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
Patent status of histone deacetylase inhibitors
TL;DR: This review summarises the patent literature published from mid-2002 to early 2004 containing claims directed towards HDAC inhibitor structures, together with discussion of the related primary literature.
Journal ArticleDOI
CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo
Z. Alexander Cao,Kathryn E. Bass,Sriram Balasubramanian,Liang Liu,Brian E. Schultz,Erik Verner,YuQin Dai,Rafael A. Molina,Jack R. Davis,Shawn Misialek,Martin Sendzik,Christine Orr,Ling Leung,Ondine Callan,Peter R. Young,Stacie A. Dalrymple,Joseph J. Buggy +16 more
TL;DR: Results reveal CRA-026440 to be a novel HDAC inhibitor with potent antitumor activity and when used in combination with Avastin, achieved greater preclinical efficacy in HCT 116 colorectal tumor model.
Journal ArticleDOI
Target specificity and off-target effects as determinants of cancer drug efficacy
Maria C. Shoshan,Stig Linder +1 more
TL;DR: Clinically effective targeted agents are reminiscent of conventional agents such as cisplatin and doxorubicin, which are known to have several cellular targets, but these drugs inhibit multiple kinases and/or may display off-target activities.
Journal ArticleDOI
Histone modifying enzymes: novel disease biomarkers and assay development.
Fei Ma,Chun-yang Zhang +1 more
TL;DR: In this review, the recent researches about the histone modifying enzymes as the disease biomarkers are summarized, and the development of methods for hist one modifying enzyme assays are highlighted.
Journal ArticleDOI
Histones: Controlling Tumor Signaling Circuitry
TL;DR: How recent discoveries about chromatin modifications, particularly histone acetylation, are shaping knowledge of cell biology and the understanding of the molecular circuitry governing tumor progression is discussed and whether recent insights may extend to novel therapeutic approaches is considered.
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.
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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.
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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.