(R)-Bicalutamide, androgen receptor antagonist

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The androgen receptor (AR) also known as NR3C4 functions mechanically as a type of nuclear receptor that is activated by binding androgens including testosterone and dihydrotestosterone. The AR has a molecular weight of approximately 110 kDa. It is expressed in various tissues notably in the prostate skeletal muscle and certain areas of the brain. Within cells AR is usually located in the cytoplasm when unbound and translocates to the nucleus upon activation by its ligands.

Biological function summary

AR interacts with androgen hormones to regulate gene expression. It forms a complex with coactivators and corepressors to modulate transcription of target genes involved in male sexual development and reproductive function. AR plays an important role in the development and maintenance of male characteristics and reproductive activity. Its expression impacts cellular processes such as proliferation differentiation and apoptosis.

Pathways

AR is intricately involved in the androgen signaling pathway which affects the regulation of genes related to male sexual characteristics. It also plays a part in the PI3K/Akt pathway influencing cell growth and survival. The AR pathway interacts with proteins such as estrogen receptors to mediate cross-talk between hormonal pathways highlighting its broad biological impacts.

AR has a significant connection to prostate cancer where it drives tumor growth and progression. Mutations and overexpression of the androgen receptor are often observed in prostate cancer cells. Another condition linked to AR is androgen insensitivity syndrome where mutations in the AR gene result in partial or complete inability of cells to respond to androgenic hormones. In these conditions AR antagonists like bicalutamide are often used as treatment inhibiting the receptor's activity to manage disease progression.