Rational approaches, design strategies, structure activity relationship and mechanistic insights for anticancer hybrids
A Hybrid drug which comprises the incorporation of two drug pharmacophores in one single
molecule are basically designed to interact with multiple targets or to amplify its effect …
molecule are basically designed to interact with multiple targets or to amplify its effect …
[HTML][HTML] Targeting histone deacetylases with natural and synthetic agents: an emerging anticancer strategy
Cancer initiation and progression are the result of genetic and/or epigenetic alterations.
Acetylation-mediated histone/non-histone protein modification plays an important role in the …
Acetylation-mediated histone/non-histone protein modification plays an important role in the …
Histone deacetylases (HDACs): characterization of the classical HDAC family
Transcriptional regulation in eukaryotes occurs within a chromatin setting, and is strongly
influenced by the post-translational modification of histones, the building blocks of …
influenced by the post-translational modification of histones, the building blocks of …
Anticancer activities of histone deacetylase inhibitors
JE Bolden, MJ Peart, RW Johnstone - Nature reviews Drug discovery, 2006 - nature.com
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 …
have a key role in the epigenetic regulation of gene expression. In addition, the activity of …
Histone deacetylase inhibitors: molecular mechanisms of action
WS Xu, RB Parmigiani, PA Marks - Oncogene, 2007 - nature.com
This review focuses on the mechanisms of action of histone deacetylase (HDAC) inhibitors
(HDACi), a group of recently discovered 'targeted'anticancer agents. There are 18 HDACs …
(HDACi), a group of recently discovered 'targeted'anticancer agents. There are 18 HDACs …
Histone-deacetylase inhibitors: novel drugs for the treatment of cancer
RW Johnstone - Nature reviews Drug discovery, 2002 - nature.com
The opposing actions of histone acetyltransferases (HATs) and histone deacetylases
(HDACs) allow gene expression to be exquisitely regulated through chromatin remodelling …
(HDACs) allow gene expression to be exquisitely regulated through chromatin remodelling …
Histone deacetylase inhibitor selectively induces p21WAF1 expression and gene-associated histone acetylation
VM Richon, TW Sandhoff… - Proceedings of the …, 2000 - National Acad Sciences
Histone deacetylases (HDACs) catalyze the removal of acetyl groups on the amino-terminal
lysine residues of core nucleosomal histones. This activity is associated generally with …
lysine residues of core nucleosomal histones. This activity is associated generally with …
Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells
PA Marks, VM Richon, RA Rifkind - Journal of the National …, 2000 - academic.oup.com
Histone deacetylase (HDAC) inhibitors have been shown to be potent inducers of growth
arrest, differentiation, and/or apoptotic cell death of transformed cells in vitro and in vivo. One …
arrest, differentiation, and/or apoptotic cell death of transformed cells in vitro and in vivo. One …
Histone deacetylase inhibitor (HDACI) mechanisms of action: emerging insights
P Bose, Y Dai, S Grant - Pharmacology & therapeutics, 2014 - Elsevier
Initially regarded as “epigenetic modifiers” acting predominantly through chromatin
remodeling via histone acetylation, HDACIs, alternatively referred to as lysine deacetylase …
remodeling via histone acetylation, HDACIs, alternatively referred to as lysine deacetylase …
Suberoylanilide Hydroxamic Acid, an Inhibitor of Histone Deacetylase, Suppresses the Growth of Prostate Cancer Cells in Vitro and in Vivo
Suberoylanilide hydroxamic acid (SAHA) is the prototype of a family of hybrid polar
compounds that induce growth arrest in transformed cells and show promise for the …
compounds that induce growth arrest in transformed cells and show promise for the …