Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance
Open accessAbstract
The androgen receptor is a major driver of prostate cancer and inhibition of its transcriptional activity using competitive antagonists, such as enzalutamide remains a frontline therapy for prostate cancer management. However, the majority of patients eventually develop drug resistance. We propose that targeting the androgen receptor for degradation via Proteolysis Targeting Chimeras (PROTACs) will be a better therapeutic strategy for targeting androgen receptor signaling in prostate cancer cells. Here we perform a head-to-head comparison between a currently approved androgen receptor antagonist enzalutamide, and its PROTAC derivative, ARCC-4, across different cellular models of prostate cancer drug resistance. ARCC-4 is a low-nanomolar androgen receptor degrader able to degrade about 95% of cellular androgen receptors. ARCC-4 inhibits prostate tumor cell proliferation, degrades clinically relevant androgen receptor point mutants and unlike enzalutamide, retains antiproliferative effect in a high androgen environment. Thus, ARCC-4 exemplifies how protein degradation can address the drug resistance hurdles of enzalutamide.
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The ER in breast cancer and the AR in prostate cancer are the leading examples of targets with well-characterized biological and biochemical properties, clinically validated roles in disease, and previously established clinical efficacy for their inhibition.
“The ER in breast cancer38,39 and the AR in prostate cancer33 are the leading examples of such targets.”
From PROTAC targeted protein degraders: the past is prologue (2022) · cites this paper as [33]
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- Authors
- Salami, J., Alabi, S., Willard, R. R., Vitale, N. J., Wang, J., Dong, H., Jin, M., McDonnell, D. P., Crew, A. P., Neklesa, T. K., & Crews, C. M.
- Affiliations
- Yale University (US)
- Arvinas (United States) (US)
- Duke University (US)
- Corresponding author
- Crews, Craig M.
- ORCID
- Venue
- Communications Biology
- Published
- 2018-08-02
- Volume
- 1
- Issue
- 1
- Pages
- 100-100
- ISSN
- 2399-3642 (ISSN-L)
- PMC
- PMC6123676
- OpenAlex
- W2883077013
- Cited by
- 349
- References
- 54
- Citations by year
- 2026: 20 · 2025: 37 · 2024: 40 · 2023: 43 · 2022: 68 · 2021: 55 · 2020: 49 · 2019: 30 · 2018: 5
- FWCI
- 12.54
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Locations
- Communications Biology (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion)
- Funders
- U.S. Department of Health & Human Services | NIH | National Cancer Institute (SBIR 1R44CA203199, R35 CA197589)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Diagnosis and Treatment
- Keywords
- androgen receptor, PROTACs, enzalutamide, prostate cancer, drug resistance, androgen receptor degradation, androgen receptor antagonists, tumor cell proliferation
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