Combination therapy with androgen receptor N‐terminal domain antagonist EPI‐7170 and enzalutamide yields synergistic activity in AR‐V7‐positive prostate cancer | Zendy

Hirayama Yukiyoshi | Zendy; Tam Teresa | Zendy; Jian Kunzhong | Zendy; Andersen Raymond J. | Zendy; Sadar Marianne D. | Zendy

Open Access

Combination therapy with androgen receptor N‐terminal domain antagonist EPI‐7170 and enzalutamide yields synergistic activity in AR‐V7‐positive prostate cancer

Author(s) -

Hirayama Yukiyoshi,

Tam Teresa,

Jian Kunzhong,

Andersen Raymond J.,

Sadar Marianne D.

Publication year - 2020

Publication title -

molecular oncology

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.332

H-Index - 88

eISSN - 1878-0261

pISSN - 1574-7891

DOI - 10.1002/1878-0261.12770

Subject(s) - enzalutamide , androgen receptor , prostate cancer , antagonist , androgen , androgen deprivation therapy , endocrinology , medicine , cancer research , chemistry , receptor , cancer , pharmacology , hormone

Ralaniten and analogs (EPI) bind androgen receptor N‐terminal domain (AR‐NTD) to block the transcriptional activities of full‐length AR (FL‐AR) and AR splice variants (AR‐Vs). Enzalutamide (ENZ) elevates levels of AR‐V7 leading to resistance and increased proliferation. Targeting AR‐NTD to block FL‐AR and AR‐Vs with EPI in combination with ENZ resulted in synergistic inhibition of proliferation of ENZ‐resistant prostate cancer cells.

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