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
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Patent
Composition and method for the treatment of diseases affected by histone deacetylase inhibitors
TL;DR: In this article, the authors describe methods of treatment and compositions for treating diseases related to the activity of a histone deacetylase in a subject by administering to the subject an effective amount of a modified FK228 compound comprising an amino acid conjugate which constitutes an amino thiol, a hydroxy thiol or a dithiol, or a hydroxamic acid, instead of a Hydroxy-mercapto-heptenoic acid moiety in FK 228.
Journal ArticleDOI
Lipotropes enhance the anti-proliferative effect of chemotherapeutic drugs in MCF-7 human breast cancer cells.
TL;DR: It is suggested that lipotropes induce apoptosis, inhibit cell growth, and display anti-proliferative effects with SAHA and DOX in MCF-7 cells, which may be tested further in animal models as potential therapeutic agents for reducing breast cancer risk.
Posted ContentDOI
Inhibition of histone deacetylase 1 or 2 reduces microglia activation through a gene expression independent mechanism.
TL;DR: This study has identified that selective HDAC inhibition with inhibitors apicidin, MS-275 or MI-192, or specific knockdown of HDAC1 or 2 using siRNA, suppresses the expression of cytokines interleukin-6 (IL-6) and tumour necrosis factor-alpha (TNF-α) in BV2 murine microglia activated with lipopolysaccharide (LPS).
Journal ArticleDOI
MS-275 Chemical Analogues Promote Hemoglobin Production and Erythroid Differentiation of K562 Cells.
Stella Voskou,Stella Voskou,Marios Phylactides,Andreas Afantitis,Georgia Melagraki,Andreas Tsoumanis,Panayotis A Koutentis,Tina Mitsidi,Styliana I. Mirallai,Marina Kleanthous +9 more
TL;DR: Nine novel agents exhibited significant hemoglobin (Hb)-inducing and erythroid differentiation activities in the human K562 erystroleukemia cell line, demonstrating the effectiveness of the evaluated analogues of the histone deacetylase inhibitor MS-275.
Journal ArticleDOI
A proteomic analysis of protein variations during differentiation of v-myb-transformed monoblasts.
Eva Ondroušková,Karolína Povolná,Petr Váňa,Petr Beneš,Hana Konečná,Zbyněk Zdráhal,Jan Šmarda +6 more
TL;DR: The first comparative proteome analysis of v-myb-transformed monoblasts BM2 focused on identification of proteins involved in their terminal differentiation is presented, finding that expression of several proteins participating in cell cytoskeleton rearrangement, heat shock response, proteosynthesis and cell signaling was altered in TPA- or TSA-treated cells.
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.
Journal ArticleDOI
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.
Journal ArticleDOI
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.