The Roles of the Androgen Receptor in Disease and Drug Discovery

Androgen Receptor (AR)

What is the Androgen Receptor (AR)?

The Androgen Receptor (AR) is a member of the nuclear receptor family of transcription factors that play a critical role in the development and function of male reproductive tissues. AR is expressed in a variety of tissues, including the prostate gland, testes, and skeletal muscle. Upon binding to androgens, such as testosterone and dihydrotestosterone (DHT), AR undergoes a conformational change that allows it to translocate to the nucleus and regulate the expression of target genes.

AR’s Role in Male and Female Diseases

The physiological role of AR is diverse and includes the regulation of male sexual differentiation, sperm production, and muscle mass maintenance. In addition, AR has been implicated in the development and progression of prostate cancer, a disease that affects millions of men worldwide. Androgen receptors are found inside the cells of male reproductive tissue and some cancer cells. In prostate cancer, androgens bind to androgen receptors inside the cancer cells, which causes the cancer cells to grow.

While the Androgen Receptor (AR) is traditionally associated with male physiology, it also plays important roles in women. Women produce androgens, such as testosterone and DHT, in their ovaries and adrenal glands, and these hormones can interact with AR to regulate various physiological processes. For example, in women, AR is involved in the regulation of bone density, muscle mass, and sexual function. In addition, some studies have suggested that AR signaling may contribute to the development of polycystic ovary syndrome (PCOS), a condition that affects women and is characterized by irregular menstrual cycles, insulin resistance, and excess androgen production.

Several types of chemicals can interact with AR, including endogenous and exogenous ligands. Endogenous ligands for the AR include testosterone and DHT, while exogenous ligands include anabolic steroids, such as oxandrolone and stanozolol. In addition, environmental pollutants such as bisphenol A (BPA) and phthalates have been shown to interact with AR and may have adverse effects on human health.

AR’s Role in Drug Discovery

There is significant interest in AR as a drug discovery target, particularly for the treatment of prostate cancer. Several drugs that target AR, including enzalutamide and abiraterone, have been approved for the treatment of advanced prostate cancer. However, the development of resistance to these drugs is a significant clinical challenge, and new AR-targeted therapies are needed. AR-targeted therapies are also being explored for the treatment of breast cancer in women. While breast cancer is traditionally thought of as an estrogen-driven disease, AR is expressed in up to 90% of breast tumors, and its signaling can promote tumor growth and metastasis. Therefore, targeting AR may be a promising therapeutic strategy for certain types of breast cancer.

INDIGO’s AR Reporter Assays

INDIGO Biosciences offers cell-based luciferase reporter assay kits for the Androgen Receptor. Our assays provide an all-inclusive luciferase reporter system that includes, in addition to AR Reporter Cells, optimized media for use during cell culture and in diluting the user’s test samples, a reference agonist, Luciferase Detection Reagent, and a cell culture-ready assay plate. INDIGO can also perform the AR assay in its own lab as a service for researchers.

INDIGO’s cell-based reporter assays allow scientists to screen and discover drugs that can be used to treat ER-related diseases. They provide an efficient way to examine a compound for its ability to regulate nuclear receptor activity in agonist, inverse-agonist, or antagonist mode using firefly luciferase reporter gene technology. Since the receptor binding controls the expression of the luciferase reporter gene, luciferase activity in the cells can be correlated directly with the activity of the receptor. Contact us today to learn more about our Androgen Receptor assay kits and screening capabilities!


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