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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Novel hybrid molecule overcomes the limited response of solid tumours to HDAC inhibitors via suppressing JAK1-STAT3-BCL2 signalling
Zhi Huang,Wei Zhou,Yongtao Li,Mei Cao,Tianqi Wang,Yakun Ma,Qingxiang Guo,Xin Wang,Chao Zhang,Chenglan Zhang,Wenzhi Shen,Yanhua Liu,Yanan Chen,Jianyu Zheng,Shengyong Yang,Yan Fan,Yan Fan,Rong Xiang,Rong Xiang +18 more
TL;DR: Xia et al. as discussed by the authors developed a hybrid histone deacetylase inhibitor that sensitized solid tumours to HDAC-targeted treatment, which showed good pharmacokinetics and low toxicity.
Journal ArticleDOI
Energy based pharmacophore mapping of HDAC inhibitors against class I HDAC enzymes
TL;DR: This study combines the insilico docking and energy-optomized pharmacophore (e-pharmacophore) mapping of several known HDACi's to identify the structural variants that are significant for the interactions against each of the four class I HDAC enzymes.
Journal ArticleDOI
A phase I, pharmacokinetic, and pharmacodynamic study of two schedules of vorinostat in combination with 5-fluorouracil and leucovorin in patients with refractory solid tumors.
Marwan Fakih,Marwan Fakih,Gerald J. Fetterly,Merrill J. Egorin,Josephia R. Muindi,Igor Espinoza-Delgado,James A. Zwiebel,Alan Litwin,Julianne L. Holleran,Kangsheng Wang,Robert B. Diasio +10 more
TL;DR: The maximum tolerated dose (MTD) of daily or twice daily vorinostat × 3 days when combined with fixed doses of 5-fluorouracil and leucovorin every 2 weeks supports further clinical development of this combination in refractory colorectal cancer.
Journal ArticleDOI
Histone deacetylase inhibitors increase virus gene expression but decrease CD8+ cell antiviral function in HTLV-1 infection.
Angelina J. Mosley,Kiran Meekings,Corinna McCarthy,Dawn Shepherd,Vincenzo Cerundolo,Ralph Mazitschek,Yuetsu Tanaka,Graham P. Taylor,Charles R. M. Bangham +8 more
TL;DR: Observations indicate that HDIs may reduce the efficiency of cytotoxic T-cell (CTL) surveillance of HTLV-1 in vivo, and recommend caution in the use of HDIs in nonmalignant cases of HTlv-1 infection.
Journal ArticleDOI
Redifferentiation of radioiodine-refractory thyroid cancers
Camille Buffet,Johanna Wassermann,Fabio Hecht,Laurence Leenhardt,Corinne Dupuy,Lionel Groussin,Charlotte Lussey-Lepoutre +6 more
TL;DR: Different redifferentiation strategies based on the underlying molecular mechanism leading to the sodium iodide symporter (NIS) and radioiodine uptake reinduction are reviewed, i.e. by modulating signaling pathways, N IS transcription, NIS trafficking to the plasma membrane, Nis post-transcriptional regulation, by gene therapy and other potential strategies.
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.
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.