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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HDAC-class II specific inhibition involves HDAC proteasome-dependent degradation mediated by RANBP2
Annamaria Scognamiglio,Angela Nebbioso,Fabio Manzo,Sergio Valente,Antonello Mai,Lucia Altucci +5 more
TL;DR: A crosstalk occurring between acetylation, deacetylation and sumoylation pathways is identified and it is suggested that class II specific HDAC inhibitors may affect different epigenetic pathways.
Journal ArticleDOI
Histone deacetylase inhibitors: A new mode for inhibition of cholesterol metabolism
TL;DR: In this article, the effects of histone deacetylases on genes involved in primary metabolism were explored in the F9 embryonal carcinoma model and 11 of 15 pathway genes in the HepG2 cell line.
Journal ArticleDOI
The therapeutic uses of chromatin-modifying agents.
TL;DR: HDACi could be useful in antimalarial and antifungal therapies and can reactivate the HIV-1 expression in latent cellular reservoirs, thus suggesting the use in a combination therapy with highly active antiretroviral therapy.
Journal ArticleDOI
Integration of Hedgehog and mutant FLT3 signaling in myeloid leukemia
Yiting Lim,Lukasz P. Gondek,Li Li,Qiuju Wang,Hayley S Ma,Emily Chang,David L. Huso,Sarah Foerster,Luigi Marchionni,Karen McGovern,David Neil Watkins,Craig D. Peacock,Mark J. Levis,Bruce Douglas Smith,Akil Merchant,Donald Small,William Matsui +16 more
TL;DR: The functional role of Hedgehog in the development of leukemia was confirmed and combined treatment targeting FLT3 and Hedgehog is effective as a therapeutic strategy in this setting, and combined FLT 3 and Hh pathway inhibition limited leukemic growth in vitro and in vivo.
Journal ArticleDOI
Treatment of chronic kidney diseases with histone deacetylase inhibitors
Na Liu,Shougang Zhuang +1 more
TL;DR: Recent advances on the treatment of various chronic kidney diseases with HDACis in pre-clinical models are summarized.
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.
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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.