Cited by 643Prostate Cancer Treatment and ResearchChromatin Remodeling and CancerHormonal and reproductive studies

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Constitutively active androgen receptor splice variants expressed in castration-resistant prostate cancer require full-length androgen receptor.

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Watson, Philip A., Chen, Yinan F., Balbas, Minna D., Wongvipat, John, Socci, Nicholas D., Viale, Agnes, Kim, Kwanghee, Sawyers, Charles L.·2010·Proceedings of the National Academy of Sciences

DOI 10.1073/pnas.1012443107PMC PMC2947883

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Abstract

Androgen receptor (AR) splice variants lacking the ligand binding domain (ARVs), originally isolated from prostate cancer cell lines derived from a single patient, are detected in normal and malignant human prostate tissue, with the highest levels observed in late stage, castration-resistant prostate cancer. The most studied variant (called AR-V7 or AR3) activates AR reporter genes in the absence of ligand and therefore, could play a role in castration resistance. To explore the range of potential ARVs, we screened additional human and murine prostate cancer models using conventional and next generation sequencing technologies and detected several structurally diverse AR isoforms. Some, like AR-V7/AR3, display gain of function, whereas others have dominant interfering activity. We also find that ARV expression increases acutely in response to androgen withdrawal, is suppressed by testosterone, and in some models, is coupled to full-length AR (AR-FL) mRNA production. As expected, constitutively active, ligand-independent ARVs such as AR-V7/AR3 are sufficient to confer anchorage-independent (in vitro) and castration-resistant (in vivo) growth. Surprisingly, this growth is blocked by ligand binding domain-targeted antiandrogens, such as MDV3100, or by selective siRNA silencing of AR-FL, indicating that the growth-promoting effects of ARVs are mediated through AR-FL. These data indicate that the increase in ARV expression in castrate-resistant prostate cancer is an acute response to castration rather than clonal expansion of castration or antiandrogen-resistant cells expressing gain of function ARVs, and furthermore, they provide a strategy to overcome ARV function in the clinic.

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Authors: Watson, P. A., Chen, Y. F., Balbas, M. D., Wongvipat, J., Socci, N. D., Viale, A., Kim, K., & Sawyers, C. L.
Affiliations: Memorial Sloan Kettering Cancer Center (US)
Human Oncology and Pathogenesis Program,
Bioinformatics Core,
University of California, Los Angeles (US)
Howard Hughes Medical Institute (US)
Corresponding author: Sawyers, Charles L.
ORCID: Watson, Philip A.
Socci, Nicholas D.
Viale, Agnes
Kim, Kwanghee
Sawyers, Charles L.
Venue: Proceedings of the National Academy of Sciences
Publisher: National Academy of Sciences
Published: 2010-09-07
Volume: 107
Issue: 39
Pages: 16759-16765
ISSN: 0027-8424 (ISSN-L)
1091-6490
DOI: 10.1073/pnas.1012443107
PMC: PMC2947883
OpenAlex: W2083926838
Cited by: 639
References: 27
Citations by year: 2026: 8 · 2025: 19 · 2024: 22 · 2023: 33 · 2022: 25 · 2021: 26 · 2020: 43 · 2019: 33 · 2018: 36 · 2017: 43 · 2016: 63 · 2015: 48 · 2014: 64 · 2013: 65 · 2012: 53
FWCI: 46.52
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: Proceedings of the National Academy of Sciences (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Funders: Howard Hughes Medical Institute
Prostate Cancer Foundation
University of Washington
National Cancer Institute
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
Keywords: androgen receptor splice variants, castration-resistant prostate cancer, AR-V7, ligand-independent receptor activation, full-length androgen receptor, androgen withdrawal, antiandrogen resistance, enzalutamide, anchorage-independent growth, siRNA knockdown, prostate cancer cell lines, androgen receptor isoforms
MeSH terms: Amino Acid Sequence, Androgens, Animals, Castration, Disease Models, Animal, Exons, Humans, Male, Molecular Sequence Data, Prostatic Neoplasms, Receptors, Androgen, RNA, Messenger, Gene Expression Regulation, Neoplastic, Alternative Splicing, Protein Structure, Tertiary, Sequence Analysis, Protein, Cell Line, Tumor, Mice, Androgen Receptor Antagonists

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Constitutively active androgen receptor splice variants expressed in castration-resistant prostate cancer require full-length androgen receptor.

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