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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Control of Apoptosis in Treatment and Biology of Pancreatic Cancer
TL;DR: Different intrinsic and extrinsic pathways in pancreatic cancer that may affect apoptosis are focused on to understand its aggressive nature and resistance to conventional treatment modalities.
Journal ArticleDOI
Identification of potential isoform-selective histone deacetylase inhibitors for cancer therapy: a combined approach of structure-based virtual screening, ADMET prediction and molecular dynamics simulation assay.
TL;DR: A large compound library containing 2,703,000 compounds retrieved from Otava database was screened against class I HDACs by exhaustive approach of structure-based virtual screening using rDOCK and Autodock Vina, and a total of 41 compounds were found to show high-isoform selectivity.
Journal ArticleDOI
Natural products: chemical instruments to apprehend biological symphony.
TL;DR: How natural products or engineered analogs can be used as chemical tools to apprehend some biological problems from the point of view of a chemical biologist is emphasized.
Journal ArticleDOI
Pretreatment dietary intake is associated with tumor suppressor DNA methylation in head and neck squamous cell carcinomas
Justin A. Colacino,Anna E. Arthur,Dana C. Dolinoy,Maureen A. Sartor,Sonia A. Duffy,Douglas B. Chepeha,Carol R. Bradford,Heather M. Walline,Jonathan B. McHugh,Nisha J. D'Silva,Thomas E. Carey,Gregory T. Wolf,Jeremy M. G. Taylor,Karen E. Peterson,Karen E. Peterson,Laura S. Rozek +15 more
TL;DR: It is suggested that intake of folate, vitamin A and vitamin B12 may be associated with the tumor DNA methylation profile in HNC and enhance tumor suppression.
Journal ArticleDOI
Alterations in cellular metabolome after pharmacological inhibition of Notch in glioblastoma cells
Ulf Dietrich Kahlert,Menglin Cheng,Katharina Koch,Luigi Marchionni,Luigi Marchionni,Xing Fan,Eric H. Raabe,Eric H. Raabe,Jarek Maciaczyk,Kristine Glunde,Kristine Glunde,Charles G. Eberhart +11 more
TL;DR: Global and targeted expression analyses revealed that multiple genes important in glutamate homeostasis, including glutaminase, are dysregulated after Notch inhibition, suggesting that notch inhibition may act at least in part by regulating glutaminases and glutamate.
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.