ABSTRACT Glucocorticoids (GCs) are commonly used topical treatments for skin diseases but are associated with both local and systemic side effects. In this study, we describe a selective non-steroidal glucocorticoid receptor (GR) agonist for topical use, LEO 134310, which is rapidly deactivated in the blood resulting in low systemic exposure and a higher therapeutic indexRead More
A ready-to-use, thermoresponsive, and extended-release delivery system for the paranasal sinuses
Abstract A drug delivery system for the paranasal sinuses consisting of a freeze-dried thermoresponsive hydrogel with degradable microspheres, called FD-TEMPS (Freeze Dried—Thermogel, Extended-release Microsphere-based delivery to the Paranasal Sinuses), was developed. Glass transition temperatures (Tg′) of the maximally freeze concentrated solutions consisting of poly(N-isopropylacrylamide) (pNIPAAm) and polyethylene glycol (PEG) were determined by differential scanning calorimetry,Read More
A thermoresponsive hydrogel system for long-acting corticosteroid delivery into the paranasal sinuses
ABSTRACT Delivering localized treatment to the paranasal sinuses for diseases such as chronic rhinosinusitis (CRS) is particularly challenging because of the small natural openings leading from the sinuses that can be further obstructed by presence of inflammation. As such, oral steroids, topical nasal sprays or irrigation, and surgery can be utilized to treat persistent sinonasalRead More
Zebrafish Glucocorticoid Receptor (zGR; nr3c1)
Zebrafish Glucocorticoid Receptor (zGR; nr3c1) Product Family Product Number Product Description Technical Manual Z0020 zGR (nr3c1) Z00201-32 Zebrafish GR Reporter Assay System, 3 x 32 assays in 96-well format Technical Manual Z00201 Zebrafish GR Reporter Assay System, 1 x 96-well format assays Technical Manual
Gene Expression: Nuclear Receptors
INTRODUCTION There are four main classes of receptors, Ion channels, G-protein coupled (GPCR), receptor tyrosine kinase and soluble (also called intracellular) receptors. The first three have ligands that are mainly present in the extracellular space (water soluble ligands). The binding of ligand causes a change in the shape/function of the protein that generates a signalRead More
Nuclear Receptors Regulate Intestinal Inflammation in the Context of IBD
ABSTRACT Gastrointestinal (GI) homeostasis is strongly dependent on nuclear receptor (NR) functions. They play a variety of roles ranging from nutrient uptake, sensing of microbial metabolites, regulation of epithelial intestinal cell integrity to shaping of the intestinal immune cell repertoire. Several NRs are associated with GI pathologies; therefore, systematic analysis of NR biology, the underlyingRead More
Quizalofop-p-ethyl induces adipogenesis in 3T3-L1 adipocytes
ABSTRACT Exposure to endocrine disrupting chemicals is an established risk factor for obesity. The most commonly used pesticide active ingredients have never been tested in an adipogenesis assay. We tested for the first time the potential of glyphosate, 2,4-dichlorophenoxyacetic acid, dicamba, mesotrione, isoxaflutole and quizalofop-p-ethyl (QpE) to induce lipid accumulation in murine 3T3-L1 adipocytes. OnlyRead More
JTP-117968, a novel selective glucocorticoid receptor modulator, exhibits improved transrepression/transactivation dissociation
ABSTRACT Classic glucocorticoids that have outstanding anti-inflammatory effects are still widely prescribed for the treatment of various inflammatory and autoimmune diseases. Conversely, glucocorticoids cause numerous unwanted side effects, particularly systemically dosed glucocorticoids. Therefore, selective glucocorticoid receptor modulator (SGRM), which maintains beneficial anti-inflammatory effects while reducing the occurrence of side effects, is one of the mostRead More
Rat Glucocorticoid Receptor (rGR; nr3c1)
Rat Glucocorticoid Receptor (rGR; nr3c1) Product Family Product Number Product Description Technical Manual R0020 rGR (nr3c1) R00201-32 Rat GR Reporter Assay System, 3 x 32 assays in 96-well format Technical Manual R00201 Rat GR Reporter Assay System, 1 x 96-well format assays Technical Manual
Glucocorticoid Receptor (GR; NR3C1)
Glucocorticoid Receptor (GR; NR3C1) Product Family Product Number Product Description Technical Manual IB0020 GR (NR3C1) IB00201-32 Human GR Reporter Assay System, 3 x 32 assays in 96-well format Technical Manual IB00201 Human GR Reporter Assay System, 1 x 96-well format assays Technical Manual IB00202 Human GR Reporter Assay System, 1 x 384-well format assays TechnicalRead More