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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Effects of valproic acid on the cell cycle and apoptosis through acetylation of histone and tubulin in a scirrhous gastric cancer cell line
Yasumichi Yagi,Sachio Fushida,Shinichi Harada,Jun Kinoshita,Isamu Makino,Katsunobu Oyama,Hidehiro Tajima,Hideto Fujita,Hiroyuki Takamura,Itasu Ninomiya,Takashi Fujimura,Tetsuo Ohta,Masakazu Yashiro,Kosei Hirakawa +13 more
TL;DR: VPA induced dynamic modulation of histone H3 and α-tubulin acetylation in relation with the anticancer effect and the enhancement of PTX in the OCUM-2MD3 cell line is expected to be a promising therapy for peritoneal dissemination of scirrhous gastric cancer.
Journal ArticleDOI
Combined inhibition of EZH2 and histone deacetylases as a potential epigenetic therapy for non-small-cell lung cancer cells.
Taichi Takashina,Ichiro Kinoshita,Junko Kikuchi,Yasushi Shimizu,Jun Sakakibara-Konishi,Satoshi Oizumi,Masaharu Nishimura,Hirotoshi Dosaka-Akita +7 more
TL;DR: The combined pharmacological targeting of EZH2 and HDACs may provide more effective epigenetic therapeutics for NSCLC, and the co‐treatment suppressed the in vivo tumor growth of EGFR‐mutant, EGFR–tyrosine kinase‐resistant H1975 cells more effectively than did each agent alone, without visible toxicity.
Journal ArticleDOI
The histone deacetylase inhibitor, Trichostatin A, enhances radiation sensitivity and accumulation of gammaH2A.X.
TL;DR: The results suggest the modulation of radiation effects observed at the lower Trichostatin A concentrations was associated with histone hyperacetylation and changes in phosphorylated ?
Journal ArticleDOI
Molecular basis of 1-deoxygalactonojirimycin arylthiourea binding to human α-galactosidase a: pharmacological chaperoning efficacy on Fabry disease mutants.
Yi Yu,Teresa Mena-Barragán,Katsumi Higaki,Jennifer L. Johnson,Jason E. Drury,Raquel L. Lieberman,Naoe Nakasone,Haruaki Ninomiya,Takahiro Tsukimura,Hitoshi Sakuraba,Yoshiyuki Suzuki,Eiji Nanba,Carmen Ortiz Mellet,José M. García Fernández,Kousaku Ohno +14 more
TL;DR: A new family of neutral amphiphilic pharmacological chaperones, namely 1-deoxygalactonojirimycin-arylthioureas (DGJ-ArTs), capable of stabilizing α-Gal A and restoring trafficking are synthesized and characterized.
Journal ArticleDOI
The application of click chemistry in the synthesis of agents with anticancer activity.
TL;DR: The present review focuses mainly on the applications of this reaction in the field of synthesis of agents with anticancer activity, which are divided into four groups: topoisomerase II inhibitors, histone deacetylase inhibitors, protein tyrosine kinase inhibitor, and antimicrotubule agents.
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.
Journal ArticleDOI
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.
Journal ArticleDOI
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.