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
HDACs and HDAC inhibitors in colon cancer [PDF]
Epigenetics, 2008 The histone deacetylase (HDAC) family of transcriptional co-repressors have emerged as important regulators of colon cell maturation and transformation. Pharmacological inhibitors of class I and II HDAC activity (HDACi) are potent inducers of growth arrest, differentiation and apoptosis of colon cancer cells in vitro and in vivo, implicating a role for
openaire +2 more sources
Dual Inhibitors Targeting DNA and Histone Deacetylases
Pharmaceutical Fronts, 2020 Histone deacetylases (HDACs) regulate the acetylation status of histones and structural status of chromatin. The chromatin structure becomes relaxed after inhibition of HDAC, leading to DNA exposed to DNA disrupting agents, and eventually causing DNA ...
Chen Chen +3 more
doaj +1 more source
Identification of Novel 4-Oxo-4H-chromen-Hydroxamic Acid Derivative Targeting Selected HDAC Isoforms
Archives of Pharmaceutical Sciences Ain Shams University, 2023 Histone deacetylase inhibitors (HDACIs) represent a well-known class of compounds that exhibit potential therapeutic efficacy in a variety of diseases, particularly cancer and neurodegenerative disorders.
Rosaline Ashraf +3 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
Pathogens, 2020 Epigenetic reprogramming in macrophages is termed trained innate immunity, which regulates immune tolerance and limits tissue damage during infection. Neisseria gonorrhoeae is a strict human pathogen that causes the sexually transmitted infection termed ...
Susu M. Zughaier +2 more
doaj +1 more source
Epigenetic Regulation of Matrix Metalloproteinase-1 and -3 Expression in Mycobacterium tuberculosis Infection. [PDF]
, 2017 In pulmonary tuberculosis (TB), the inflammatory immune response against Mycobacterium tuberculosis (Mtb) is associated with tissue destruction and cavitation, which drives disease transmission, chronic lung disease, and mortality.
Alland +52 more
core +2 more sources
HDAC 1 and 6 modulate cell invasion and migration in clear cell renal cell carcinoma [PDF]
, 2016 Indexación: Web of ScienceBackground: Class I histone deacetylases (HDACs) have been reported to be overexpressed in clear cell renal cell carcinoma (ccRCC), whereas the expression of class II HDACs is unknown.
Attwood, Kris +14 more
core +2 more sources
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