N-Terminal domain antiandrogen

See also: Discovery and development of antiandrogens § N-Terminal domain antagonists
N-Terminal domain antiandrogen
Drug class
EPI-001, the first major N-terminal domain AR antagonist to be developed.
Class identifiers
SynonymsN-Terminal domain AR antagonists; AR NTD antagonists
UseProstate cancer
Biological targetAndrogen receptor
Legal status
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.[1][2]

See also

References

  1. ^ Sekhon, Inderpal; Ashong, Dennis; Chen, Guanglin; Chen, Qiao-Hong (2026-03-05). "Small-molecule modulators of the androgen receptor N-terminal domain: Advances in medicinal chemistry for prostate cancer". European Journal of Medicinal Chemistry. 305 118580. doi:10.1016/j.ejmech.2026.118580. ISSN 1768-3254. PMID 41544581.
  2. ^ Rajwa, Pawel; Zapała, Piotr; Merseburger, Axel S. (January 2025). "Targeting Androgen Receptor Alterations in Metastatic Prostate Cancer". European Urology Focus. 11 (1): 79–81. doi:10.1016/j.euf.2024.07.012. ISSN 2405-4569. PMID 39107195.


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