp Med Biol. 2017;978:39-62 pubmed publisher
    ..Even though there has been intensive research on the genetic and epigenetic function of the CREBBP gene in rodents, the etiology of this devastating congenital human disorder is largely unknown. ..
  81. Yoshida M, Kudo N, Kosono S, Ito A. Chemical and structural biology of protein lysine deacetylases. Proc Jpn Acad Ser B Phys Biol Sci. 2017;93:297-321 pubmed publisher
    ..This review mainly focuses on structural aspects of HDAC enzymatic activity regulated by interaction with substrates, co-factors, small molecule inhibitors, and activators. ..
  82. Mehndiratta S, Wang R, Huang H, Su C, Hsu C, Wu Y, et al. 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. Eur J Med Chem. 2017;134:13-23 pubmed publisher
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