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Review

AR-V7 in Metastatic Prostate Cancer: A Strategy beyond Redemption

1
Department of Medicine, Section of Epidemiology and Population Sciences, Baylor College of Medicine, Houston, TX 77030, USA
2
Department of Biology and Biochemistry, University of Bath, Bath BA2 7AY, UK
3
Department of Surgery and Cancer, Imperial College London, London W12 0NN, UK
4
Azienda Socio-Sanitaria Territoriale Cremona, 26100 Cremona, Italy
5
Histopathology and Molecular Diagnostics, Careggi Teaching Hospital, 50139 Florence, Italy
6
Department of Health Sciences, University of Florence, 50139 Florence, Italy
*
Author to whom correspondence should be addressed.
Academic Editor: Josiah Ochieng
Int. J. Mol. Sci. 2021, 22(11), 5515; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22115515
Received: 4 May 2021 / Revised: 20 May 2021 / Accepted: 20 May 2021 / Published: 24 May 2021
(This article belongs to the Special Issue Molecular Determinants of Prostate Cancer Metastasis)
Metastatic prostate cancer is the most common cancer in males and the fifth cause of cancer mortality worldwide. Despite the major progress in this field, leading to the approval of novel anti-androgens, the prognosis is still poor. A significant number of patients acquire an androgen receptor splice variant 7 (AR-V7), which is constitutively activated and lacks the ligand-binding domain (LBD) while maintaining the nuclear localization signal and DNA-binding domain (DBD). This conformational change, even in the absence of the ligand, allows its retention within the nucleus, where it acts as a transcription factor repressing crucial tumor suppressor genes. AR-V7 is an important oncogenic driver and plays a role as an early diagnostic and prognostic marker, as well as a therapeutic target for antagonists such as niclosamide and TAS3681. Anti-AR-V7 drugs have shown promise in recent clinical investigations on this subset of patients. This mini-review focuses on the relevance of AR-V7 in the clinical manifestations of castration-resistant prostate cancer (CRPC) and summarizes redemptive therapeutic strategies. View Full-Text
Keywords: androgen receptor; androgen receptor splice variant 7; castration-resistant prostate cancer; AR-V7 antagonists; niclosamide androgen receptor; androgen receptor splice variant 7; castration-resistant prostate cancer; AR-V7 antagonists; niclosamide
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MDPI and ACS Style

Sobhani, N.; Neeli, P.K.; D’Angelo, A.; Pittacolo, M.; Sirico, M.; Galli, I.C.; Roviello, G.; Nesi, G. AR-V7 in Metastatic Prostate Cancer: A Strategy beyond Redemption. Int. J. Mol. Sci. 2021, 22, 5515. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22115515

AMA Style

Sobhani N, Neeli PK, D’Angelo A, Pittacolo M, Sirico M, Galli IC, Roviello G, Nesi G. AR-V7 in Metastatic Prostate Cancer: A Strategy beyond Redemption. International Journal of Molecular Sciences. 2021; 22(11):5515. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22115515

Chicago/Turabian Style

Sobhani, Navid, Praveen K. Neeli, Alberto D’Angelo, Matteo Pittacolo, Marianna Sirico, Ilaria C. Galli, Giandomenico Roviello, and Gabriella Nesi. 2021. "AR-V7 in Metastatic Prostate Cancer: A Strategy beyond Redemption" International Journal of Molecular Sciences 22, no. 11: 5515. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22115515

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