Results 261 to 270 of about 208,828 (307)

Hydrazides as Inhibitors of Histone Deacetylases

Journal of Medicinal Chemistry
In this Perspective, we have brought together available biological evidence on hydrazides as histone deacetylase inhibitors (HDACis) and as a distinct type of Zn-binding group (ZBG) to be reviewed for the first time in the literature. N-Alkyl hydrazides have transformed the field, providing innovative and practical chemical tools for selective and ...
Maria do Carmo Carreiras, José Marco-Contelles   +1 more
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Histone deacetylase inhibitors

Expert Opinion on Therapeutic Patents, 2007
Sustained efforts towards identifying novel histone deacetylase (HDAC) inhibitors as suitable therapies for the treatment of cancer and other human diseases has been a goal for the pharmaceutical industry during the last decade. In the second half of 2006 these efforts culminated in the FDA granting approval for the first HDAC inhibitor ...
Steve Price, Hazel J Dyke
openaire   +1 more source

The Pharmaceutical Potential of Histone Deacetylase Inhibitors

Current Pharmaceutical Design, 2007
Protein acetylation, catalyzed by the opposing activities of histone deacetylases (HDAC) and histone acetyltransferases, is now recognized to be an important epigenetic modulator of gene transcriptional activity and cell function. As a result of the intense search for HDAC inhibitors (HDACi) during the past fifteen years, a large number of structurally
Elaut, Greetje, Rogiers, Vera, Vanhaecke, Tamara   +2 more
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Heterocyclic ketones as inhibitors of histone deacetylase

Bioorganic & Medicinal Chemistry Letters, 2003
Several heterocyclic ketones were investigated as potential inhibitors of histone deacetylase. Nanomolar inhibitors such as 22 and 25 were obtained, the anti-proliferative activity of which were shown to be mediated by HDAC inhibition.
Anil, Vasudevan, Zhiqin, Ji, Robin R, Frey, Carol K, Wada, Douglas, Steinman, H Robin, Heyman, Yan, Guo, Michael L, Curtin, Jun, Guo, Junling, Li, Lori, Pease, Keith B, Glaser, Patrick A, Marcotte, Jennifer J, Bouska, Steven K, Davidsen, Michael R, Michaelides   +15 more
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Induction of TAp63 by histone deacetylase inhibitors

Biochemical and Biophysical Research Communications, 2010
TAp63 belongs to the p53-tumour suppressor family and is capable of transactivating a set of target genes to induce cell cycle arrest and apoptosis. We showed that treatment of cancer cells with chemo-therapeutic drugs or the histone deacetylase (HDAC) inhibitor Trichostatin A (TSA) results in induction of TAp63 expression, which is in turn related ...
Sayan, BS, Yang, AL, Conforti, F, BERNARDINI, SERGIO, TUCCI, PAOLA, Vasa Nicotera, M, Knight, RA, MELINO, GENNARO   +7 more
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Histone Deacetylase Inhibitors in Cancer Therapy

Current Topics in Medicinal Chemistry, 2019
Histone deacetylases (HDACs), as epigenetic modifiers, are essential for gene transcriptional activities. The alternation of HDACs expression, mutation and/or inappropriate recruitments has been discovered in a broad range of tumors contributing to the tumorigenesis through a serial of biological pathways.
Yijie, Sun, Yanyi, Sun, Saichao, Yue, Yaohe, Wang, Fanghui, Lu   +4 more
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Histone deacetylase inhibitors: gathering pace

Current Opinion in Pharmacology, 2006
Reversible histone acetylation is one of the key mechanisms involved in the epigenetic control of gene expression. A variety of recent studies has revealed a role for acetylation in a much broader repertoire of physiological processes, including proliferation control and protein folding, and has highlighted how a variety of non-histone regulatory ...
Nessa, Carey, Nicholas B, La Thangue
openaire   +2 more sources

Trifluoromethyl ketones as inhibitors of histone deacetylase

Bioorganic & Medicinal Chemistry Letters, 2002
Trifluoromethyl ketones were found to be inhibitors of histone deacetylases (HDACs). Optimization of this series led to the identification of submicromolar inhibitors such as 20 that demonstrated antiproliferative effects against the HT1080 and MDA 435 cell lines.
Robin R, Frey, Carol K, Wada, Robert B, Garland, Michael L, Curtin, Michael R, Michaelides, Junling, Li, Lori J, Pease, Keith B, Glaser, Patrick A, Marcotte, Jennifer J, Bouska, Shannon S, Murphy, Steven K, Davidsen   +11 more
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Anticancer activities of histone deacetylase inhibitors

Nature Reviews Drug Discovery, 2006
Histone deacetylases (HDACs) are enzymes involved in the remodelling of chromatin, and have a key role in the epigenetic regulation of gene expression. In addition, the activity of non-histone proteins can be regulated through HDAC-mediated hypo-acetylation.
Jessica E, Bolden, Melissa J, Peart, Ricky W, Johnstone   +2 more
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Histone deacetylase inhibitors in myelodysplastic syndrome

Best Practice & Research Clinical Haematology, 2004
Histone deacetylase (HDAC) inhibitors are amongst the newer therapies being introduced in refractory, relapsed, and resistant disease. These agents are mechanism-based and their use is targeted to the diseased cell or tissue. HDACs are key enzymes in the regulation of gene expression.
Kapil, Bhalla, Alan, List
openaire   +2 more sources