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
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.
Journal ArticleDOI
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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Journal ArticleDOI
Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation.
Kathryn M. Koeller,Stephen J. Haggarty,Brian D. Perkins,Igor Leykin,Jason C. Wong,Ming-Chih J. Kao,Stuart L. Schreiber +6 more
TL;DR: To examine cell cycle arrest induced by HDAC inhibitor trichostatin A, a cytoblot cell-based screen was used to identify small molecule suppressors of this process, and TSA suppressors (ITSAs) counteract TSA-induced cell cycle Arrest, histone acetylation, and transcriptional activation.
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Novel hydroxamate and anilide derivatives as potent histone deacetylase inhibitors: synthesis and antiproliferative evaluation.
Giliane Bouchain,Daniel Delorme +1 more
TL;DR: The recent progress being made in the laboratories in the development of two new families of potent HDAC inhibitors: sulfonamide hydroxamic acids and anilides, as well as TSA-like straight chain derivatives are reviewed.
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The discovery of NVP-LAQ824: from concept to clinic.
TL;DR: A systematic structural exploration of cinnamyl hydroxamates based on NVP-LAK974 was undertaken with the goal of finding a novel, well-tolerated and efficacious HDAC inhibitor, and several derivatives were found to be efficacious in the xenograft assay.
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Analogues of trichosтatin a and trapoxin B as histone deacetylase inhibitors
TL;DR: A set of simple analogues in as little as four synthetic steps that have inhibitory potencies in the range of known cyclotetrapeptide inhibitors are prepared for the design of potent inhibitors of histone deacetylase.
Journal ArticleDOI
Design and synthesis of a novel class of histone deacetylase inhibitors
Rico Lavoie,Giliane Bouchain,Sylvie Frechette,Soon Hyung Woo,Elie Abou Khalil,Silvana Leit,Marielle Fournel,Pu T. Yan,Marie-Claude Trachy-Bourget,Carole Beaulieu,Zuomei Li,Jeffrey M. Besterman,Daniel Delorme +12 more
TL;DR: The synthesis of a series of sulfonamide hydroxamic acids is described, and optimization of this series by substitution of the terminal aromatic ring yielded HDAC inhibitors with good in vitro and in vivo activities.