Glucocorticoid Receptor (GR; NR3C1)
These Glucocorticoid Receptor Assay Systems utilize proprietary non-human mammalian reporter cells engineered to provide consitutive high-level expression of full-length, unmodified human NR3C1 protein, commonly referred to as GR.
INDIGO's Reporter Cells include the luciferase reporter gene functionally linked to a GR-responsive promoter. Thus, quantifying changes in luciferase expression in the treated reporter cells provides a sensitive surrogate measure of the changes in GR activity. Luciferase gene expression occurs after ligand-bound GR undergoes nuclear translocation, DNA binding, recruitment, and assembly of the co-activators and accessory factors required to forma functional transcription complex, culminating in expression of the reporter gene. Unlike some other cell-based assay strategies, the readout from INDIGO's reporter cells demands the same orchestration of all intracellular molecular interactions and events that can be expected to occur in vivo.
The glucocorticoid receptor is the receptor that cortisol and other glucocorticoids bind to. The GR is expressed in almost every cell in the body and regulates genes controlling the development, metabolism, and immune response.
For more information on GR, visit the Nuclear Receptor Resource.
Also available in: Mouse
Kits are offered in different assay formats to accommodate researchers' needs: 3x 32, 1x 96, and 1x 384 assay formats for screening small numbers of test compounds, as well as custom bulk reagents for HTS applications. Assay systems are all inclusive, providing reporter cells, optimized growth media, media for diluting test compounds, a positive-control agonist, luciferase detection reagent, a white assay plate, a detailed protocol, and a protocol quick guide. All kits are shipped on dry ice.
Reporter Cells are prepared using INDIGO’s proprietary CryoMite™ process. This cryo-preservation method yields high cell viability post-thaw, and provides the convenience of immediately dispensing healthy, division-competent reporter cells into assay plates. There is no need for intermediate spin-and-wash steps, viability determinations, or cell titer adjustments.
The principle application of this assay product is in the screening of test samples to quantify functional activities, either agonist or antagonist, that they may exert against the human androgen receptor. This kit product is an all-inclusive assay system that includes, in addition to GR Reporter Cells, two optimized media for use during cell culture and (optionally) in diluting the test samples, a reference agonist, Luciferase Detection Reagent, a cell culture-ready assay plate, and a detailed protocol.
Assay Kit & Platforms
| Product Family | Product Number | Product Description |
| IB0020 GR (NR3C1) | IB00201-32 | Human GR Reporter Assay System, 3 x 32 assays in 96-well format |
| IB00201 | Human GR Reporter Assay System, 1 x 96-well format assays | |
| IB00202 | Human GR Reporter Assay System, 1 x 384-well format assays |
Service Assays: Human, Rat, Mouse
The primary application of INDIGO's cell-based nuclear receptor assays are to quantitatively assess the bioactivity of a test compound as an agonist (activator) or antagonist (inhibition of an agonist response) of a given receptor. Service assays include a positive control reference compound and 'vehicle' control for every experiment. A formal study report and all data files are provided to the client upon completion of the study.
To receive a quote for your proposed study, complete & submit the online "Request a Quote" form or contact an INDIGO Customer Service Representative to discuss your desired study parameters. To initiate a Service Study, download and complete all fields of the Excel worksheet "Service Work Order" then submit the electronic file to INDIGO Customer Service.
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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
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