Androgen Receptor (AR; NR3C4)
Also available in: Rat
This nuclear receptor assay system utilizes proprietary non-human mammalian cells engineered to provide constitutive, high-level expression of full length, unmodified Human Androgen Receptor (NR3C4), a ligand-dependent transcription factor commonly referred to as AR.
INDIGO’s Reporter Cells include the luciferase reporter gene functionally linked to a
The androgen receptor is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA binding transcription factor which regulates gene expression; however, the androgen receptor has other functions as well.
Androgen regulated genes are critical for the development and maintenance of the male sexual phenotype. In some cell types testosterone interacts directly with androgen receptors while in others testosterone is converted by 5-alpha-reductase to dihydrotestosterone, an even more potent agonist for androgen receptor activation. Testosterone appears to be the primary androgen receptor activating hormone in the Wolffian duct while dihydrotestosterone is the main androgenic hormone in the urogenital sinus, urogenital tubercle, and hair follicles. Hence testosterone is primarily responsible for the development of male primary sexual characteristics while dihydrotestosterone is responsible for secondary male characteristics.
For more information on AR, visit the Nuclear Receptor Resource.
Also available in: Rat
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.
AR 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 AR 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 |
| IB0300 AR (NR3C4) | IB03001-32 | Human AR Reporter Assay System, 3 x 32 assays in 96-well format |
| IB03001 | Human AR Reporter Assay System, 1 x 96-well format assays | |
| IB03002 | Human AR Reporter Assay System, 1 x 384-well format assays |
Service Assays: Human, Rat
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.
Intramolecular [2+2] Photocycloaddition of Altrenogest: Confirmation of Product Structure, Theoretical Mechanistic Insight, and Bioactivity Assessment
ABSTRACT While studying the environmental fate of potent endocrine-active steroid hormones, we observed the formation of an intramolecular [2+2] photocycloaddition product (2) with a novel hexacyclic ring system following photolysis of altrenogest (1). The structure and absolute configuration were established by X-ray diffraction analysis. Theoretical computations identified a barrierless two-step cyclization mechanism for the formationRead More
Novel Small Molecule Guanidine Sigma1 Inhibitors for Advanced Prostate Cancer
ABSTRACT Prostate cancer is the most frequently diagnosed malignancy and the leading cause of cancer related death in men. First line therapy for disseminated disease relies on androgen deprivation, leveraging the addiction of these tumors on androgens for both growth and survival. Treatment typically involves antagonizing the androgen receptor (AR) or blocking the synthesis ofRead 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
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
An Automated Cell-Based Platform for the Rapid Detection of Novel Androgen Receptor Modulators
View Full Size Research conducted by: Brad Larson (1), Bruce Sherf (2), & Peter Banks (1) (1)BioTek Instruments, Inc., Winooski, VT, USA (2) INDIGO Biosciences, Inc., State College, PA, USA Date of Publication: March 2012
An Automated, Cell-based Platform for the Rapid Detection of Novel Androgen Receptor Modulators
ABSTRACT The Androgen Receptor (AR) is a member of the family of nuclear receptors responsive to steroid hormones. AR activity is regulated through the binding of androgenic hormones (eg., testosterone and di-hydroxy testosterone). In turn, AR functions to regulate the expression of a myriad of genes involved in metabolic processes, cell proliferation/apoptosis, and male sexual differentiation and development. AR dysfunction often hasRead More