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

open access: yesResults 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
doaj   +2 more sources

Tau Stabilizes Chromatin Compaction

open access: yesFrontiers 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   +11 more
doaj   +1 more source

Efficacy of histone deacetylase and estrogen receptor inhibition in breast cancer cells due to concerted down regulation of Akt. [PDF]

open access: yesPLoS 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   +4 more
doaj   +1 more source

Cancer cell histone density links global histone acetylation, mitochondrial proteome and histone acetylase inhibitor sensitivity

open access: yesCommunications 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   +2 more
doaj   +1 more source

Histone Deacetylases and Their Isoform-Specific Inhibitors in Ischemic Stroke

open access: yesBiomedicines, 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   +2 more
doaj   +1 more source

Small Molecules Targeting HATs, HDACs, and BRDs in Cancer Therapy

open access: yesFrontiers in Oncology, 2020
Evidence for research over the past decade shows that epigenetic regulation mechanisms run through the development and prognosis of tumors. Therefore, small molecular compounds targeting epigenetic regulation have become a research hotspot in the ...
Donglu Wu   +8 more
doaj   +1 more source

Potential of histone deacetylase inhibitors for the therapy of ovarian cancer

open access: yesFrontiers 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
doaj   +1 more source

Histone deacetylase 2-mediated deacetylation of the Ribonuclease 1 promoter in inflamed human endothelial cells [PDF]

open access: yes, 2020
Endothelial cells (ECs) function as protective barrier to separate the blood from the surrounding tissue by conducting crucial roles in regulation and maintenance of vascular homeostasis, such as control of vessel permeability or coagulation.
Bedenbender, Katrin
core   +1 more source

Design, synthesis, and biological evaluation of novel histone deacetylase 6 selective inhibitors

open access: yesJournal of Saudi Chemical Society, 2022
Histone deacetylase 6 (HDAC6) is distinguished from other HDACs by its ability to deacetylate α-tubulin and HSP90, and was reported to be related to a variety of human diseases, such as cancers, neurodegenerative diseases, and immunological disorders ...
Tianyi Zhang   +8 more
doaj   +1 more source

Reactivation of DNA viruses in association with histone deacetylase inhibitor therapy: a case series report

open access: yesHaematologica, 2009
Histone deacetylase inhibitors are a class of anti-neoplastic agents that induce growth arrest, differentiation, and/or apoptotic cell death of transformed cells in vitro and in vivo.
David Ritchie   +9 more
doaj   +1 more source

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