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Therapeutic resistance

Two steps ahead

Nature Reviews Cancer volume 13, page 383 (2013)Cite this article

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this mutation converts enzalutamide from an AR antagonist to an AR agonist

Using a mixed population of wild-type LNCaP prostate cancer cells and LNCaP cells expressing a known resistance mutant (W741C) to another AR antagonist, bicalutamide, and sorting for cells that reactivated AR transcription (assessed by an AR-regulated enhanced green fluorescent protein (EGFP) reporter), the authors showed that the resistance mutant is selected for following several rounds of bicalutamide treatment. Following this proof-of-concept study, they carried out a screen for mutants of AR that could reactivate AR-dependent transcription following enzalu-tamide treatment using a randomly generated library of AR mutants. From this, they identified the AR mutant F876L, which was enriched in two of three replicates.

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ORIGINAL RESEARCH PAPER

  1. Balbas, M. D. et al. Overcoming mutation-based resistance to antiandrogens with rational drug design. eLife 9 Apr 2013 (doi:10.7554/eLife.00499)

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Authors
  1. Sarah Seton-Rogers
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Seton-Rogers, S. Two steps ahead. Nat Rev Cancer 13, 383 (2013). https://doi.org/10.1038/nrc3532

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