''N''-Terminal domain antiandrogen

N-Terminal domain antiandrogen
Drug class
EPI-001, the first major N-terminal domain AR antagonist to be developed.
Class identifiers
Synonyms N-Terminal domain AR antagonists; AR NTD antagonists
Use Prostate cancer
Biological target Androgen receptor
In Wikidata

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 bisphenol A diglycidyl ether (BADGE), EPI-001, ralaniten (EPI-002), and ralaniten acetate, (EPI-506).[1]

See also

References

  1. ↑ 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. doi:10.4103/1008-682X.181081. ISSN 1008-682X.


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