Estrogen Receptor Beta (ERβ; ESR2; NR3A2)
These ERβ Reporter Assay Systems utilize non-human mammalian cells engineered to express human ESR2, commonly referred to as NR3A2 or ERβ.
Estrogen receptor beta (ER-beta), also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2), is a nuclear receptor which is activated by the sex hormone estrogen. ER beta is encoded by the human gene ESR2 (EStrogen Receptor 2). This gene encodes a member of the family of estrogen receptors and superfamily of nuclear receptor transcription factors. The gene product contains an N-terminal DNA binding domain and C-terminal ligand binding domain and is localized to the nucleus, cytoplasm, and mitochondria. Upon binding to 17beta-estradiol or related ligands, the encoded protein forms homo- or hetero-dimers that interact with specific DNA sequences to activate transcription. Some isoforms dominantly inhibit the activity of other estrogen receptor family members. Several alternatively spliced transcript variants of this gene have been described, but the full-length nature of some of these variants has not been fully characterized. ERβ is expressed by many tissues including blood monocytes and tissue macrophages, colonic and pulmonary epithelial cells and in prostatic epithelium and in malignant counterparts of these tissues. ERβ may have anti-proliferative effects and therefore oppose the actions of ERα in reproductive tissue. ERβ may also have an important role in adaptive function of the lung during pregnancy.
For more information on ERβ, visit the Nuclear Receptor Resource.
Kits are offered in different assay formats to accommodate researchers’ needs: 3 x 32, 1 x 96, and 1 x 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.
ER Beta 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 estrogen receptor beta. This kit product is an all-inclusive assay system that includes, in addition to ER Beta 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.
| Product Family | Product Number | Product Description |
| IB0041 ERα (NR3A1) | IB00411-32 | Human ERβ Reporter Assay System, 3 x 32 assays in 96-well format |
| IB00411 | Human ERβ Reporter Assay System, 1 x 96-well format assays | |
| IB00412 | Human ERβ Reporter Assay System, 1 x 384-well format assays |
Service Assays: Human
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.
Novel synthesised flavone derivatives provide significant insight into the structural features required for enhanced anti-proliferative activity
ABSTRACT With many cancers showing resistance to current chemotherapies, the search for novel anti-cancer agents is attracting considerable attention. Natural flavonoids have been identified as useful leads in such programmes. However, since an in-depth understanding of the structural requirements for optimum activity is generally lacking, further research is required before the full potential of flavonoids as anti-proliferative agentsRead More
Novel synthesised flavone derivatives provide significant insight into the structural features required for enhanced anti-proliferative activity
ABSTRACT With many cancers showing resistance to current chemotherapies, the search for novel anti-cancer agents is attracting considerable attention. Natural flavonoids have been identified as useful leads in such programmes. However, since an in-depth understanding of the structural requirements for optimum activity is generally lacking, further research is required before the full potential of flavonoidsRead More
Phytoestrogenic activity of blackcurrant (Ribes nigrum) anthocyanins is mediated through estrogen receptor alpha
ABSTRACT Blackcurrants (Ribes nigrum L., Grossulariaceae) contain high amounts of anthocyanin polyphenols, which have antioxidant and anti-carcinogenic health benefits. This study analyzed the potential phytoestrogenic effects of blackcurrant extract (BCE) in breast cancer (MCF-7) and human endometrial cancer (Ishikawa) cell lines that over-express estrogen receptor alpha (ERα), as well as in immature female rats. ToRead More
Cholesterol synthesis inhibitor RO 48-8071 suppresses transcriptional activity of human estrogen and androgen receptor
ABSTRACT Breast cancer cells express enzymes that convert cholesterol, the synthetic precursor of steroid hormones, into estrogens and androgens, which then drive breast cancer cell proliferation. In the present study, we sought to determine whether oxidosqualene cyclase (OSC), an enzyme in the cholesterol biosynthetic pathway, may be targeted to suppress progression of breast cancer cells. In previous studies, weRead 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
Probing the human estrogen receptor-a binding requirements for phenolic mono- and di-hydroxyl compounds: A combined synthesis, binding and docking study
ABSTRACT Various estrogen analogs were synthesized and tested for binding to human ERα using a florescence polarization displacement assay. Binding affinity and orientation were also predicted using docking calculations. Docking was able to accurately predict relative binding affinity and orientation for estradiol, but only if a tightly bound water molecule bridging Arg394/Glu353 is present. Di-hydroxylRead 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