Androgen Receptors
Androgen receptors (ARs) (dihydrotestosterone receptors) are nuclear hormone receptors of the NR3C class, which includes mineralocorticoid, progesterone and glucocorticoid receptors. ARs are expressed in bone marrow, mammary gland and prostate tissues.
Androgen Receptor Agonists |
|
|---|---|
| Cat. No. | Product Name / Activity |
| 5274 | BMS 564929 |
| Highly potent and muscle-selective androgen receptor (AR) agonist | |
| 3812 | Cl-4AS-1 |
| Steroidal androgen receptor agonist | |
Androgen Receptor Antagonists |
|
| Cat. No. | Product Name / Activity |
| 4094 | Flutamide |
| Non-steroidal androgen receptor antagonist | |
| 6108 | Galeterone |
| Androgen receptor antagonist; also CYP17 inhibitor | |
Androgen Receptor Modulators |
|
| Cat. No. | Product Name / Activity |
| 3813 | TFM-4AS-1 |
| Selective androgen receptor modulator (SARM) | |
Androgen Receptor Inhibitors |
|
| Cat. No. | Product Name / Activity |
| 5842 | MK 386 |
| Potent, selective human type 1 5α-reductase inhibitor | |
Degraders |
|
| Cat. No. | Product Name / Activity |
| 7254 | ARCC 4 |
| Potent and selective androgen receptor degrader | |
Other |
|
| Cat. No. | Product Name / Activity |
| 4946 | AIM 100 |
| Potent and selective Ack1 inhibitor | |
| 3293 | Finasteride |
| Type II 5α-reductase inhibitor | |
| 3572 | GSK 650394 |
| Serum- and glucocorticoid-regulated kinase (SGK) inhibitor | |
| 2968 | Spironolactone |
| Antiandrogen; inhibits steroid hormone biosynthesis. Also MR antagonist | |
| 6223 | XY 018 |
| Inhibits AR expression; RORγ antagonist | |
Androgen receptors (ARs) (also known as dihydrotestosterone receptors) are nuclear hormone receptors of the NR3C class, which also includes mineralocorticoid, progesterone and glucocorticoid receptors. They are expressed in bone marrow, mammary gland, prostate, testicular and muscle tissues where they exist as dimers coupled to Hsp90 and HMGB proteins, which are shed upon ligand binding.
Activated androgen receptors bind to nuclear response elements of the genome, with an inverted palindromic 15 nucleotide sequence, to regulate gene transcription. Androgen receptors also affect gene expression through interaction with transcription factors including AP-1, NF-κB and STAT.
Target genes of androgen receptors include insulin-like growth factor 1 (IGF-1) and genes involved in the development of primary and secondary male sexual characteristics, maintenance of sexual function and possibly have a causative role in aggressive behavior. Furthermore, androgen receptors have recently been shown to have actions that are independent of DNA interactions.
Congential mutations in androgen receptors are associated with androgen insensitivity syndromes, virility and spinal and bulbar muscular atrophy. Perturbations in androgen receptor expression is also a common feature of prostate cancer. The human gene encoding the androgen receptor has been localized to Xq11-12.