Results 171 to 180 of about 13,054 (213)

Downregulation of Mcl-1 potentiates HDACi-mediated apoptosis in leukemic cells [PDF]

Leukemia, 2008
Mcl-1 is an antiapoptotic Bcl-2 family member, whose degradation is supposedly required for the induction of apoptosis. However, histone deacetylase inhibitors (HDACi) induce apoptosis primarily through the Bak/Mcl-1/Noxa and Bim pathways without decreasing Mcl-1.
M J S Dyer, G M Cohen, Dyer M J S
exaly   +5 more sources

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HDACi – Targets beyond chromatin

Cancer Letters, 2009
Histone deacetylases (HDACs) play an important role in gene regulation. Inhibitors of HDACs (HDACi) are novel anti-cancer drugs, which induce histone (hyper-) acetylation and counteract aberrant gene repression. On the other hand, HDACi treatment can also result in decreased gene expression, and targeting HDACs affects more than chromatin.
Oliver H Kramer, Thorsten Heinzel
exaly   +3 more sources

Analysis of HDACi-Coupled Nanoparticles: Opportunities and Challenges

2022
Systemic administration of histone deacetylase inhibitors (HDACi), like valproic acid (VPA), is often associated with rapid drug metabolization and untargeted tissue distribution. This requires high-dose application that can lead to unintended side effects.
Marie, Kühne, Susanne, Hofmann, Henry, Lindemann, Zoltán, Cseresnyés, Andreas, Dzierza, Daniel, Schröder, Maren, Godmann, Andreas, Koschella, Christian, Eggeling, Dagmar, Fischer, Marc Thilo, Figge, Thomas, Heinze, Thorsten, Heinzel   +12 more
openaire   +2 more sources

HDACi Delivery Systems Based on Cellulose Valproate Nanoparticles

2022
The ability of histone deacetylase inhibitors (HDACi) like valproic acid (VPA) as a therapeutic for inflammatory diseases or cancer has increased the interest in HDACi and their targeted transport to diseased tissues. Administration of VPA immobilized on polymeric carriers was found to be a suitable approach to circumvent drawbacks such as rapid ...
Henry, Lindemann, Marie, Kühne, Andreas, Koschella, Maren, Godmann, Thorsten, Heinzel, Thomas, Heinze   +5 more
openaire   +2 more sources

DNMTi/HDACi combined epigenetic targeted treatment induces reprogramming of myeloma cells in the direction of normal plasma cells

British Journal of Cancer, 2018
International audienceBackground: Multiple myeloma (MM) is the second most common hematologic malignancy. Aberrant epigenetic modifications have been reported in MM and could be promising therapeutic targets.
Angelique Bruyer, Ken Maes, Alboukadel Kassambara   +2 more
exaly   +2 more sources

Assessment of HDACi-Induced Cytotoxicity

2016
The chromatin contains the genetic and the epigenetic information of a eukaryotic organism. Posttranslational modifications of histones, such as acetylation and methylation, regulate their structure and control gene expression. Histone acetyltransferases (HATs) acetylate lysine residues in histones while histone deacetylases (HDACs) remove this ...
Lisa, Marx-Blümel, Christian, Marx, Marie, Kühne, Jürgen, Sonnemann   +3 more
openaire   +2 more sources

Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat

Bioorganic & Medicinal Chemistry Letters, 2022
The combination of androgen receptor antagonists with histone deacetylase inhibitors (HDACi) has been shown to be more effective than antiandrogens alone in halting growth of prostate cancer cell lines. Here we have designed, synthesized and assessed a series of antiandrogen/HDACi hybrids by combining structural features of enzalutamide with either ...
Ryan R.G. Barrett, Claire Nash, Marine Diennet, David Cotnoir-White, Christopher Doyle, Sylvie Mader, Axel A. Thomson, James L. Gleason   +7 more
openaire   +2 more sources

Effects of HDACi on Immunological Functions

2016
Histone deacetylase inhibitors (HDACi) are used as therapeutics for several B cell-derived malignancies. Furthermore, they have been shown to modulate the response of the immune system, like the B cell function. HDACi treatment affects differentiation, proliferation, and survival of B cells.
René, Winkler, Christian, Kosan
openaire   +2 more sources

Analyzing Lymphoma Development and Progression Using HDACi in Mouse Models

2022
Besides the physiological role of histone deacetalylases in maintaining normal cellular integrity, the acetylation landscape is changed in cancer cells, which has been implicated as a potential target in cancer therapy. The overexpression of certain HDACs correlates with specific cancer types.
Eva-Maria, Piskor, René, Winkler, Christian, Kosan   +2 more
openaire   +2 more sources

Generation and Assessment of Fusions Between HDACi and TKi

2016
Chimeric compounds combine the structural features of inhibitors of histone deacetylases (HDACi) and tyrosine kinase inhibitors (TKi), and therefore unite the effects of a dual-targeting strategy in one compound. Here, we describe the generation of such hybrid molecules.
Siavosh, Mahboobi, Bernadette, Pilsl, Andreas, Sellmer   +2 more
openaire   +2 more sources