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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Organization, Integration and Assembly of Genetic and Epigenetic Regulatory Machinery in Nuclear Microenvironments: Implications for Biological Control in Cancer
Gary S. Stein,Sayyed K. Zaidi,Janet L. Stein,Jane B. Lian,Andre J. Van Wijnen,Martin Montecino,Daniel W. Young,Amjad Javed,Jitesh Pratap,Je-Yong Choi,Syed A. Ali,Sandhya Pande,Mohammad Q. Hassan +12 more
TL;DR: High throughput imaging of cells, tissues, and tumors, including live cell analysis, is expanding research's capabilities toward translating components of nuclear organization into novel strategies for cancer diagnosis and therapy.
QSAR Modeling of Sulfonamide Inhibitors of Histone Deacetylase
TL;DR: In this paper, a new set of sulfonamide derivatives applying linear free energy related (LFER) approach of Hansch was used to explain the structural requirements of sulfamide derivatives for histone deacetylase inhibition.
Journal ArticleDOI
The effect of combined treatment with sodium phenylbutyrate and cisplatin, erlotinib, or gefitinib on resistant NSCLC cells.
TL;DR: Results suggest a potential role of NaPB as a sensitizing agent in NSCLC and suggest that NaPB can potentiate the effect of cisplatin, erlotinib, and gefitinib on A549, Calu1, and H1650 cell lines.
Molecular Mechanism of Nucleotide Excision Repair Deficiency in Novel Breast Cancer Cell Lines
TL;DR: The Unscheduled DNA Synthesis Assay has shown that stage I and stage II breast tumors are deficient in functional NER capacity as compared to non-diseased controls, consistent with a transcriptional regulatory mechanism including both methylation and other transcription factor based functions.
Journal Article
A structure–activity relationship survey of histone deacetylase (HDAC) inhibitors
TL;DR: A novel rank-based ant system is elaborated to generate a QSAR model for the prediction of histone deacetylase inhibition activity that had high prediction power and was validated by predicting the enzyme inhibition of 79 compounds as the external validation set.
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.