Results 81 to 90 of about 152,498 (307)

Epigenetic potentiation of 5-fluorouracil by HDAC inhibitor quisinostat enhances antitumor effects in colorectal cancer

open access: yesCancer Cell International
Background Histone deacetylase (HDAC) inhibitors have emerged as promising epigenetic therapeutics in cancer treatment; however, their clinical efficacy in solid tumors remains limited.
Gizem Calibasi-Kocal   +4 more
doaj   +1 more source

Droxinostat, a Histone Deacetylase Inhibitor, Induces Apoptosis in Hepatocellular Carcinoma Cell Lines via Activation of the Mitochondrial Pathway and Downregulation of FLIP

open access: yesTranslational Oncology, 2016
Background: The current chemotherapeutic outcomes for hepatocellular carcinoma (HCC) are not encouraging, and long-term survival of this patient group remains poor.
Jing Liu   +9 more
doaj   +1 more source

A focus on the preclinical development and clinical status of the histone deacetylase inhibitor, romidepsin (depsipeptide, Istodax®)

open access: yesEpigenomics, 2012
Romidepsin (Istodax®, depsipeptide, FR901228, FK228, NSC 630176) is a cyclic peptide, broad-spectrum, potent histone deacetylase inhibitor, with activity mainly against class I histone deacetylase enzymes.
S. Harrison   +9 more
semanticscholar   +1 more source

Single‐Dose TACE‐Like Injection of Sustained‐Release Panobinostat/IL‐12 Polymeric Microparticles is Effective in Preclinical Liver Cancer Models

open access: yesAdvanced Science, EarlyView.
A novel PLGA/PBAE polymer microparticle platform revolutionizes intermediate‐stage liver cancer treatment by co‐delivering panobinostat and IL‐12 via a single TACE‐like injection. This sustained‐release system overcomes tumor immunosuppression, triggers robust innate and adaptive immune responses, and establishes tertiary lymphoid structures ...
Hongzhe Yu   +7 more
wiley   +1 more source

Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation

open access: yesAdvanced Science, EarlyView.
Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Kongjun Liu   +8 more
wiley   +1 more source

ZBTB18 Dysfunction Promotes Neuropathic Pain via CHD4‐based Epigenetic Disinhibition of CLIC1 Channels in Sensory Neurons

open access: yesAdvanced Science, EarlyView.
In this study, we identify a novel functional role of ZBTB18 in regulating trigeminal‐mediated neuropathic pain. Nerve injury reduces ZBTB18 in trigeminal ganglion neurons, impairing CHD4/NuRD recruitment and de‐repressing Clic1. Elevated CLIC1 enhances chloride channel activity and neuronal hyperexcitability, thereby driving pain.
Shoupeng Wang   +11 more
wiley   +1 more source

Impaired Chaperone‐Mediated Autophagy Accelerates Intervertebral Disc Degeneration by Inducing MIDN Accumulation to Target TSC2 for Proteasomal Degradation

open access: yesAdvanced Science, EarlyView.
This graphical abstract illustrates how chaperone‐mediated autophagy (CMA) regulates intervertebral disc degeneration (IDD). Under normal homeostasis (B), CMA degrades cytoplasmic Midnolin (MIDN) to maintain proteostasis. Under inflammatory stress (A), impaired CMA leads to cytoplasmic MIDN accumulation.
Xianglong Chen   +9 more
wiley   +1 more source

Histone deacetylase inhibition modulates cell fate decisions during myeloid differentiation

open access: yesHaematologica, 2010
Background The clinical use of chromatin-modulating drugs, such as histone deacetylase inhibitors, for the treatment of bone marrow failure and hematopoietic malignancies has increased dramatically over the last few years.
Marije Bartels   +4 more
doaj   +1 more source

Multi‐Technique Integration Identifies O‐GlcNAc Transferase in Fibroblast‐Like Synoviocytes as a Therapeutic Target for Rheumatoid Arthritis

open access: yesAdvanced Science, EarlyView.
AI‑guided single‑cell transcriptomics identifies OGT as a key regulator enriched in rheumatoid arthritis fibroblast‑like synoviocytes (RA‐FLSs). Inflammatory stimuli activate the OGT–SAP130 axis, which modulates the H3K27ac/H3K27me3 balance and epigenetically silences BTG2, promoting aggressive transformation of RA‑FLSs.
Duoli Xie   +14 more
wiley   +1 more source

Targeting the KAT7/H3K14ac/RAC2 Axis Mediates OXPHOS to Promote Stemness Maintenance and Malignancy in Glioblastoma

open access: yesAdvanced Science, EarlyView.
SOX2 upregulates KAT7 in glioma stem cells, where KAT7 deposits H3K14 acetylation at the RAC2 promoter to activate RAC2 transcription. RAC2‐GTP subsequently promotes PAK1/2/3 phosphorylation, increasing tricarboxylic acid cycle flux and mitochondrial respiration to support glioblastoma malignancy.
Jilong Liu   +13 more
wiley   +1 more source

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