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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Coordinated changes of histone modifications and HDAC mobilization regulate the induction of MHC class II genes by Trichostatin A
Manolis Gialitakis,Androniki Kretsovali,Charalampos G. Spilianakis,Lara Kravariti,Jörg Mages,Reinhard Hoffmann,Antonis K. Hatzopoulos,Joseph Papamatheakis +7 more
TL;DR: A complex pattern of gene reprogramming by TSA involves immune recognition, antiviral, apoptotic and inflammatory pathways and extends the rationale for using Histone Deacetylase Inhibitors (HDACi) to modulate the immune response.
Journal ArticleDOI
Histone deacetylase (HDAC) inhibitors in cancer: a patent review (2017-present).
TL;DR: Although great accomplishments have been achieved in developing HDAC selective inhibitors, there is still an urgent need for discovery of novel HDAC inhibitors with new zinc-binding groups avoiding the unfavorable pharmacokinetics profiles of hydroxamic acid.
Journal ArticleDOI
Molecular endocrinology of vitamin D on the epigenome level.
TL;DR: This model provides the present basis of the molecular endocrinology of vitamin D and will be in future refined by the integration ofitamin D-sensitive chromatin markers and other genome-wide data, such as the 1,25(OH)2D3-sensitive binding of co-factors, chromatin modifying enzymes and chromatin remodeling proteins.
Journal ArticleDOI
A phase I, pharmacokinetic and pharmacodynamic study on vorinostat in combination with 5-fluorouracil, leucovorin, and oxaliplatin in patients with refractory colorectal cancer.
Marwan Fakih,Lakshmi Pendyala,Gerald J. Fetterly,Karoli Toth,James A. Zwiebel,Igor Espinoza-Delgado,Alan Litwin,Youcef M. Rustum,Mary Ellen Ross,Julianne L. Holleran,Merrill J. Egorin +10 more
TL;DR: The maximum tolerated dose of vorinostat in combination with FOLFOX is 300 mg orally twice daily × 1 week every 2 weeks, suggesting alternative vorInostat dosing schedules may be needed for optimal down-regulation of TS expression.
Journal ArticleDOI
3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.
TL;DR: 3-hydroxypyridin-2-thione (3-HPT) is identified as a novel ZBG that is compatible with HDAC inhibition and a subset of these inhibitors induces apoptosis in various cancer cell lines.
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.
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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.
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.