Histone Deacetylase Inhibitors Research

RNA-sequencing of butyrate-treated human lymphoblastoid cell lines shows dysregulated genes of multiple disease-related pathways

This study uses RNA-seq to analyze the transcriptomic effects of butyrate on human lymphoblastoid cell lines, identifying dysregulated genes in multiple disease-related pathways.

Epigenetic regulation of alveolar macrophage homeostasis by histone deacetylase 1 and 2

This study shows HDAC1 and HDAC2 are essential for alveolar macrophage homeostasis by suppressing Bim expression and co-regulating differentiation with LSD1.

Binding of a Macrocyclic Nonapeptide Inhibitor to Histone Deacetylase 6

The paper reports the crystal structure of HDAC6 CD2 complexed with a macrocyclic nonapeptide inhibitor, revealing key interactions that contribute to its inhibitory potency.

Transient histone deacetylase inhibition reveals cell type invariant and specific effects of chromatin decondensation on irradiation response

This paper shows that transient HDAC inhibition increases DNA damage and reduces cell viability in both cancerous and healthy breast cells after high-dose radiation, but effects vary with radiation dose and cell type.

Identification of novel HDAC11 inhibitors: In silico & in vitro studies

This study identifies novel HDAC11 inhibitors through in silico and in vitro approaches, showing they reduce breast cancer cell viability and induce apoptosis.

HDAC4/5 regulate epidermal barrier function by modulating the epigenetic landscape of human keratinocytes

This study shows HDAC4/5 regulate epidermal barrier function by modulating histone acetylation in keratinocytes, affecting proliferation and differentiation.

MeFluHyA: a novel fluorescent screening tool for high-throughput identification of HDAC6-selective inhibitors

The paper introduces MeFluHyA, a fluorescent probe for identifying HDAC6-selective inhibitors through cell imaging and competitive binding assays.

HDAC Inhibition Sensitizes Pancreatic Tumors to DNA Damage by Global Redistribution of the Transcriptional Machinery

This study shows HDAC inhibition reduces DDR gene expression in pancreatic tumors by altering transcriptional machinery distribution, enhancing sensitivity to DNA damage, and introduces a nanoparticle delivery system to reduce toxicity.

Quinazolinone and Phthalazinone Inhibitors of the HDAC6/Ubiquitin Protein-Protein Interaction

The paper identifies and optimizes quinazolinone and phthalazinone inhibitors targeting the HDAC6 ZnF-UBD/ubiquitin interaction, using computational and experimental methods to improve their physicochemical properties and predict binding affinity.

Transcriptomic response to histone deacetylase inhibitors in cultured feline cells

This study examines the transcriptomic effects of HDAC inhibitors on feline cells, finding organ-specific responses and differential gene expression patterns compared to human cells.

A Highly Selective, Cell-Permeable Fluorescent Probe for Imaging Histone Deacetylase 6 in Live Cells

The paper develops a fluorescent probe for visualizing HDAC6 in live cells, showing high selectivity and utility in imaging its interactions with microtubules and stress granules.

HDAC6 and SSAT2 orchestrate acetyllysine metabolism and protein homeostasis

The paper identifies HDAC6 and SSAT2 as enzymes regulating acetyllysine metabolism and protein homeostasis through opposing deacetylation and acetylation reactions.

Hierarchical small molecule inhibition of MYST acetyltransferases

This paper evaluates the potency and selectivity of MYST KAT inhibitors using chemoproteomic profiling and identifies new complex members, highlighting dose-dependent inhibition patterns and potential therapeutic applications.

HDAC inhibition unlocks tumor plasticity and enhances immunotherapy response in Myc- Driven Small Cell Lung Cancer

This study shows that HDAC inhibition with entinostat enhances immunotherapy response in SCLC by reprogramming tumor immunology and neuroendocrine status.

Neuronal HDAC9: A key regulator of cognitive and synaptic aging, rescuing Alzheimer's disease-related phenotypes

This study identifies HDAC9 as a critical regulator of cognitive and synaptic aging, showing its protective role in Alzheimer's disease.

