Targeting HDAC3 Activity with RGFP966 Protects Against Retinal Ganglion Cell Nuclear Atrophy and Apoptosis After Optic Nerve Injury [PDF]
HDAC3 regulates nuclear atrophy as an early response to axonal injury in retinal ganglion cells (RGCs) following optic nerve crush (ONC). Since conditional knockout of Hdac3 prevents nuclear atrophy post ONC, HDAC3 selective inhibition with RGFP966 through localized and systemic dosing of RGFP966 is necessary for application to acute and chronic models
Heather M, Schmitt +2 more
openaire +2 more sources
Mechanisms of NF-κB p65 and strategies for therapeutic manipulation [PDF]
The transcription factor NF-κB is a critical regulator of immune and inflammatory responses. In mammals, the NF-κB/Rel family comprises five members: p50, p52, p65 (Rel-A), c-Rel, and Rel-B proteins, which form homo- or heterodimers and remain as an ...
Giridharan, Sivagami +1 more
core +1 more source
Destabilization of Fatty Acid Synthase by Acetylation Inhibits De Novo Lipogenesis and Tumor Cell Growth [PDF]
Fatty acid synthase (FASN) is the terminal enzyme in de novo lipogenesis and plays a key role in cell proliferation. Pharmacological inhibitors of FASN are being evaluated in clinical trials for treatment of cancer, obesity and other diseases.
Cheng, Zhou-Li +13 more
core +2 more sources
LMK235, a small molecule inhibitor of HDAC4/5, protects dopaminergic neurons against neurotoxin- and α-synuclein-induced degeneration in cellular models of Parkinson's disease [PDF]
Epigenetic modifications in neurodegenerative disease are under investigation for their roles in disease progression. Alterations in acetylation rates of certain Parkinson's disease (PD)-linked genes have been associated with the pathological progression
Collins, Louise M. +5 more
core +1 more source
Hsp90 chaperone facilitates E2F1/2-dependent gene transcription in human breast cancer cells
The 90 kDa heat shock protein, Hsp90, is involved in the conformational stabilization and functional maturation of diverse cancer-promoting proteins.
Akhil Kotwal +2 more
doaj +1 more source
Histone deacetylase 3-specific inhibitor RGFP966 attenuates oxidative stress and inflammation after traumatic brain injury by activating the Nrf2 pathway. [PDF]
Abstract Background Oxidative stress (OS) and inflammatory reactions play pivotal roles in secondary brain injury after traumatic brain injury (TBI). Histone deacetylase 3 (HDAC3) controls the acetylation of histones and non-histones, which has a significant impact on the central nervous system’s ...
Xu L +7 more
europepmc +3 more sources
MeCP2 Lactylation Protects against Ischemic Brain Injury by Transcriptionally Regulating Neuronal Apoptosis. [PDF]
MeCP2 lactylation protects against ischemic stroke by reducing brain infarct volume and improving neurological outcomes. Lactylation at K210/K249 exerts neuroprotective effects by repressing the transcription of apoptosis‐associated genes, including Pdcd4 and Pla2g6. HDAC3 and p300 serve as key regulatory enzymes for MeCP2 lactylation following stroke.
Sun M +13 more
europepmc +2 more sources
HDAC3 is essential for Human Leukemic Cell Growth and the Expression of β-catenin, MYC, and WT1 [PDF]
Therapy of acute myeloid leukemia (AML) is unsatisfactory. Histone deacetylase inhibitors (HDACi) are active against leukemic cells in vitro and in vivo.
Beyer, M. +3 more
core +1 more source
HDAC3 has been shown to regulate inflammation. However, the role of HDAC3 in primary microglia is largely unknown. RGFP966 is a newly discovered selective HDAC3 inhibitor. In this study, we used protein mass spectrometry to analyze protein alterations in
Mingxu Xia +6 more
doaj +1 more source
Osteoarthritis (OA) is a disease characterized by non-bacterial inflammation. Histone deacetylase 3 (HDAC3) is a crucial positive regulator in the inflammation that leads to the development of non-OA inflammatory disease. However, the precise involvement
He Zhang +7 more
doaj +1 more source

