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N-Terminal domain antiandrogen

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N-Terminal domain antiandrogen
Drug class
EPI-001.svg
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
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.{{cite journal}}: CS1 maint: article number as page number (link)
  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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