Ar splicing variants and resistance to ar targeting agents

Mayuko Kanayama, Changxue Lu, Jun Luo, Emmanuel S. Antonarakis

Research output: Contribution to journalReview articlepeer-review

26 Scopus citations


Over the past decade, advances in prostate cancer research have led to discovery and development of novel biomarkers and effective treatments. As treatment options diversify, it is critical to further develop and use optimal biomarkers for the purpose of maximizing treatment benefit and minimizing unwanted adverse effects. Because most treatments for prostate cancer target androgen receptor (AR) signaling, aberrations affecting this drug target are likely to emerge following the development of castration-resistant prostate cancer (CRPC), and it is conceivable that such aberrations may play a role in drug resistance. Among the many AR aberrations, we and others have been studying androgen receptor splice variants (AR-Vs), especially AR-V7, and have conducted preclinical and clinical studies to develop and validate the clinical utility of AR-V7 as a prognostic and potential predictive biomarker. In this review, we first describe mechanisms of AR-V generation, regulation and their functions from a molecular perspective. We then discuss AR-Vs from a clinical perspective, focusing on the significance of AR-Vs detected in different types of human specimens and AR-Vs as potential therapeutic targets.

Original languageEnglish (US)
Article number2563
Issue number11
StatePublished - Jun 1 2021
Externally publishedYes

Bibliographical note

Funding Information:
E.S. Antonarakis is partially funded by NIH grants P30 CA006973 and R01 CA238384.

Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.


  • AR-V7
  • Androgen receptor splice variants
  • Castration-resistant prostate cancer
  • Circulating tumor cells


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