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
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Chromatin-modifying enzymes as therapeutic targets--Part 1.
TL;DR: A review of the roles of chromatin-modifying enzymes in gene regulation and their potentials as therapeutic targets for epigenetic therapies is focused on enzymes responsible for histone acetylation, deacetylation and demethylation.
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Ligand Based Pharmacophore Modeling and Virtual Screening Studies to Design Novel HDAC2 Inhibitors
TL;DR: This model was utilized as a 3D query for virtual screening to validate against NCI and Maybridge database and the hits further screened by Lipinski's rule of 5 were found and were subjected to molecular docking in the active site of HDAC2 (PDB: 3MAX).
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Treatment with a Histone Deacetylase Inhibitor after Nuclear Transfer Improves the Preimplantation Development of Cloned Bovine Embryos
Satoshi Akagi,Kazutsugu Matsukawa,Eiji Mizutani,Kazuhiro Fukunari,Masahiro Kaneda,Shinya Watanabe,Seiya Takahashi +6 more
TL;DR: Results suggest that HDACi treatment of bovine SCNT embryos improves the blastocyst formation rate; however, the optimal treatment conditions may differ among donor cell lines.
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Inhibitors of histone deacetylases in class I and class II suppress human osteoclasts in vitro
Melissa Cantley,David P. Fairlie,P. M. Bartold,Kim D. Rainsford,Giang Thanh Le,Andrew J. Lucke,C.A. Holding,David R. Haynes +7 more
TL;DR: Results suggest that inhibition of both classes I and II HDACs may be required to suppress human osteoclastic bone resorption in vitro.
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Global histone H3 lysine 27 (H3K27) methylation levels and their prognostic relevance in renal cell carcinoma
Sebastian Rogenhofer,Philip Kahl,Claudia Mertens,Stefan Hauser,Wolfgang Hartmann,Reinhard Büttner,Stefan Müller,Alexander von Ruecker,Jörg Ellinger +8 more
TL;DR: It’s shown that direct hits to the immune system are more likely to be associated with dementia than other types of injuries, including gunshot wounds.
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.
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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.