Dec 29, 2024 · HDIs that inhibit all classical zinc-dependent HDACs are known as pan-HDIs. Pan-HDI Trichostatin A (TSA) attenuates cardiac hypertrophy and preserves contractile functions in transverse aortic constriction (TAC) or angiotensin II-induced hypertrophy animal models 1–3.

Histone deacetylases (HDAC) catalyze the removal of acetylation modifications on histones and non-histone proteins, which regulates gene expression and other cellular processes. HDAC inhibitors (HDACi), approved anti-cancer agents, emerge as a …

Apr 18, 2023 · HDAC3 is critical for early embryonic growth, development of vital organs, and numerous metabolic processes. HDAC3 is closely correlated to mitochondria function and metabolism, ROS-produced...

Jul 23, 2021 · Histone deacetylase 3 (HDAC3) plays a crucial role in chromatin remodeling, which, in turn, regulates gene transcription. Hence, HDAC3 has been implicated in various diseases, including...

HDAC3 is a Class I member of the histone deacetylase superfamily (comprising four classes based on function and DNA sequence homology) that is recruited to enhancers to modulate both the epigenome and nearby gene expression.

In this review, we describe that histone deacetylase-3 (HDAC3) is a particularly crucial regulator of both neurodevelopment and neurodegeneration. In addition, HDAC3 regulates memory formation, synaptic plasticity, and the cognitive impairment associated with normal aging.

Feb 9, 2017 · Histone deacetylase 3 (HDAC3) is essential in the maintenance of endothelial homeostasis. Our previous study indicates that mouse HDAC3 mRNA can undergo unconventional splicing, and that the HDAC3α spliced isoform promotes the EndMT process in human aortic endothelial cells (HAECs).

Aug 11, 2023 · Here, we report a novel HDAC3/8 dual degrader YX968 that induces highly potent, rapid, and selective degradation of both HDAC3/8 without triggering pan-HDAC inhibitory effects. Unbiased quantitative proteomic experiments confirmed its high selectivity.

We discovered XZ9002, a first-in-class HDAC3-specific PROTAC that potently degraded HDAC3. Importantly, XZ9002 is more effective to inhibit cancer cell proliferation than its proteolysis-inactive counterpart, suggesting HDAC3 degradation is a novel and promising anticancer approach.

Dec 26, 2013 · HDAC3 depletion in mouse liver upregulates lipogenic genes and results in severe hepatosteatosis. Here we show that pharmacologic HDAC inhibition in primary hepatocytes causes histone hyperacetylation but does not upregulate expression of HDAC3 target genes.