Results 81 to 90 of about 776,666 (283)

Unraveling 4‐Phenylbutyrate's Therapeutic Role in SLC6A1 Disorders: Pharmacochaperoning Over HDAC Inhibition

open access: yesAnnals of Clinical and Translational Neurology, EarlyView.
ABSTRACT Objective Variants in SLC6A1, encoding the GABA transporter 1 (GAT‐1), cause epilepsy, autism spectrum disorder, and developmental delay via loss of GABA uptake, impaired trafficking, and ER retention. We previously found that 4‐Phenylbutyrate (PBA), an FDA‐approved drug, restores GABA uptake and reduces seizures in SLC6A1‐related disorders ...
Melissa B. DeLeeuw   +5 more
wiley   +1 more source

Phosphorylation‐Facilitated CKB Lactylation At K11 By GCN5 Enhances Creatine Kinase Activity and Mitigates Neuronal Damage After Cerebral Ischemia‐Reperfusion

open access: yesAdvanced Science, EarlyView.
This study uncovers hierarchical coordination between K11 lactylation and S199 phosphorylation of CKB in cerebral ischemia‐reperfusion injury. Such dual modifications potentiate CKB enzymatic function, remodel energy metabolism, alleviate oxidative stress and neuronal damage, and represent a viable therapeutic target for stroke treatment.
Chao Duan   +17 more
wiley   +1 more source

Comparative effects of histone deacetylases inhibitors and resveratrol on Trypanosoma cruzi replication, differentiation, infectivity and gene expression

open access: yesInternational Journal for Parasitology: Drugs and Drug Resistance, 2017
Histone post-translational modification, mediated by histone acetyltransferases and deacetylases, is one of the most studied factors affecting gene expression.
Vanina A. Campo
doaj   +1 more source

The Broad Spectrum HDAC Inhibitor PCI-24781 Induces Caspase- and ROS-Dependent Apoptosis and is Synergistic with Bortezomib in Lymphoma [PDF]

open access: yes, 2008
We investigated the cytotoxicity and biology of the novel broad-spectrum hydroxamic acid-based histone deacetylase inhibitor (HDACi), PCI-24781. PCI-24781 was studied alone and combined with bortezomib in Hodgkin lymphoma (L428) and non-Hodgkin's ...
Kevin David   +9 more
core  

BAP31 Drives Cartilage Calcification through Disruption of Autophagosome–Lysosome Fusion in Osteoarthritis

open access: yesAdvanced Science, EarlyView.
Mechanical stress activates BAP31 in chondrocytes. BAP31 competes with ATG14 for binding to STX17, disrupting the STX17–ATG14 complex required for autophagosome–lysosome fusion. The resultant autophagic flux blockade drives the generation of autophagy‐derived exosomes, which mediate pathological cartilage calcification in OA. Chondrocyte‐targeted BAP31
Zhi‐hua Xu   +13 more
wiley   +1 more source

HISTONE DEACETYLASE INHIBITORS FOR CANCER TREATMENT DRUG DEVELOPMENT IN CONTEMPORARY ONCOLOGY

open access: yes, 2014
inhibitors as novel anticancer therapeutics D.R. Walkinshaw MSc * and X.J. Yang PhD* Histone deacetylase inhibitors represent a promising new class of compounds for the treatment of cancer.
Key Words, Histone Deacetylase
core  

Visible-Light-Controlled Histone Deacetylase Inhibitors for Targeted Cancer Therapy

open access: yes, 2023
The lack of selectivity of anticancer drugs limits current chemotherapy. Light-activatable drugs, whose activity can be precisely controlled with external light, could provide a more localized action of the drugs in the tumor, thus decreasing side ...
Josa-Culleré, Laia, Llebaria, Amadeu
core   +1 more source

Modulation of Lung Adenocarcinoma by Phosphorylated FOXN3‐Mediated Transcriptional Inactivation of p53

open access: yesAdvanced Science, EarlyView.
In non‐tumorous lung tissues, FOXN3 promotes the transcriptional activation of p53 by facilitating its recruitment to target promoters, thereby suppressing lung tumorigenesis through activation of the p53 signaling pathway. Conversely, in lung adenocarcinoma tissues, hyperphosphorylated FOXN3 dissociates from the promoters of p53‐responsive genes and ...
Jinjin Yu   +16 more
wiley   +1 more source

The CBX7 protein, whose expression is decreased in human carcinomas, positively regulates E-cadherin expression by interacting with the HDAC2 protein. [PDF]

open access: yes, 2009
CBX7, chromobox homolog 7, is a chromobox family protein encoding a novel Polycomb protein, component of the Polycomb repressive complex 1 (PRC1). The Polycomb group (PcG) proteins are epigenetic transcriptional repressors involved in the control of ...
Bianco, Mimma
core   +1 more source

Histone H3K18 Lactylation Promotes the Malignant Progression of Wilms Tumor via a PSRC1/AKT/HIF‐1α Positive Feedback Loop

open access: yesAdvanced Science, EarlyView.
In nephroblastoma, aberrant glycolysis drives lactate accumulation, which elevates histone H3K18 lactylation via p300. Lactylation of the PSRC1 promoter activates its transcription. PSRC1 competitively binds AKT, relieving PTEN‐mediated inhibition and triggering AKT/mTOR/HIF‐1α signaling.
Yanping Wang   +6 more
wiley   +1 more source

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