Inhibition of androgen receptor activity by histone deacetylase 4 through receptor SUMOylation [PDF]
The transcriptional activity of the androgen receptor (AR) is regulated by both ligand binding and post-translational modifications, including acetylation and small ubiquitin-like modifier (SUMO)ylation. Histone deacetylases (HDACs) are known to catalyze the removal of acetyl groups from both histones and non-histone proteins.
Yang, Yonghua +8 more
openaire +2 more sources
Clinical trials on PARP inhibitors in urothelial carcinoma (UC) showed limited efficacy and a lack of predictive biomarkers. We propose SLFN5, SLFN11, and OAS1 as UC‐specific response predictors. We suggest Talazoparib as the better PARP inhibitor for UC than Olaparib.
Jutta Schmitz +15 more
wiley +1 more source
Pharmacological activation of SIRT6 triggers lethal autophagy in human cancer cells [PDF]
Sirtuin 6 (SIRT6) is a member of the NAD+-dependent class III deacetylase sirtuin family, which plays a key role in cancer by controlling transcription, genome stability, telomere integrity, DNA repair, and autophagy.
Annamaria Biroccio, And +13 more
core +2 more sources
Caspase-dependent Regulation of Histone Deacetylase 4 Nuclear-Cytoplasmic Shuttling Promotes Apoptosis [PDF]
Histone deacetylases (HDACs) are important regulators of gene expression as part of transcriptional corepressor complexes. Here, we demonstrate that caspases can repress the activity of the myocyte enhancer factor (MEF)2C transcription factor by regulating HDAC4 processing. Cleavage of HDAC4 occurs at Asp 289 and disjoins the carboxy-terminal fragment,
PARONI G +5 more
openaire +4 more sources
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
The simultaneous effect of valproic acid and gamma radiation on telomerase activity and bax and Bcl-2 protein levels in MCF-7 breast cancer cell line [PDF]
Background: Breast cancer is one of the most prevalent types of cancer. Factors such as ionizing radiation and chemotherapeutic agents can trigger apoptosis and cancer cell death.
Asadi, J. +3 more
core +1 more source
Dephosphorylation and Caspase Processing Generate Distinct Nuclear Pools of Histone Deacetylase 4 [PDF]
From the nucleus, histone deacetylase 4 (HDAC4) regulates a variety of cellular processes, including growth, differentiation, and survival, by orchestrating transcriptional changes. Extracellular signals control its repressive influence mostly through regulating its nuclear-cytoplasmic shuttling.
PARONI, Gabriela +7 more
openaire +3 more sources
ATF4‐mediated stress response as a therapeutic vulnerability in chordoma
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
Interaction between cellular retinoic acid-binding protein II and histone hypoacetylation in renal cell carcinoma [PDF]
Renal cell carcinoma is a rare but serious malignancy. Since a reduction in the level of retinoic acid receptor beta 2 (RARbeta2) expression in cancer cells due in part to histone hypoacetylation which is controlled by histone deacetylase (HD), the study
Wiwanitkit, Viroj
core +1 more source
Sirtuin functions and modulation: from chemistry to the clinic [PDF]
Sirtuins are NAD+ -dependent histone deacetylases regulating important metabolic pathways in prokaryotes and eukaryotes and are involved in many biological processes such as cell survival, senescence, proliferation, apoptosis, DNA repair, cell ...
Altucci, Lucia +9 more
core +2 more sources

