Measure nuclear receptor activity with functional promoter reporter assays
Nuclear receptors, ligand-activated transcription factors, are critical for understanding gene regulation and the genomic events that lead to development, differentiation, and growth in an organism. Ligands for nuclear receptors (NRs) include a variety of small molecules such as steroids and fatty acids. Xenobiotics and various pharmaceutical agents also serve as NR ligands, illustrating the importance of NR-mediated toxicity screening.
SwitchGear Genomics offers comprehensive panels of cell-based reporter assays to evaluate NR-mediated transcriptional regulation. Our collection of promoter reporters consist of known and predicted targets for key nuclear receptors: aryl hydrocarbon receptor (AhR)*, peroxisome proliferator-activated receptors (PPARs), constitutive androstane receptor (CAR), pregnane X receptor (PXR), androgen receptor (AR), estrogen receptor (ER), and glucocorticoid receptor (GR). The AR, ER, and GR sets are also specifically available as empirically-validated profiling panels and biomarker sets, assembled using pathway-specific inductions.
Our assay-ready constructs allow you to measure the response of nuclear receptor proteins upon exposure to small molecules by rapidly and reliably measuring NR-mediated transcriptional activity.
Nuclear receptor functional assay workflow
| 1. Expose NR protein to small molecule. | 2. Small molecule binds to ligand binding domain and activates the NR. | 3. Activated NR binds to human promoter and activates or represses transcription. | 4. Promoter activity is measured by luciferase reporter assay allowing functional evaluation of the NR response to a small molecule. |
SwitchGear Promoter Reporter Assay for Nuclear Receptors
| Cell-based reporter assay Expose each well to small molecule |
Selected Promoter Targets of Specific Nuclear Receptors |
1. Each well has a reporter construct for a different NR target promoter (see panel descriptions).
2. Light signal measures the NR-driven response for each human promoter.
3. Top responding promoters can be implemented in a routine screen.
SwitchGear Nuclear Receptor Panels
We offer the following assay-ready promoter reporters for known and predicted NR targets.
| Transcription factor | Number of constructs available |
Example target genes | Known ligands |
| AhR* | 99 | CYP1A1, CYP1B1, GLRX5 | Aromatic hydrocarbons, dioxins, dibenzofurans, biphenyls, bilirubin |
| PPARs | 288 | CCDC51, PLTP | Fatty acids, eicosanoids, prostaglandin, leukotrienes, TZDs |
| PXR/CAR | 112 | CYP3A, CYP2B, CYP2C | Steroids, xenobiotics |
| AR | Validated constructs | PSA, ABCC4, SOCS2 | Testosterone, dihydrotestosterone, 2-quinolones, phthalamides |
| ER | Validated constructs | GAPDH, TFF1, CASP7 | 17-beta-estradiol, estrone, raloxifene, estriol, genistein |
| GR | Validated constructs | SLC38A4, SDPR, SNTA1 | Cortisol, dexamethasone, prednisone, RU486, cyproterone |
Other nuclear receptor promoter reporter assays not listed above are also available such as for RXR and RAR. Please inquire.
*AhR, though not in the nuclear receptor superfamily, is taken into consideration along with nuclear receptors due to its functional similarities. Selection criteria for all constructs include a combination of sequence motif analysis, available published data, as well as ChIP-chip and other binding data. The AR, ER, and GR panels have been experimentally-validated through specific induction studies.
The SwitchGear Advantage
SwitchGear’s nuclear receptor panel of reporter vectors is:
- Quantitative: Measure nuclear receptor activity in response to stimuli using a highly quantitative luciferase assay to measure NR-mediated activity.
- Simple and quick: Perform your experiments today through simple transfection of our luciferase reporter constructs. No cloning or DNA preparation is needed.
- Comprehensive and verified: Choose from SwitchGear’s complete set of sequence verified and transfection ready NR targets.