RAR-related Orphan Receptor Gamma (RORγ; NR1F3)
Also available in Mouse
INDIGO’s Human RAR-related Orphan Receptor Gamma (NR1F3; RORγ) Assay utilizes proprietary human cells engineered to provide high-level expression of a hybrid form of RORγ. The N-terminal DNA binding domains (DBD) of the native RORγ and RORγt receptors (isoforms 1 and 2, respectively) have been substituted with that of the yeast GAL4-DBD. Hence, the GAL4-RORγ hybrid expressed in these reporter cells will not discern functional differences that may exist between the native isoform 1 and isoform 2 receptors. Endogenous molecular activators maintain RORγ in a state of constitutive high-level activity. Therefore, the principle application of this reporter assay system is in the screening of test samples to quantify inverse-agonist or antagonist activities that they may exert against human RORγ.
RAR-related orphan receptor gamma (ROR-gamma), also known as NR1F3 is a nuclear receptor encoded by the RORG gene.The RAR-related orphan receptors (RORs) are members of the nuclear receptor family of intracellular transcription factors. There are three forms of ROR, ROR-α, -β, and -γ and each is encoded by a separate gene (RORA, RORB, and RORC respectively). The RORs are somewhat unusual in that they appear to bind as monomers to hormone response elements as opposed to the majority of other nuclear receptors which bind as dimers. Melatonin has been reported to be the endogenous ligand for ROR-α while CGP 52608 has been identified as a ROR-α selective synthetic ligand. However X-ray crystallographic (PDB 1n83 and 1s0x) and functional data both suggest that cholesterol or a cholesterol derivative may be the endogenous ligand. In contrast, all-trans retinoic acid binds with high affinity to ROR-β and -γ but not ROR-α.
For more information on RORγ, visit the Nuclear Receptor Resource.
Also available in: Mouse
Kits are offered in different assay formats to accommodate researchers’ needs: 3x 32 and 1x 96 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 inverse-agonist, luciferase detection reagent, a white assay plate, a detailed protocol, and a protocol quick guide. All kits are shipped on dry ice.
RORγ 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.
This kit product is an all-inclusive assay system that includes, in addition to RORγ Reporter Cells, two optimized media for use during cell culture and (optionally) in diluting the test samples, a reference inverse-agonist, Luciferase Detection Reagent, a cell culture-ready assay plate, and a detailed protocol.
| Product Family | Product Number | Product Description |
| IB0400 RORγ (NR1F3) | IB04001-32 | Human RORγ Reporter Assay System, 3 x 32 assays in 96-well format |
| IB04001 | Human RORγ Reporter Assay System, 1 x 96-well format assays |
Service Assays: Human, 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.
Discovery of Retinoic Acid-Related Orphan Receptor γt Inverse Agonists via Docking and Negative Image-Based Screening
ABSTRACT Retinoic acid-related orphan receptor γt (RORγt) has a vital role in the differentiation of T-helper 17 (TH17) cells. Potent and specific RORγt inverse agonists are sought for treating TH17-related diseases such as psoriasis, rheumatoid arthritis, and type 1 diabetes. Here, the aim was to discover novel RORγt ligands using both standard molecular docking andRead More
Metadichol, A Novel ROR Gamma Inverse Agonist and Its Applications in Psoriasis
ABSTRACT Psoriasis affects 3% of the population worldwide, and there is no known cure. Psoriasis is associated with an increased risk of psoriatic arthritis, lymphomas, cardiovascular disease, and Crohn’s disease. Psoriasis treatments today include steroid and vitamin D3 cream, ultraviolet light, and immune system suppressing medications such as methotrexate. The T cells responsible for psoriasisRead More
ROR Modulators and Their Uses
Compound binding to the human RORγ LBD was assessed using the Human RORγ Assay System from Indigo Biosciences. ABSTRACT There are high unmet medical needs in the few established therapies for several autoimmune, inflammatory and metabolic diseases. Despite the diverse clinical manifestations of these diseases, Retinoic Acid Receptor-Related Orphan Receptors (RORs) regulate and contribute to theRead 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