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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Histone deacetylase inhibitors suppress the expression of inflammatory and innate immune response genes in human microglia and astrocytes
TL;DR: The effects of two non-selective HDACi, trichostatin A and valproic acid, on antiviral and cytokine gene expression in primary human microglia and astrocytes stimulated with TLR3 or TLR4 ligand are examined.
Journal ArticleDOI
Inhibitors of histone deacetylase 1 reverse the immune evasion phenotype to enhance T-cell mediated lysis of prostate and breast carcinoma cells
TL;DR: It is demonstrated that prostate (LNCAP) and breast (MDA-MB-231) carcinoma cells are more sensitive to T-cell mediated lysis in vitro after clinically relevant exposure to epigenetic therapy with either the pan-HDAC inhibitor vorinostat or the class I HDAC inhibitor ent inostat.
Journal ArticleDOI
Activation of elastin transcription by transforming growth factor-β in human lung fibroblasts
Ping-Ping Kuang,Xiao-Hui Zhang,Celeste B. Rich,Judith Ann Foster,Mangalalaxmy Subramanian,Ronald H. Goldstein +5 more
TL;DR: Together, the results demonstrated that TGF-beta activates elastin transcription that is dependent on phosphatidylinositol 3-kinase/Akt activity.
Journal ArticleDOI
A phase I trial of vorinostat and bortezomib in children with refractory or recurrent solid tumors: A Children's Oncology Group phase I consortium study (ADVL0916)
Jodi A. Muscal,Patrick A. Thompson,Terzah M. Horton,Ashish M. Ingle,Charlotte H. Ahern,Renee M. McGovern,Joel M. Reid,Matthew M. Ames,Igor Espinoza-Delgado,Brenda J. Weigel,Susan M. Blaney +10 more
TL;DR: A pediatric Phase I trial was performed to determine the maximum‐tolerated dose, dose‐limiting toxicities (DLTs), and pharmacokinetics (PK) of vorinostat and bortezomib, in patients with solid tumors.
Journal ArticleDOI
Histone deacetylase inhibitors (HDACIs). Structure—activity relationships: history and new QSAR perspectives
TL;DR: The QSAR analysis presented here is an attempt to organize the knowledge on the HDACIs with the purpose of designing new chemical entities with enhanced inhibitory potencies and to study the mechanism of action of the compounds.
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.