Search Results - "Holson, Edward"
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Exercise promotes the expression of brain derived neurotrophic factor (BDNF) through the action of the ketone body β-hydroxybutyrate
Published in eLife (02-06-2016)“…Exercise induces beneficial responses in the brain, which is accompanied by an increase in BDNF, a trophic factor associated with cognitive improvement and the…”
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Lactate is an antidepressant that mediates resilience to stress by modulating the hippocampal levels and activity of histone deacetylases
Published in Neuropsychopharmacology (New York, N.Y.) (01-05-2019)“…Chronic stress promotes depression in some individuals, but has no effect in others. Susceptible individuals exhibit social avoidance and anxious behavior and…”
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Selective HDAC inhibition for the disruption of latent HIV-1 infection
Published in PloS one (19-08-2014)“…Selective histone deacetylase (HDAC) inhibitors have emerged as a potential anti-latency therapy for persistent human immunodeficiency virus type 1 (HIV-1)…”
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EHMT1 and EHMT2 inhibition induces fetal hemoglobin expression
Published in Blood (15-10-2015)“…Fetal hemoglobin (HbF, α2γ2) induction is a well-validated strategy for sickle cell disease (SCD) treatment. Using a small-molecule screen, we found that…”
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Hdac3 Is Essential for the Maintenance of Chromatin Structure and Genome Stability
Published in Cancer cell (16-11-2010)“…Hdac3 is essential for efficient DNA replication and DNA damage control. Deletion of Hdac3 impaired DNA repair and greatly reduced chromatin compaction and…”
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Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia
Published in Science translational medicine (07-03-2018)“…Glycogen synthase kinase 3 (GSK3), a key regulatory kinase in the wingless-type MMTV integration site family (WNT) pathway, is a therapeutic target of interest…”
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Epigenetic Priming of Memory Updating during Reconsolidation to Attenuate Remote Fear Memories
Published in Cell (16-01-2014)“…Traumatic events generate some of the most enduring forms of memories. Despite the elevated lifetime prevalence of anxiety disorders, effective strategies to…”
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In Vivo Imaging of Histone Deacetylases (HDACs) in the Central Nervous System and Major Peripheral Organs
Published in Journal of medicinal chemistry (09-10-2014)“…Epigenetic enzymes are now targeted to treat the underlying gene expression dysregulation that contribute to disease pathogenesis. Histone deacetylases (HDACs)…”
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Isoform-selective inhibitor of histone deacetylase 3 (HDAC3) limits pancreatic islet infiltration and protects female nonobese diabetic mice from diabetes
Published in The Journal of biological chemistry (27-10-2017)“…Preservation of insulin-secreting β-cells is an important goal for therapies aimed at restoring normoglycemia in patients with diabetes. One approach, the…”
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Signal-dependent repression of DUSP5 by class I HDACs controls nuclear ERK activity and cardiomyocyte hypertrophy
Published in Proceedings of the National Academy of Sciences - PNAS (11-06-2013)“…Cardiac hypertrophy is a strong predictor of morbidity and mortality in patients with heart failure. Small molecule histone deacetylase (HDAC) inhibitors have…”
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Histone deacetylases 1 and 2 inhibition suppresses cytokine production and osteoclast bone resorption in vitro
Published in Journal of cellular biochemistry (01-01-2020)“…The regulation of epigenetic factors is an emerging therapeutic target of immune function in a variety of osteolytic pathologies. Histone deacetylases (HDAC)…”
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Small Molecule Inhibitors of Zinc-dependent Histone Deacetylases
Published in Neurotherapeutics (01-10-2013)“…Lysine acetylation is an ancient, evolutionarily conserved, reversible post-translational modification. A multitude of diverse cellular functions are regulated…”
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A selective HDAC 1/2 inhibitor modulates chromatin and gene expression in brain and alters mouse behavior in two mood-related tests
Published in PloS one (14-08-2013)“…Psychiatric diseases, including schizophrenia, bipolar disorder and major depression, are projected to lead global disease burden within the next decade…”
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14
Selective inhibition of glycogen synthase kinase 3α corrects pathophysiology in a mouse model of fragile X syndrome
Published in Science translational medicine (20-05-2020)“…Fragile X syndrome is caused by gene silencing and loss of the encoded fragile X mental retardation protein (FMRP), which binds to mRNA and regulates…”
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Potent and Selective Inhibition of Histone Deacetylase 6 (HDAC6) Does Not Require a Surface-Binding Motif
Published in Journal of medicinal chemistry (28-02-2013)“…Hydroxamic acids were designed, synthesized, and evaluated for their ability to selectively inhibit human histone deacetylase 6 (HDAC6). Several inhibitors,…”
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Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries
Published in Journal of organic chemistry (07-09-2012)“…The synthesis and diversification of a densely functionalized azetidine ring system to gain access to a wide variety of fused, bridged, and spirocyclic ring…”
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HDAC2 targeting stabilizes the CoREST complex in renal tubular cells and protects against renal ischemia/reperfusion injury
Published in Scientific reports (27-04-2021)“…Histone/protein deacetylases (HDAC) 1 and 2 are typically viewed as structurally and functionally similar enzymes present within various co-regulatory…”
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Discovery of the First Histone Deacetylase 6/8 Dual Inhibitors
Published in Journal of medicinal chemistry (13-06-2013)“…We disclose the first small molecule histone deacetylase (HDAC) inhibitor (3, BRD73954) capable of potently and selectively inhibiting both HDAC6 and HDAC8…”
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Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors
Published in Bioorganic & medicinal chemistry (15-09-2016)“…[Display omitted] The structure–activity and structure–kinetic relationships of a series of novel and selective ortho-aminoanilide inhibitors of histone…”
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Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging
Published in Angewandte Chemie (International ed.) (08-08-2016)“…Glycogen synthase kinase‐3 (GSK‐3) regulates multiple cellular processes in diabetes, oncology, and neurology…”
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