Genome Biology, 2019 Histone acetylation plays a central role in gene regulation and is sensitive to the levels of metabolic intermediates. However, predicting the impact of metabolic alterations on acetylation in pathological conditions is a significant challenge.
Fangzhou Shen +4 more
doaj +1 more source
Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPX
E-Journal of Chemistry, 2011 The inhibition of HDAC (histone deacetylase) activity by specific inhibitors induces growth arrest, differentiation and apoptosis of transformed or several cancer cells. Some of these inhibitors are in clinical trial at phase I or phase II. The discovery
Lynda Ekou +3 more
doaj +1 more source
Histone Deacetylase Inhibitors from Marine Invertebrates
Biology, 2020 Histone deacetylases (HDACs) are key components of the epigenetic machinery controlling gene expression. They are involved in chromatin remodeling events via post-translational histone modifications but may also act on nonhistone proteins, influencing ...
Claudio Luparello +3 more
doaj +1 more source
Sirtuin functions and modulation: from chemistry to the clinic [PDF]
, 2016 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
HDAC1 inhibition by MS-275 in mesothelial cells limits cellular invasion and promotes MMT reversal [PDF]
, 2018 Peritoneal fibrosis is a pathological alteration of the peritoneal membrane occurring in a variety of conditions including peritoneal dialysis (PD), post-surgery adhesions and peritoneal metastases.
Battistelli, Cecilia +14 more
core +1 more source
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 +2 more
doaj +1 more source
New histone deacetylase inhibitors as potential therapeutic tools for advanced prostate carcinoma [PDF]
, 2008 The anti-epileptic drug valproic acid is also under trial as an anti-cancer agent due to its histone deacetylase (HDAC) inhibitory properties. However, the effects of valproic acid (VPA) are limited and concentrations required for exerting anti ...
Atmaca, Akin +8 more
core +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
New clinical developments in histone deacetylase inhibitors for epigenetic therapy of cancer
Journal of Hematology & Oncology, 2009 DNA methylation and histone acetylation are two well known epigenetic chromatin modifications. Epigenetic agents leading to DNA hypomethylation and histone hyperacetylation have been approved for treatment of hematological disorders.
Ma Yuehua, Cang Shundong, Liu Delong
doaj +1 more source
Phase I dose-escalation study of the mTOR inhibitor sirolimus and the HDAC inhibitor vorinostat in patients with advanced malignancy. [PDF]
, 2016 Preclinical models suggest that histone deacetylase (HDAC) and mammalian target of rapamycin (mTOR) inhibitors have synergistic anticancer activity. We designed a phase I study to determine the safety, maximum tolerated dose (MTD), recommended phase II ...
Falchook, Gerald S. +17 more
core +2 more sources