HDAC inhibitors increase NRF2-signaling in tumour cells and blunt the efficacy of co-adminstered cytotoxic agents [PDF]
, 2014 The NRF2 signalling cascade provides a primary response against electrophilic chemicals and oxidative stress. The activation of NRF2-signaling is anticipated to have adverse clinical consequences; NRF2 is activated in a number of cancers and ...
Campbell, Kathryn H. +5 more
core +7 more sources
Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer [PDF]
, 2019 Pancreatic ductal adenocarcinoma (PDAC) is an aggressive, incurable cancer with a 20% 1 year survival rate. While standard-of-care therapy can prolong life in a small fraction of cases, PDAC is inherently resistant to current treatments, and novel ...
Adile, Ashley A. +19 more
core +3 more sources
Archives of Pharmaceutical Sciences Ain Shams University, 2018 Despite the increased success rates of histone deacetylases inhibitors (HDACi) as potent anticancer agents, many metabolic obstacles face the hydroxamic acid-based HDAC inhibitors, which inspired us to develop non-hydroxamate HDAC inhibitors.
Heba M. Hesham +2 more
doaj +1 more source
Viruses, 2023 Porcine epidemic diarrhea virus (PEDV) is an alpha-coronavirus causing acute diarrhea and high mortality in neonatal suckling piglets, resulting in huge economic losses for the global swine industry.
Ying Yang +5 more
doaj +1 more source
Trichostatin A induces 5-lipoxygenase promoter activity and mRNA expression via inhibition of histone deacetylase 2 and 3 [PDF]
, 2012 The 5-lipoxygenase (5-LO) is the key enzyme in the formation of leukotrienes. We have previously shown that the histone deacetylase (HDAC) inhibitor trichostatin A (TSA) activates 5-LO transcription via recruitment of Sp1, Sp3 and RNA polymerase II to ...
Grez, Manuel +6 more
core +1 more source
Histone deacetylase 2-mediated deacetylation of the Ribonuclease 1 promoter in inflamed human endothelial cells [PDF]
, 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
Rational Combinations Using HDAC Inhibitors [PDF]
Clinical Cancer Research, 2009 Abstract In addition to well-characterized genetic abnormalities that lead to cancer onset and progression, it is now recognized that alterations to the epigenome may also play a significant role in oncogenesis. As a result, epigenetic-modulating agents such as histone deacetylase inhibitors (HDACi) have attracted enormous attention as ...
Bots, Michael, Johnstone, Ricky W.
openaire +2 more sources
Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents
Molecules, 2015 Histone dacetylases (HDACs) are a group of enzymes that remove acetyl groups from histones and regulate expression of tumor suppressor genes. They are implicated in many human diseases, especially cancer, making them a promising therapeutic target for ...
Madhusoodanan Mottamal +3 more
doaj +1 more source
HDAC-mediated control of ERK- and PI3K-dependent TGF-β-induced extracellular matrix-regulating genes [PDF]
, 2010 Histone deacetylases (HDACs) regulate the acetylation of histones in the control of gene expression. Many non-histone proteins are also targeted for acetylation, including TGF-ß signalling pathway components such as Smad2, Smad3 and Smad7. Our studies in
Andrew D. Rowan +54 more
core +1 more source
Axitinib and HDAC Inhibitors Interact to Kill Sarcoma Cells
Frontiers in Oncology, 2021 We have extended our analyses of HDAC inhibitor biology in sarcoma. The multi-kinase inhibitor axitinib interacted with multiple HDAC inhibitors to kill sarcoma cells.
Jane L. Roberts +3 more
doaj +1 more source