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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Valproic acid inhibits proliferation of HER2-expressing breast cancer cells by inducing cell cycle arrest and apoptosis through Hsp70 acetylation
Toshiki Mawatari,Itasu Ninomiya,Masafumi Inokuchi,Shinichi Harada,Hironori Hayashi,Katsunobu Oyama,Isamu Makino,Hisatoshi Nakagawara,Tomoharu Miyashita,Hidehiro Tajima,Hiroyuki Takamura,Sachio Fushida,Tetsuo Ohta +12 more
TL;DR: It is demonstrated that VPA inhibited cell proliferation and induced cell cycle arrest and apoptosis of HER2-overexpressing breast cancer cells, and an alternative mechanism whereby acetylation of Hsp70 disrupts the function of HSp90 and leads to downregulation of its client proteins, including HER2 is proposed that might be the indirect function of VPA.
Journal ArticleDOI
Malignant pleural mesothelioma: from the bench to the bedside
TL;DR: An overview of the recent advances in the biology of malignant pleural mesothelioma and their potential therapeutic applications in the field of MPM diagnosis and treatment is presented.
Journal ArticleDOI
Histone Deacetylase 1/2 Mediates Proliferation of Renal Interstitial Fibroblasts and Expression of Cell Cycle Proteins
Maoyin Pang,Li Ma,Na Liu,Na Liu,Murugavel Ponnusamy,Ting C. Zhao,Haidong Yan,Shougang Zhuang,Shougang Zhuang +8 more
TL;DR: An important role is revealed in regulating proliferation of renal interstitial fibroblasts, expression of cell cycle proteins and activation of STAT3, which mediates the proliferative action of HDACs.
Journal ArticleDOI
Histone deacetylase activity is retained in primary neurons expressing mutant huntingtin protein.
Masataka Hoshino,Kazuhiko Tagawa,Tomohiro Okuda,Miho Murata,Kiyomitsu Oyanagi,Nobutaka Arai,Toshio Mizutani,Ichiro Kanazawa,Erich E. Wanker,Hitoshi Okazawa +9 more
TL;DR: In this article, the effect of mutant huntingtin (htt) protein on the expression and activity of histone deacetylase (HDAC) proteins in rat primary cortical neurons as well as in human Huntington's disease (HD) brains was investigated.
Journal ArticleDOI
The effects of short-chain fatty acids on the cardiovascular system
TL;DR: The current review addresses the effects of short-chain fatty acids on the human cardiovascular system and investigates potential novel interventions for prevention and treatment of cardiovascular disorders using these fatty acids.
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.
Journal ArticleDOI
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.