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Inside HDACs with more selective HDAC inhibitors

European Journal of Medicinal Chemistry, 2016
Inhibitors of histone deacetylases (HDACs) are nowadays part of the therapeutic arsenal mainly against cancers, with four compounds approved by the Food and Drug Administration. During the last five years, several groups have made continuous efforts to improve this class of compounds, designing more selective compounds or compounds with multiple ...
Roche, Joëlle, Bertrand, Philippe
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NO-HDAC dual inhibitors

European Journal of Medicinal Chemistry, 2022
HDAC inhibitors and NO donors have both demonstrated independently broad therapeutic potential in a variety of diseases. Borretto et al. presented the topic of NO-HDAC dual inhibitors for the first time in 2013 as an attractive new topic. Here we collected the general structure of all synthesized NO-HDAC dual inhibitors, lead compounds, synthesis ...
Negar, Omidkhah, Razieh, Ghodsi
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HDAC Inhibitors

2016
Lysine acetylation in proteins is one of the most abundant posttranslational modifications in eukaryotic cells. The dynamic homeostasis of lysine acetylation and deacetylation is dictated by the action of histone acetyltransferases (HAT) and histone deacetylases (HDAC).
Heidi, Olzscha   +3 more
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Inside HDAC with HDAC inhibitors

European Journal of Medicinal Chemistry, 2010
Histone deacetylase inhibitors are a large group of diverse molecules intrinsically able to inhibit cell proliferation in various cancer cell lines. Their apoptotic effects have been linked to the modulation in the expression of several regulatory tumor suppressor genes caused by the modified status of histone acetylation, a key event in chromatin ...
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HDAC inhibitors in HIV

Immunology & Cell Biology, 2011
Combination antiretroviral therapy (cART) has led to a very substantial reduction in morbidity and mortality in HIV‐infected patients; however, cART alone is unable to cure HIV and therapy is lifelong. Therefore, a new strategy to cure HIV is urgently needed.
Wightman, F   +3 more
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ChemInform Abstract: Inside HDACs with More Selective HDAC Inhibitors

ChemInform, 2016
AbstractReview: 194 refs.
Joelle Roche, Philippe Bertrand
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Teratogenic Activity of HDAC Inhibitors

Current Pharmaceutical Design, 2014
Modification of the terminal tails of histones is considered one of the documented mechanisms for epigenetic control of gene expression. Histone deacetylase inhibitors (HDACi) lead to a state of hyperacetylation of histone, a condition that can affect normal gene transcription.
E. Giavini, E. Menegola
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Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

Nature Biotechnology, 2011
The development of selective histone deacetylase (HDAC) inhibitors with anti-cancer and anti-inflammatory properties remains challenging in large part owing to the difficulty of probing the interaction of small molecules with megadalton protein complexes. A combination of affinity capture and quantitative mass spectrometry revealed the selectivity with
Marcus, Bantscheff   +23 more
openaire   +2 more sources

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