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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Journal ArticleDOI
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
Victor Andrianov,Vija Gailite,Daina Lola,Einars Loza,Valentina Semenikhina,Ivars Kalvinsh,Paul W. Finn,Kamille Dumong Petersen,James Ritchie,Nagma Khan,Anthony Tumber,Laura S. Collins,Sree M. Vadlamudi,Fredrik Björkling,Maxwell Sehested +14 more
TL;DR: A series of novel amide derivatives have been synthesized and evaluated for their ability to inhibit human HDACs, and compounds such as (E)-N-[6-(hydroxyamino)-6-oxohexyl]-3-quinolinyl)-2-propenamide (27) (HDAC IC(50) 8 nM) showed potent in vivo activity in the P388 mouse leukemia syngeneic model.
Journal ArticleDOI
Biological and Biophysical Properties of the Histone Deacetylase Inhibitor Suberoylanilide Hydroxamic Acid Are Affected by the Presence of Short Alkyl Groups on the Phenyl Ring
Frédérik Oger,Aurélien Lecorgne,Elisa Sala,Vanessa Nardese,Florence Demay,Soizic Chevance,Danielle C. Desravines,Nataliia Aleksandrova,Rémy Le Guével,Simone Lorenzi,Andrea R. Beccari,Peter Barath,Darren J. Hart,Arnaud Bondon,Daniele Carettoni,Gérard Simonneaux,Gilles Salbert +16 more
TL;DR: The synthesis and biological evaluation of a new series of compounds derived from SAHA by substituting short alkyl chains at various positions of the phenyl ring induced variable effects ranging from partial loss of activity to increased potency.
Patent
Combination therapies using HDAC inhibitors
Henri Lichenstein,Mike Jeffers,Xiaozhang Qian,Maxwell Sehested,Kamille Dumong Petersen,James Ritchie +5 more
TL;DR: In this paper, a method for treating cancer such as lung cancer, multiple myeloma, lymphoma, and epithelial ovarian cancer, comprising the administration to a patient in need thereof a first amount or dose of a histone deacetylase (HDAC) inhibitor, such as PXD-101, and a second amount of another chemotherapeutic agent such as dexamethasone or 5fluorouracil, or an epidermal growth factor receptor (EGFR) inhibitor such as TarcevaU, wherein the first and second amounts or
Journal ArticleDOI
Hypoxia suppresses E‐cadherin and enhances matrix metalloproteinase‐2 expression favoring esophageal carcinoma migration and invasion via hypoxia inducible factor‐1 alpha activation
Shaowu Jing,Y.‐d. Wang,Chen Lq,M.‐x. Sang,M.‐m. Zheng,Guo-gui Sun,Qing Liu,Y. J. Cheng,Cong-rong Yang +8 more
TL;DR: In this paper, the authors explored the molecular mechanism of hypoxia inducible factor-1 alpha (HIF-1 Alpha) action on migration and invasion of esophageal carcinoma cells.
Journal ArticleDOI
The HDAC Inhibitor Quisinostat (JNJ-26481585) Supresses Hepatocellular Carcinoma alone and Synergistically in Combination with Sorafenib by G0/G1 phase arrest and Apoptosis induction.
Bin He,Longfei Dai,Xiaoqian Zhang,Diyu Chen,Jingbang Wu,Xiaode Feng,Yanpeng Zhang,Haiyang Xie,Lin Zhou,Jian Wu,Shusen Zheng +10 more
TL;DR: This study indicated that quisinostat, as a novel chemotherapy for HCC, exhibited excellent antitumor activity in vitro and vivo, which was even enhanced by the addition of sorafenib, implying combination of quisinOSTat with sorafanib a promising and alternative therapy for patients with advanced hepatocellular carcinoma.
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.
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.