Results 51 to 60 of about 116,207 (325)
Design and Synthesis of Hybrid Compounds as Epigenetic Modifiers
Pharmaceuticals, 2021 Epigenetic modifiers acting through polypharmacology mechanisms are promising compounds with which to treat several infectious diseases. Histone deacetylase (HDAC) enzymes, mainly class I, and extra-terminal bromodomains (BET) are involved in viral ...
Juliana Romano Lopes +4 more
doaj +1 more source
The role of histone modifications in transcription regulation upon DNA damage
FEBS Letters, EarlyView.This review discusses the critical role of histone modifications in regulating gene expression during the DNA damage response (DDR). By modulating chromatin structure and recruiting repair factors, these post‐translational modifications fine‐tune transcriptional programmes to maintain genomic stability.
Angelina Job Kolady, Siyao Wang
wiley +1 more source
Quantification of histone deacetylase isoforms in human frontal cortex, human retina, and mouse brain. [PDF]
PLoS ONE, 2015 Histone deacetylase (HDAC) inhibition has promise as a therapy for Alzheimer's disease (AD) and other neurodegenerative diseases. Currently, therapeutic HDAC inhibitors target many HDAC isoforms, a particularly detrimental approach when HDAC isoforms are
Kyle W Anderson +5 more
doaj +1 more source
AKT activation controls cell survival in response to HDAC6 inhibition. [PDF]
, 2016 HDAC6 is emerging as an important therapeutic target for cancer. We investigated mechanisms responsible for survival of tumor cells treated with a HDAC6 inhibitor.
Aboagye, EO +3 more
core +1 more source
Molecular Oncology, EarlyView.HDAC4 is degraded by the E3 ligase FBXW7. In colorectal cancer, FBXW7 mutations prevent HDAC4 degradation, leading to oxaliplatin resistance. Forced degradation of HDAC4 using a PROTAC compound restores drug sensitivity by resetting the super‐enhancer landscape, reprogramming the epigenetic state of FBXW7‐mutated cells to resemble oxaliplatin ...
Vanessa Tolotto +13 more
wiley +1 more source
Drug Design, Development and Therapy, 2022 Suhua Wang,1,2 Siyuan Han,1,2 Weiyan Cheng,1,2 Ruoyang Miao,1,2 Shasha Li,1,2 Xin Tian,1,2 Quancheng Kan1,2 1Department of Pharmacy, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, 450052, People’s Republic of China; 2Henan Key ...
Wang S +6 more
doaj
Effects of 5-Fluorouracil on the Expression of Epigenetic Enzymes and Promoter Methylation of Selected Genes in Monolayer and Spheroid Cultures of Colorectal Cancer Cells [PDF]
Pharmaceutical SciencesBackground: Emerging evidence suggests that epigenetic mechanisms contribute to 5-fluorouracil (5-FU) resistance in colorectal cancer (CRC). However, there is limited research on the direct impact of 5-FU on epigenetic alterations in CRC.
Maryam Niknam +4 more
doaj +1 more source
Bifunctional HDAC Therapeutics: One Drug to Rule Them All?
Molecules, 2020 Histone deacetylase (HDAC) enzymes play crucial roles in epigenetic gene expression and are an attractive therapeutic target. Five HDAC inhibitors have been approved for cancer treatment to date, however, clinical applications have been limited due to ...
Joshua P. Smalley +2 more
doaj +1 more source
Human gut bacteria as potent class I histone deacetylase inhibitors in vitro through production of butyric acid and valeric acid. [PDF]
PLoS ONE, 2018 Overexpression of histone deacetylase (HDAC) isoforms has been implicated in a variety of disease pathologies, from cancer and colitis to cardiovascular disease and neurodegeneration, thus HDAC inhibitors have a long history as therapeutic targets.
Samantha Yuille +4 more
doaj +1 more source
ATF4‐mediated stress response as a therapeutic vulnerability in chordoma
Molecular Oncology, EarlyView.We screened 5 chordoma cell lines against 100+ inhibitors of epigenetic and metabolic pathways and kinases and identified halofuginone, a tRNA synthetase inhibitor. Mechanistically halofuginone induces an integrated stress response, with eIF2alpha phosphorylation, activation of ATF4 and its target genes CHOP, ASNS, INHBE leading to cell death ...
Lucia Cottone +11 more
wiley +1 more source