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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Journal ArticleDOI
Inflammation and tuberculosis: host‐directed therapies
Alimuddin Zumla,Martin Rao,Shreemanta Parida,Salmaan Keshavjee,Gail H. Cassell,Robert S. Wallis,R Axelsson-Robertsson,R Axelsson-Robertsson,M. Doherty,Jan Andersson,Markus Maeurer,Markus Maeurer +11 more
TL;DR: Current concepts of inflammation in TB disease are reviewed, candidate pathways for host‐directed therapies to achieve better clinical outcomes are discussed and biological agents or already approved drugs can be ‘re‐purposed’ to interfere with biologically relevant cellular checkpoints are discussed.
Journal ArticleDOI
Molecular mechanism of SAHA on regulation of autophagic cell death in tamoxifen-resistant MCF-7 breast cancer cells.
TL;DR: Results suggest that SAHA can induce caspase-independent autophagic cell death rather than apoptotic cell death in TAMR/MCF-7 cells, which is a promising new strategy to treatment of tamoxifen-resistant human breast cancer.
Journal ArticleDOI
Histone acetyltransferase inhibitors and preclinical studies.
TL;DR: Despite the fact that other drugs able to regulate the histone modifier enzymes (such as histone deacetylase inhibitors) have been already approved for the treatment of cancer, HAT inhibitors seem promising for the Treatment of human diseases such as AD and diabetes, although side effects and toxicity need to be investigated.
Journal ArticleDOI
Histone deacetylase inhibitors as novel anticancer therapeutics.
TL;DR: An overview of the histone deacetylase superfamily is provided, the positive results of de acetylase inhibitors in cancer clinical trials are highlighted, and the prospects for the next generation of such inhibitors are commented on.
Journal ArticleDOI
Exercise and BMI in Overweight and Obese Children and Adolescents: A Systematic Review and Trial Sequential Meta-Analysis
TL;DR: Exercise is associated with improvements in BMI among overweight and obese children and adolescents, and changes in BMI crossed the monitoring boundary for a type 1 error in 2010, remaining stable thereafter.
References
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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.