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
Oxysterols are agonist ligands of RORγt and drive Th17 cell differentiation
ABSTRACT The RAR-related orphan receptor gamma t (RORγt) is a nuclear receptor required for generating IL-17–producing CD4+ Th17 T cells, which are essential in host defense and may play key pathogenic roles in autoimmune diseases. Oxysterols elicit profound effects on immune and inflammatory responses as well as on cholesterol and lipid metabolism. Here, we describe the identification of several naturally occurringRead More
Structural Stereochemistry of Androstane Hormones Determines Interactions with Human Androgen, Estrogen, and Glucocorticoids Receptors
ABSTRACT DHEA, 17α-AED, 17β-AED, and 17β-AET exhibit strong biological activity that has been attributed to androgenic, estrogenic, or antiglucocorticoid activity in vivo and in vitro. This study compared DHEA, 17α-AED, 17β-AED, and 17β-AET for their ability to activate the human AR, ER, and GR and determine the relative androgenicity, estrogenicity, and glucocorticoid activity. The results show that, at theRead More