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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Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer
TL;DR: Investigating aspects of HDACi action both in vitro and in vivo will further improve the design of optimized clinical protocols and help to understand the role of histone deacetylases in tumorigenesis.
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Histone deacetylase inhibitors: molecular mechanisms of action
TL;DR: This review focuses on the mechanisms of action of histone deacetylase ( HDAC) inhibitors (HDACi), a group of recently discovered ‘targeted’ anticancer agents that induces different phenotypes in various transformed cells.
Journal ArticleDOI
The role of short-chain fatty acids in microbiota-gut-brain communication.
TL;DR: This Review summarizes existing knowledge on the potential of SCFAs to directly or indirectly mediate microbiota–gut–brain interactions and their interaction with gut–brain signalling pathways including immune, endocrine, neural and humoral routes.
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Epigenetic therapy of cancer: past, present and future
Christine B. Yoo,Peter A. Jones +1 more
TL;DR: With the advent of numerous drugs that target specific enzymes involved in the epigenetic regulation of gene expression, the utilization of epigenetic targets is emerging as an effective and valuable approach to chemotherapy as well as chemoprevention of cancer.
Journal ArticleDOI
Beyond the sequence : Cellular organization of genome function
TL;DR: The functional relevance of spatial and temporal genome organization at three hierarchical levels: the organization of nuclear processes, the higher-order organization of the chromatin fiber, and the spatial arrangement of genomes within the cell nucleus are discussed.
References
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Butyric acid: A small fatty acid with diverse biological functions
TL;DR: In vitro studies suggest that sodium butyrate may be useful in the management of neoplasms by causing selective cell death, and/or cell differentiation and by increasing the cell killing effect in conjuction with currently used tumor therapeutic agents.
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Depudecin induces morphological reversion of transformed fibroblasts via the inhibition of histone deacetylase.
TL;DR: It is demonstrated that depudecin inhibits histone deacetylase (HDAC) activity effectively both in vivo and in vitro and suggested that its ability to induce morphological reversion of transformed cells is the result of its HDAC inhibitory activity.
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Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation.
TL;DR: This is the first report that shows the correlation between HD inhibitory activity and action on cancer cells on a larger series of similar compounds, and supports the use of in vitro systems as screening tools and provides structure-activity relationships that merit further investigation of this interesting target.
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Apicidin, a Histone Deacetylase Inhibitor, Induces Apoptosis and Fas/Fas Ligand Expression in Human Acute Promyelocytic Leukemia Cells
So Hee Kwon,Seong Hoon Ahn,Yong Kee Kim,Gyu-Un Bae,Jong Woo Yoon,Sungyoul Hong,Hoi Young Lee,Yin Won Lee,Hyang Woo Lee,Jeung Whan Han +9 more
TL;DR: The results suggest that apicidin might induce apoptosis through selective induction of Fas/Fas ligand, resulting in the release of cytochrome c from the mitochondria to the cytosol and subsequent activation of caspase-9 and caspases-3.
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Multidimensional Chemical Genetic Analysis of Diversity-Oriented Synthesis-Derived Deacetylase Inhibitors Using Cell-Based Assays
TL;DR: The use of a panel of cell-based assays and small molecule "chemical genetic modifiers" for the discovery of 617 small molecule inhibitors of histone deacetylases from a multidimensional screen of an encoded, diversity-oriented synthesis library is reported.