What are androgen receptor ligands?
Androgen receptor (AR) is a ligand-activated transcription factor that plays a pivotal role in the development and progression of many severe diseases such as prostate cancer, muscle atrophy, and osteoporosis. Therefore, AR ligands have great potential to treat these diseases.
How is androgen receptor activated?
The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone in the cytoplasm and then translocating into the nucleus.
What is ligand independent signaling?
Instead, ligand-independent EGFR signaling triggers a non-canonical EGFR pathway that is regulated by activation of the transcription factor IRF3. Thus, EGFR overexpression leads to phosphorylation and activation of IRF3 and transcription of IRF3-dependent downstream genes such as IFIT1, IFI27 and TRAIL.
What is the ligand of testosterone?
Endogenous AR ligands include testosterone and its active metabolite, 5α-DHT. Testosterone is primarily synthesized from cholesterol (Figure 6) in Leydig cells in the testes. It is also synthesized in adrenal cortex, liver, and ovary in women.
What is the role of the androgen receptor?
Androgen receptors allow the body to respond appropriately to these hormones. The receptors are present in many of the body’s tissues, where they attach (bind) to androgens. The resulting androgen-receptor complex then binds to DNA and regulates the activity of androgen-responsive genes.
What is constitutive activation?
Constitutive activity is defined as ligand-independent activity, resulting in the production of a second messenger, even in the absence of an agonist (Fig. 1). It is also referred to as a ‘gain-of-function’ phenotype.
What is the difference between androgen and testosterone?
Androgens are sex hormones Androgens are the group of sex hormones that give men their ‘male’ characteristics (collectively called virilisation). The major sex hormone in men is testosterone, which is produced mainly in the testes.