Epigenetic remodeling via HDAC6 inhibition amplifies anti-tumoral immune responses in myeloid leukemia cells

This study shows HDAC6 inhibition enhances anti-tumoral immune responses and chemosensitivity in myeloid leukemia cells by upregulating RNase T2 and improving chromatin accessibility.

Enhanced efficacy of a specific HDAC3 inhibitor in combination with 5-Azacitidine against diffuse large B-cell lymphoma

This study shows that combining a HDAC3 inhibitor with 5-Azacitidine enhances anti-tumor effects against DLBCL in vitro and in vivo, with reduced toxicity compared to single agents.

Sodium valproate induces chromatin remodeling in U-251MG glioblastoma cells

This study shows that sodium valproate induces chromatin remodeling in U-251MG glioblastoma cells through histone modifications rather than DNA demethylation.

Phytic Acid (InsP6) Activates HDAC3 Epigenetic Axis to Maintain Intestinal Barrier Function

The paper shows that phytic acid activates the HDAC3 epigenetic axis to maintain intestinal barrier function, with therapeutic potential in inflammatory bowel disease.

Defining the heterogeneous molecular landscape of lung cancer cell responses to epigenetic inhibition

The paper profiles molecular responses to HDAC inhibitors in diverse cell lines, revealing heterogeneous protein remodeling and cell-type specific effects.

Selective class IIa HDAC inhibition reverses diastolic dysfunction in cardiometabolic HFpEF

This study shows that selective class IIa HDAC inhibition improves diastolic dysfunction in HFpEF without adverse effects.

The Deacetylases HDAC1 and HDAC2 Safeguard BCR-ABL-positive Cells from Replication Stress-Induced Apoptosis via the Nuclear to Mitochondrial p73-NOXA Axis

This study shows HDAC1 and HDAC2 protect BCR-ABL-positive CML cells from replication stress-induced apoptosis via the p73-NOXA axis.

Somatic Hdac4-902fs mutations lead to loss of HDAC4 function through nonsense-mediated mRNA degradation

This study shows that somatic HDAC4-902fs mutations cause loss of HDAC4 function via nonsense-mediated mRNA decay, leading to premature ossification and early death in mice.

Combined HDAC and eIF4A inhibition: A novel epigenetic therapy for pancreatic adenocarcinoma

This paper shows that combining HDAC and eIF4A inhibitors effectively treats pancreatic cancer by inducing epigenetic reprogramming and metabolic stress in preclinical models.

N-terminal oligomerization drives HDAC4 nuclear condensation and neurodevelopmental dysfunction in Drosophila

This study shows that HDAC4 nuclear condensation, driven by oligomerization and stabilized by MEF2, causes neurodevelopmental defects in Drosophila, suggesting therapeutic targets for related diseases.

Mutations on the surface of HDAC1 reveal molecular determinants of specific complex assembly and their requirement for gene regulation

The paper identifies molecular determinants of HDAC1 complex assembly through mutations, showing that specific residues are critical for complex binding and gene regulation.

PRECLINICAL DEVELOPMENT OF A ROMIDEPSIN NANOPARTICLE DEMONSTRATES SUPERIOR TOLERABILITY AND EFFICACY IN MODELS OF HUMAN T-CELL LYMPHOMA AND LARGE GRANULAR LYMPHOCYTE LEUKEMIA

Rapid degradation of 6 class I HDAC complexes reveals minimal functional overlap between complexes

This study identifies primary targets of individual class I HDAC complexes and shows that their rapid degradation leads to gene regulation with significant specificity and antagonistic effects.

Chemical perturbations impacting histone acetylation governcolorectal cancer differentiation

The paper identifies HDAC1/2 inhibition as a method to promote colorectal cancer differentiation through H3K27ac gains, which can be reversed by blocking EP300.

Sorbate Induces Lysine Sorbylation Through Non-Canonical Activities of Class I HDACs to Regulate the Expression of Inflammation Genes

This study shows sorbate induces lysine sorbylation via Class I HDACs, altering inflammation gene expression without affecting histone acetylation.