Results 1 to 10 of about 83,225 (311)

Thermal shift engagement assay for Class IIA histone deacetylase inhibitor screening [PDF]

Results in Chemistry
Histone deacetylase (HDAC) proteins are the targets of several anti-cancer clinical drugs, which motivates future inhibitor development. Class IIA HDAC proteins, HDAC4, HDAC5, HDAC7, and HDAC9, are pseudodeacetylases that lack a key catalytic amino acid ...
Lauren N. Kotsull, Mary Kay H. Pflum
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Tau Stabilizes Chromatin Compaction

Frontiers in Cell and Developmental Biology, 2021
An extensive body of literature suggested a possible role of the microtubule-associated protein Tau in chromatin functions and/or organization in neuronal, non-neuronal, and cancer cells. How Tau functions in these processes remains elusive.
Thomas Rico, Melissa Gilles, Alban Chauderlier, Thomas Comptdaer, Romain Magnez, Maggy Chwastyniak, Herve Drobecq, Florence Pinet, Xavier Thuru, Luc Buée, Marie-Christine Galas, Bruno Lefebvre   +11 more
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Histone Deacetylases and Histone Deacetylase Inhibitors in Neuroblastoma [PDF]

Frontiers in Cell and Developmental Biology, 2020
Histone deacetylases (HDACs) are enzymes that play a key role in regulating gene expression by remodeling chromatin structure. An imbalance of histone acetylation caused by deregulated HDAC expression and activity is known to promote tumor progression in a number of tumor types, including neuroblastoma, the most common solid tumor in children ...
Monica Phimmachanh, Jeremy Z. R. Han, Yolande E. I. O’Donnell, Sharissa L. Latham, Sharissa L. Latham, David R. Croucher, David R. Croucher   +6 more
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Efficacy of histone deacetylase and estrogen receptor inhibition in breast cancer cells due to concerted down regulation of Akt. [PDF]

PLoS ONE, 2013
Hormonal therapy resistance remains a considerable barrier in the treatment of breast cancer. Activation of the Akt-PI3K-mTOR pathway plays an important role in hormonal therapy resistance.
Scott Thomas, K Ted Thurn, Paromita Raha, Stephanie Chen, Pamela N Munster   +4 more
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Cancer cell histone density links global histone acetylation, mitochondrial proteome and histone acetylase inhibitor sensitivity

Communications Biology, 2022
Elevated histone density is associated with global histone acetylation, histone deacetylase inhibitor sensitivity and altered mitochondrial proteome composition, with histone regulator HMGB1 linked to histone density aberrations in many cancer cell lines.
Christopher Bruhn, Giulia Bastianello, Marco Foiani   +2 more
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Histone Deacetylases and Their Isoform-Specific Inhibitors in Ischemic Stroke

Biomedicines, 2021
Cerebral ischemia is the second leading cause of death in the world and multimodal stroke therapy is needed. The ischemic stroke generally reduces the gene expression due to suppression of acetylation of histones H3 and H4.
Svetlana Demyanenko, Valentina Dzreyan, Svetlana Sharifulina   +2 more
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Macrocyclic Histone Deacetylase Inhibitors [PDF]

Current Topics in Medicinal Chemistry, 2010
Histone deacetylase inhibitors (HDACi) are an emerging class of novel anti-cancer drugs that cause growth arrest, differentiation, and apoptosis of tumor cells. In addition, they have shown promise as anti-parasitic, anti-neurodegenerative, anti-rheumatologic and immunosuppressant agents. To date, several structurally distinct small molecule HDACi have
Sandra C, Mwakwari, Vishal, Patil, William, Guerrant, Adegboyega K, Oyelere   +3 more
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Histone deacetylase inhibitors

Journal of Education, Health and Sport, 2020
The human genome is contained in chromatin, which is a complex macromolecular complex. It is made of DNA, histones and non-histone proteins. The structure of chromatin and the process of its rearrangement regulate the process of transcription, and hence gene expression.
Marzena Baran, Paulina Anna Miziak, Katarzyna Bonio   +2 more
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Potential of histone deacetylase inhibitors for the therapy of ovarian cancer

Frontiers in Oncology, 2022
Malignant ovarian tumors bear the highest mortality rate among all gynecological cancers. Both late tumor diagnosis and tolerance to available chemotherapy increase patient mortality.
Fengyi Guo, Hongjing Wang, Hongjing Wang
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Non-Hydroxamate Histone Deacetylase Inhibitors [PDF]

Current Medicinal Chemistry, 2005
A number of histone deacetylase (HDAC) inhibitors have been developed as anticancer agents and most of them are hydroxamic acid derivatives, typified by suberoylanilide hydroxamic acid (SAHA), Trichostatin A (TSA) and NVP-LAQ824. However, hydroxamic acids have been associated with poor pharmacokinetics and severe toxicity. In addition, although isozyme-
Takayoshi, Suzuki, Naoki, Miyata
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