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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Delphinidin sensitizes prostate cancer cells to TRAIL-induced apoptosis, by inducing DR5 and causing caspase-mediated HDAC3 cleavage
Hyeonseok Ko,Mi-Hyeon Jeong,Hyelin Jeon,Gi-Jun Sung,Youngsin So,Inki Kim,Jaekyoung Son,Sang-wook Lee,Ho-Geun Yoon,Kyung-Chul Choi +9 more
TL;DR: Delphinidin sensitizes prostate cancer cells to TRAIL-induced apoptosis by inducing DR5, thus causing caspase-mediated HDAC3 cleavage, and reveals a potential way of chemoprevention of prostate cancer by enabling TRAil-mediated apoptosis.
Journal ArticleDOI
Combination therapy with the histone deacetylase inhibitor LBH589 and radiation is an effective regimen for prostate cancer cells.
Weiwei Xiao,Peter Graham,Peter Graham,Jingli Hao,Jingli Hao,Lei Chang,Lei Chang,Jie Ni,Jie Ni,Carl Power,Qihan Dong,Qihan Dong,John H. Kearsley,John H. Kearsley,Yong Li,Yong Li +15 more
TL;DR: Investigation of the in vitro effect of LBH589 alone and in combination with RT on the growth and survival of CaP cell lines and the possible mechanisms of radiosensitization suggest thatLBH589 is a potential agent to increase radiosensitivity of human CaP cells.
Journal ArticleDOI
YM753, a novel histone deacetylase inhibitor, exhibits antitumor activity with selective, sustained accumulation of acetylated histones in tumors in the WiDr xenograft model.
Nobuaki Shindoh,Masamichi Mori,Yoh Terada,Kazuo Oda,Nobuaki Amino,Aya Kita,Masatoshi Taniguchi,Kin-Ya Sohda,Koji Nagai,Yoshihiro Sowa,Yuhta Masuoka,Masaya Orita,Masao Sasamata,Hitoshi Matsushime,Kiyoshi Furuichi,Toshiyuki Sakai +15 more
TL;DR: Evidence is provided that YM753 has antitumor activity that is the result of selective, sustained accumulation of acetylated histones in tumor tissues despite rapid disappearance of the drug from the plasma, suggesting that the novel HDAC inhibitors has attractive pharmacodynamic and pharmacokinetic properties giving it potential as an antitumors agent.
Journal ArticleDOI
Improved Synthesis and Structural Reassignment of MC1568: A Class IIa Selective HDAC Inhibitor
TL;DR: An improved synthesis and structural reassignment of the class IIa selective histone deacetylase (HDAC) inhibitor MC1568 are described.
Journal ArticleDOI
Phase I and pharmacokinetic study of vorinostat (suberoylanilide hydroxamic acid) in Japanese patients with solid tumors.
Yutaka Fujiwara,Noboru Yamamoto,Yasuhide Yamada,Kazuhiko Yamada,Tetsuya Otsuki,Shinichi Kanazu,Takashi Iwasa,James S. Hardwick,Tomohide Tamura +8 more
TL;DR: Vorinostat doses of 200 mg twice daily or 500 mg once daily for 14 days followed by a 7‐day rest were well tolerated and are candidate doses for phase II trials, although a maximum tolerated dose was not reached.
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.