N-Terminal domain antiandrogen
N-Terminal domain antiandrogens are a novel type of antiandrogen that bind to the N-terminal domain of the androgen receptor (AR) instead of the ligand-binding domain (where all currently-available antiandrogens bind) and disrupt interactions between the AR and its coregulatory binding partners, thereby blocking AR-mediated gene transcription. They are being investigated for the treatment of prostate cancer. Examples of these drugs include EPI-001, EPI-506, and BAY-1024767.[1]
See also
References
- ↑ Monaghan, AmyE; McEwan, IainJ (2016). "A sting in the tail: the N-terminal domain of the androgen receptor as a drug target". Asian Journal of Andrology. 0 (0): 0. ISSN 1008-682X. doi:10.4103/1008-682X.181081.
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Androgens
(incl. AAS) | |
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| Antiandrogens | | AR antagonists | |
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Steroidogenesis
inhibitors | |
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| Antigonadotropins |
- D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, sulpiride)
- Estrogens (e.g., bifluranol, diethylstilbestrol, estradiol, estradiol esters, ethinylestradiol, ethinylestradiol sulfonate, paroxypropione)
- GnRH agonists (e.g., leuprorelin)
- GnRH antagonists (e.g., cetrorelix)
- Progestogens (incl., chlormadinone acetate, cyproterone acetate, hydroxyprogesterone caproate, gestonorone caproate, medroxyprogesterone acetate, megestrol acetate)
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| Others | |
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See also: Estrogens and antiestrogens • Progestogens and antiprogestogens • Glucocorticoids and antiglucocorticoids • Mineralocorticoids and antimineralocorticoids • Gonadotropins and GnRH |