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Structure of a SIN3–HDAC complex from budding yeast
SIN3–HDAC (histone deacetylases) complexes have important roles in facilitating local histone deacetylation to regulate chromatin accessibility and...
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Development of a Cellular Model Mimicking Specific HDAC Inhibitors
Class I histone deacetylases (HDACs) are important regulators of cellular functions in health and disease. HDAC1, HDAC2, HDAC3, and HDAC8 are...
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Novel dual inhibitors of PARP and HDAC induce intratumoral STING-mediated antitumor immunity in triple-negative breast cancer
PARP inhibitors and HDAC inhibitors have been approved for the clinical treatment of malignancies, but acquired resistance of or limited effects on...
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Dual inhibitors of DNMT and HDAC induce viral mimicry to induce antitumour immunity in breast cancer
The existing conventional treatments for breast cancer, including immune checkpoint blockade, exhibit limited effects in some cancers, particularly...
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Evaluation of Small-Molecule HDAC Inhibitors Through In Vitro and In Cellulo Approaches
The aberrant activity of histone deacetylases (HDACs) across a broad range of cancers and other disease indications has led to the development of...
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NUP98 and RAE1 sustain progenitor function through HDAC-dependent chromatin targeting to escape from nucleolar localization
Self-renewing somatic tissues rely on progenitors to support the continuous tissue regeneration. The gene regulatory network maintaining progenitor...
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The HDAC inhibitor zabadinostat is a systemic regulator of adaptive immunity
Protein acetylation plays a key role in regulating cellular processes and is subject to aberrant control in diverse pathologies. Although histone...
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Complete remission of diabetes with a transient HDAC inhibitor and insulin in streptozotocin mice
Despite the growing epidemic worldwide, diabetes is an incurable disease. We have been focusing on why diabetes manifests refractoriness to any...
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Assessment of HDAC Inhibitor-Induced Endoplasmic Reticulum (ER) Stress
The endoplasmic reticulum (ER) is a multifunctional cell organelle which is important for the folding and processing of proteins. Different...
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The impact of selective HDAC inhibitors on the transcriptome of early mouse embryos
BackgroundHistone acetylation, which is regulated by histone acetyltransferases (HATs) and histone deacetylases (HDACs), plays a crucial role in the...
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Defined Human Leukemic CD34+ Liquid Cultures to Study HDAC/Transcriptional Repressor Complexes
Defined human primary cell model systems with growth dependence on oncogenes are highly requested to investigate tumor pathogenesis and to validate...
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HDAC/HAT Function Assessment and Inhibitor Development Methods and Protocols
This fully updated edition provides a series of methods for how best to assess functions of histone deacetylases and acetyltransferases. The...
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Diaryl Pyrazoline, 1,3,4-Oxadizole, and 1,2,4-Triazole Pharmacophore Hybridization: Design, Synthesis, HDAC Inhibition, and Caspase 3/7 Activation Studies
AbstractObjective: The study aimed to employ the pharmacophore hybridization technique for the synthesis of novel anticancer compounds by combining...
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Evaluation of Antitumor and On-Target Activity of HDAC Inhibitors with the Zebrafish Embryo Xenograft Model
Reliable preclinical drug testing models for cancer research are urgently needed with zebrafish embryo models emerging as a powerful vertebrate model...
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Class I HDAC overexpression promotes temozolomide resistance in glioma cells by regulating RAD18 expression
Overexpression of histone deacetylases (HDACs) in cancer commonly causes resistance to genotoxic-based therapies. Here, we report on the novel...
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Acetate Abates Arsenic-Induced Male Reproductive Toxicity by Suppressing HDAC and Uric Acid–Driven Oxido-inflammatory NFkB/iNOS/NO Response in Rats
Arsenic is associated with male reproductive toxicity through histone deacetylation and oxido-inflammatory injury. Notwithstanding, short-chain fatty...
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CRISPR Activation/Interference Screen to Identify Genetic Networks in HDAC-Inhibitor-Resistant Cells
Epigenetic alterations have been identified in various tumor types. In part, these alterations are mediated via increased histone deacetylase...
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Anti-tumor effects of dual PI3K-HDAC inhibitor CUDC-907 on activation of ROS-IRE1α-JNK-mediated cytotoxic autophagy in esophageal cancer
BackgroundPI3K-Akt pathway activation and the expression of histone deacetylases (HDACs) are highly increased in esophageal cancer, suggesting that...
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HDAC inhibitor chidamide overcomes drug resistance in chronic myeloid leukemia with the T315i mutation through the Akt–autophagy pathway
Currently, therapy for Chronic Myeloid Leukemia (CML) patients with the T315I mutation is a major challenge in clinical practice due to its high...
