Results 71 to 80 of about 2,934,766 (329)

Epigenetic and antitumor effects of platinum(IV)-octanoato conjugates [PDF]

open access: yes, 2017
We present the anticancer properties of cis, cis, trans-[Pt(IV)(NH3)2Cl2(OA)2] [Pt(IV)diOA] (OA = octanoato), Pt(IV) derivative of cisplatin containing two OA units appended to the axial positions of a six-coordinate Pt(IV) center.
Brabec, Viktor   +8 more
core   +1 more source

Class IIa HDACs forced degradation allows resensitization of oxaliplatin‐resistant FBXW7‐mutated colorectal cancer

open access: yesMolecular 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

Epigenetic Regulation of Matrix Metalloproteinase-1 and -3 Expression in Mycobacterium tuberculosis Infection. [PDF]

open access: yes, 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

ATF4‐mediated stress response as a therapeutic vulnerability in chordoma

open access: yesMolecular 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

Efficacy and safety of histone deacetylase inhibitors in peripheral T-cell lymphoma: a systematic review and meta-analysis on prospective clinical trials

open access: yesFrontiers in Oncology, 2023
BackgroundThe overall survival of peripheral T-cell lymphoma (PTCL) is dismal. Histone deacetylase (HDAC) inhibitors have exhibited promising treatment outcomes for PTCL patients. Therefore, this work aims to systematically evaluate the treatment outcome
Peipei Yang   +12 more
doaj   +1 more source

Disengaging the Engine: Histone Deacetylases 1 and 2‐Mediated Acetylation of Hexokinase‐2 Regulates Energy Metabolism in Microglia Following Intracerebral Hemorrhage

open access: yesAdvanced Science, EarlyView.
This study demonstrates that HDAC1/2 knockout in microglia alleviates neurological deficits, preserves white matter, and accelerates hematoma clearance after ICH. HDAC1/2 inhibition reduces HK2 acetylation, shifts metabolism from glycolysis to fatty acid oxidation, reduces inflammation, and enhances phagocytosis.
Zhiwen Jiang   +9 more
wiley   +1 more source

Histone deacetylase inhibitors (HDACIs): multitargeted anticancer agents

open access: yesBiologics: Targets & Therapy, 2013
Katherine Ververis,1 Alison Hiong,1 Tom C Karagiannis,1,* Paul V Licciardi2,*1Epigenomic Medicine, Alfred Medical Research and Education Precinct, 2Allergy and Immune Disorders, Murdoch Childrens Research Institute, Melbourne, VIC, Australia*These ...
Ververis K   +3 more
doaj  

EIF1AX Nucleolar Condensates Enhance Susceptibilities for the Management of Endometrial Cancer

open access: yesAdvanced Science, EarlyView.
This schematic illustrates the mechanism of a senolytic strategy in endometrial cancer. EIF1AX facilitates the incorporation of DDX21 into nucleolar condensates, an event that suppresses rDNA transcription and induces cellular senescence. The compound 2,5‐MeC exploits this pathway by promoting EIF1AX nucleolar translocation and condensate formation ...
Chengyu Lv   +8 more
wiley   +1 more source

Targeting phosphoinositide 3-kinase (PI3K) in head and neck squamous cell carcinoma (HNSCC). [PDF]

open access: yes, 2018
The landscape of head and neck squamous cell carcinoma (HNSCC) has been changing rapidly due to growing proportion of HPV-related disease and development of new therapeutic agents.
Jung, Kyungsuk   +2 more
core   +2 more sources

USP9X as a Candidate Mediator of Prenatal Aspirin‐Induced Ovarian Reserve Reduction in Offspring Mice

open access: yesAdvanced Science, EarlyView.
This study suggests that prenatal aspirin exposure is associated with reduced ovarian reserve in offspring, associated with HDAC1‐linked epigenetic downregulation of Usp9x as a candidate mechanism. These preclinical findings provide new insights into fetal‐origin ovarian disorders and contribute to the evidence base concerning aspirin's gestational ...
Yating Li   +11 more
wiley   +1 more source

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