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

Niek G.J. Leus, Petra E. van der Wouden, Thea van den Bosch, +7

Biochemical Pharmacology

HDAC1-3 inhibitor MS-275 enhances IL10 expression in RAW264.7 macrophages and reduces cigarette smoke-induced airway inflammation in mice

Niek G.J. Leus, Thea van den Bosch, Petra E. van der Wouden, +11

Scientific Reports

Anti-VCAM-1 SAINT-O-Somes enable endothelial-specific delivery of siRNA and downregulation of inflammatory genes in activated endothelium in vivo

Piotr S. Kowalski, Peter J. Zwiers, Henriëtte W. M. Morselt, +5

Journal of Controlled Release

InflammationEndothelial Cell PathobiologyCytokineAnti-inflammatoryMedicine +8

The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases

Thea van den Bosch, Alexander P. Boichenko, Niek G.J. Leus, +8

Biochemical Pharmacology

Histone ModificationsChromatinInflammationHistone DeacetylasesChromatin Remodeling +10

Anti-VCAM-1 and Anti-E-selectin SAINT-O-Somes for Selective Delivery of siRNA into Inflammation-Activated Primary Endothelial Cells

Piotr S. Kowalski, Lucas L. Lintermans, Henriëtte W. M. Morselt, +4

Molecular Pharmaceutics

NanotherapeuticsEndothelial CellsEngineeringImmunologyInnate Immunity +19

Rational Development of a Potent 15-Lipoxygenase-1 Inhibitor with <i>in Vitro</i> and <i>ex Vivo</i> Anti-inflammatory Properties

Nikolaos Eleftheriadis, Constantinos G. Neochoritis, Niek G.J. Leus, +3

Journal of Medicinal Chemistry

Drug TargetRational DevelopmentMammalian LipoxygenaseChemical BiologyOxidative Stress +16

Design of a novel thiophene inhibitor of 15-lipoxygenase-1 with both anti-inflammatory and neuroprotective properties

Nikolaos Eleftheriadis, Hessel Poelman, Niek G.J. Leus, +5

European Journal of Medicinal Chemistry

Anti-inflammatoryNovel Thiophene InhibitorBiochemistryMedicineLipid Peroxidation +6

Effective siRNA delivery to inflamed primary vascular endothelial cells by anti-E-selectin and anti-VCAM-1 PEGylated SAINT-based lipoplexes

Niek G.J. Leus, Eduard G. Talman, Pranov Ramana, +5

International Journal of Pharmaceutics

Cell-based Drug DeliveryNanomedicineTranslational MedicineEngineeringMedicine +8

VCAM-1 specific PEGylated SAINT-based lipoplexes deliver siRNA to activated endothelium in vivo but do not attenuate target gene expression

Niek G.J. Leus, Henriëtte W. M. Morselt, Peter J. Zwiers, +4

International Journal of Pharmaceutics

Lipid SynthesisVascular BiologyGene DeliveryGene VectorGene Expression +5

A 6-alkylsalicylate histone acetyltransferase inhibitor inhibits histone acetylation and pro-inflammatory gene expression in murine precision-cut lung slices

Thea van den Bosch, Niek G.J. Leus, Hannah Wapenaar, +5

Pulmonary Pharmacology & Therapeutics

InflammationChromatinInflammatory Lung DiseaseLung InflammationMedicine +7