Broadened ligand responsiveness of androgen receptor mutants obtained by random amino acid substitution of H874 and mutation hot spot T877 in prostate cancer.

@article{Steketee2002BroadenedLR,
  title={Broadened ligand responsiveness of androgen receptor mutants obtained by random amino acid substitution of H874 and mutation hot spot T877 in prostate cancer.},
  author={Karine Steketee and Leon Timmerman and Angelique C. J. Ziel-van der Made and Paul Doesburg and Albert O. Brinkmann and Jan Trapman},
  journal={International journal of cancer},
  year={2002},
  volume={100 3},
  pages={309-17}
}
In a subset of endocrine therapy-resistant prostate cancers, amino acid substitutions H874Y, T877A and T877S, which broaden ligand specificity of the ligand binding domain (LBD) of the androgen receptor (AR), have been detected. To increase our knowledge of the role of amino acid substitutions at these specific positions in prostate cancer, codons 874 and 877 were subjected to random mutagenesis. AR mutants were screened in a yeast readout system for responsiveness to 5 alpha… CONTINUE READING

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