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April 19, 2026Cancer Research0 citations

TAU-1-Directed Androgen Receptor Degrader Targets AR and AR-V7 in Prostate Cancer

Abstract LB346: A first-in-class TAU-1-directed androgen receptor (AR) and AR-V7 degrader recruits DDB1-CUL4-RBX1 E3 ligase to eliminate AR signaling in lethal prostate cancer

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Authors

MNMichelle NaidooCACherie AuKSKiran K. Sahu

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Overview

Demonstrates a novel degradation strategy for AR and AR-V7 in lethal prostate cancer, indicating potential treatment advances.

Key Points

  • The aim is to develop a first-in-class degrader for androgen receptor (AR) and AR-V7 to address treatment resistance in metastatic castration-resistant prostate cancer.
  • Performed high-throughput screening of ~170,000 compounds to identify potential degraders.
  • Conducted structure-activity relationship studies to optimize compound #15 efficacy.
  • Utilized CRISPR-Cas9 to identify E3 ligases involved in degrading AR and AR-V7.
  • Compound #15 selectively degraded both AR and AR-V7 within 3 hours.
  • Degradation was shown to require the DDB1-CUL4-RBX1 E3 ligase complex.
  • TAU-1 was established as a novel target for inducing AR degradation.

Cite This Study

Naidoo et al. (2026) studied this question.

synapsesocial.com/papers/69e4745f010ef96374d902b3https://doi.org/10.1158/1538-7445.am2026-lb346
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Abstract 1231: First-in-class AR-V7/AR-fl small molecule molecular glue degrader for prostate cancer treatment2024 · 1 citations
  2. 2Abstract NG10: First-in-class dual AR/AR-V7 molecular glue degraders targeting the undruggable N-terminal domain to overcome therapeutic resistance in prostate cancer2026
  3. 3Abstract 6059: Discovery of ETS-007, a first-in-class degrader targeting N-terminal domain of androgen receptor derived from AR liquid-liquid phase separation inhibitor2024 · 1 citations
  4. 4Abstract 4601: Rational design of potent androgen receptor degraders via AI-assisted molecular modeling and validation of anti-tumor efficacy in prostate cancer2026
  5. 5Abstract 6071: Identification of a molecular glue degrader targeting the full-length AR and AR-V7 splice variant2024