Search Results - "Leus, Niek G. J."
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HDAC1-3 inhibitor MS-275 enhances IL10 expression in RAW264.7 macrophages and reduces cigarette smoke-induced airway inflammation in mice
Published in Scientific reports (27-03-2017)“…Chronic obstructive pulmonary disease (COPD) constitutes a major health burden. Studying underlying molecular mechanisms could lead to new therapeutic targets…”
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Anti-VCAM‑1 and Anti-E-selectin SAINT-O-Somes for Selective Delivery of siRNA into Inflammation-Activated Primary Endothelial Cells
Published in Molecular pharmaceutics (05-08-2013)“…Activated endothelial cells play a pivotal role in the pathology of inflammatory diseases and present a rational target for therapeutic intervention by…”
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Anti-VCAM-1 SAINT-O-Somes enable endothelial-specific delivery of siRNA and downregulation of inflammatory genes in activated endothelium in vivo
Published in Journal of controlled release (28-02-2014)“…The pivotal role of endothelial cells in the pathology of inflammatory diseases raised interest in the development of short interfering RNA (siRNA) delivery…”
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VCAM-1 specific PEGylated SAINT-based lipoplexes deliver siRNA to activated endothelium in vivo but do not attenuate target gene expression
Published in International journal of pharmaceutics (20-07-2014)“…[Display omitted] In recent years much research in RNA nanotechnology has been directed to develop an efficient and clinically suitable delivery system for…”
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Targeted siRNA delivery to diseased microvascular endothelial cells—Cellular and molecular concepts
Published in IUBMB life (01-08-2011)“…Increased insight in the role of endothelial cells in the pathophysiology of cancer, inflammatory and cardiovascular diseases, has drawn great interest in…”
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Reassessment of the Role of Mut S Homolog 5 in Ig Class Switch Recombination Shows Lack of Involvement in cis- and trans-Switching
Published in The Journal of immunology (1950) (15-12-2008)“…When B cells are activated after immunization or infection, they exchange the gene encoding the Ig H chain C region by class switch recombination (CSR). CSR…”
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7
HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity
Published in Biochemical pharmacology (15-05-2016)“…[Display omitted] The increasing number of patients suffering from chronic obstructive pulmonary disease (COPD) represents a major and increasing health…”
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Histone deacetylase 3 (HDAC 3) as emerging drug target in NF-κB-mediated inflammation
Published in Current opinion in chemical biology (01-08-2016)“…[Display omitted] •HDAC 3 plays a key role in NF-κB-mediated signaling.•HDAC inhibitors demonstrate promising anti-inflammatory effects.•Selective HDAC 3…”
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Rational Development of a Potent 15-Lipoxygenase‑1 Inhibitor with in Vitro and ex Vivo Anti-inflammatory Properties
Published in Journal of medicinal chemistry (08-10-2015)“…Human 15-lipoxygenase-1 (h-15-LOX-1) is a mammalian lipoxygenase and plays an important role in several inflammatory lung diseases such as asthma, COPD, and…”
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The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases
Published in Biochemical pharmacology (15-02-2016)“…[Display omitted] Lysine acetylations are reversible posttranslational modifications of histone and non-histone proteins that play important regulatory roles…”
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Design of a novel thiophene inhibitor of 15-lipoxygenase-1 with both anti-inflammatory and neuroprotective properties
Published in European journal of medicinal chemistry (21-10-2016)“…The enzyme 15-lipoxygenase-1 (15-LOX-1) plays a dual role in diseases with an inflammatory component. On one hand 15-LOX-1 plays a role in pro-inflammatory…”
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Activity-Based Probes for 15-Lipoxygenase-1
Published in Angewandte Chemie (26-09-2016)“…Human 15‐lipoxygenase‐1 (15‐LOX‐1) plays an important role in several inflammatory lung diseases, such as asthma, COPD, and chronic bronchitis, as well as…”
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A 6-alkylsalicylate histone acetyltransferase inhibitor inhibits histone acetylation and pro-inflammatory gene expression in murine precision-cut lung slices
Published in Pulmonary pharmacology & therapeutics (01-06-2017)“…Abstract Lysine acetylations are post-translational modifications of cellular proteins, that are crucial in the regulation of many cellular processes. Lysine…”
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14
Activity-Based Probes for 15-Lipoxygenase-1
Published in Angewandte Chemie International Edition (26-09-2016)“…Human 15‐lipoxygenase‐1 (15‐LOX‐1) plays an important role in several inflammatory lung diseases, such as asthma, COPD, and chronic bronchitis, as well as…”
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15
The relevance of K i calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor
Published in European journal of medicinal chemistry (18-08-2017)“…Histone acetyltransferases (HATs) are important mediators of epigenetic post-translational modifications of histones that play important roles in health and…”
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The relevance of Ki calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor
Published in European journal of medicinal chemistry (18-08-2017)“…Histone acetyltransferases (HATs) are important mediators of epigenetic post-translational modifications of histones that play important roles in health and…”
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Effective siRNA delivery to inflamed primary vascular endothelial cells by anti-E-selectin and anti-VCAM-1 PEGylated SAINT-based lipoplexes
Published in International journal of pharmaceutics (01-01-2014)“…PEGylated anti-E-selectin and anti-VCAM-1-SAINTPEGarg are effective devices for siRNA delivery into the inflammation-activated primary endothelial cells (ECs)…”
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ATM increases activation-induced cytidine deaminase activity at downstream S regions during class-switch recombination
Published in The Journal of immunology (1950) (15-05-2014)“…Activation-induced cytidine deaminase (AID) initiates Ab class-switch recombination (CSR) in activated B cells resulting in exchanging the IgH C region and…”
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SAINT-liposome-polycation particles, a new carrier for improved delivery of siRNAs to inflamed endothelial cells
Published in European journal of pharmaceutics and biopharmaceutics (01-01-2015)“…•Design of new SAINT-C18 and protamine based carriers for siRNA delivery.•High siRNA encapsulation and low cellular toxicity.•Stability and siRNA integrity…”
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Reassessment of the Role of Mut S Homolog 5 in Ig Class Switch Recombination Shows Lack of Involvement in cis- and trans-Switching1
Published in The Journal of immunology (1950) (15-12-2008)“…When B cells are activated after immunization or infection, they exchange the gene encoding the Ig H chain C region by class switch recombination (CSR). CSR…”
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