Journal ArticleDOI
Histone deacetylase inhibitors.
TLDR
Design of a second generation ofHDACs was based upon data affording potent HDACs such as LAQ824 and PDX101 currently under phase I clinical trials, and two of them, MS-275 and CI-994, have reached phase II and I clinical Trials, respectively.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2005-01-01. It has received 819 citations till now. The article focuses on the topics: Histone deacetylase & Phenylbutyrate.read more
Citations
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Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors
Isabelle Paquin,Stephane Raeppel,Silvana Leit,Frédéric Gaudette,Nancy Z. Zhou,Oscar Moradei,Oscar Mario Saavedra,Naomy Bernstein,Franck Raeppel,Giliane Bouchain,Sylvie Frechette,Soon Hyung Woo,Arkadii Vaisburg,Marielle Fournel,Ann Kalita,Marie-France Robert,Aihua Lu,Marie-Claude Trachy-Bourget,Pu Theresa Yan,Jianhong Liu,Jubrail Rahil,A. Robert MacLeod,Jeffrey M. Besterman,Zuomei Li,Daniel Delorme +24 more
TL;DR: From the different series bearing a six-membered heteroaromatic ring studied, the s-triazine series showed the best HDAC1 enzyme and in vitro anti-proliferative activities with IC(50) values below micromolar range.
Journal ArticleDOI
Inhibition of bladder tumour growth by histone deacetylase inhibitor
Akira Ozawa,Nozomu Tanji,Tadahiko Kikugawa,Toyokazu Sasaki,Yutaka Yanagihara,Noriyoshi Miura,Masayoshi Yokoyama +6 more
TL;DR: To examine the expression profile of histone deacetylase (HDAC)‐1 and explore its potential role in the development of bladder cancer, using valproic acid (VPA), a HDAC inhibitor, which reduces tumour growth and metastasis formation in animal models.
Journal ArticleDOI
A breach in the scaffold: the possible role of cytoskeleton dysfunction in the pathogenesis of major depression.
TL;DR: The disruption of microtubule and actin in terms of morphology and functions may be a leading cause of dendritic regression and decrease in dendrite spine in depression.
Journal ArticleDOI
Epigenetic Modifications in Alzheimer's Neuropathology and Therapeutics
TL;DR: The intricate packaging of DNA in eukaryotic cells, and the various modifications in epigenetic mechanisms that are now linked to the neuropathology and the progression of Alzheimer’s disease (AD), as well as potential therapeutic interventions are reviewed.
Journal ArticleDOI
Epigenetic therapeutic strategies for the treatment of neuropsychiatric disorders: ready for prime time?
TL;DR: The epigenetic therapeutic strategy has much promise, and its development will foster collaboration and cross fertilization between molecular and cell biologists, oncologists, psychiatrists, and neurologists.
References
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Journal ArticleDOI
Crystal structure of the nucleosome core particle at 2.8 Å resolution
TL;DR: The X-ray crystal structure of the nucleosome core particle of chromatin shows in atomic detail how the histone protein octamer is assembled and how 146 base pairs of DNA are organized into a superhelix around it.
Journal ArticleDOI
hSIR2SIRT1 Functions as an NAD-Dependent p53 Deacetylase
Homayoun Vaziri,Scott K. Dessain,Scott K. Dessain,Elinor Ng Eaton,Shin-ichiro Imai,Roy A. Frye,Tej K. Pandita,Leonard Guarente,Robert A. Weinberg +8 more
TL;DR: It is proposed that hSir2, the human homolog of the S. cerevisiae Sir2 protein known to be involved in cell aging and in the response to DNA damage, binds and deacetylates the p53 protein with a specificity for its C-terminal Lys382 residue.
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Negative Control of p53 by Sir2α Promotes Cell Survival under Stress
Jianyuan Luo,Anatoly Y. Nikolaev,Shin-ichiro Imai,Delin Chen,Fei Su,Ariel L. Shiloh,Leonard Guarente,Wei Gu +7 more
TL;DR: It is shown that mammalian Sir2alpha physically interacts with p53 and attenuates p53-mediated functions, and Nicotinamide inhibits an NAD-dependent p53 deacetylation induced by Sir2 alpha, and also enhances the p53 acetylation levels in vivo.
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Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A.
TL;DR: 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.
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Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells
Martin Göttlicher,Saverio Minucci,Ping Zhu,Oliver H. Krämer,Annemarie Schimpf,Sabrina Giavara,Jonathan P. Sleeman,Francesco Lo Coco,Clara Nervi,Pier Giuseppe Pelicci,Thorsten Heinzel +10 more
TL;DR: Valproic acid induces differentiation of carcinoma cells, transformed hematopoietic progenitor cells and leukemic blasts from acute myeloid leukemia patients, and tumor growth and metastasis formation are significantly reduced in animal experiments, suggesting that it might serve as an effective drug for cancer therapy.