Peptidomimetic targeting of critical androgen receptor-coregulator interactions in prostate cancer.

@article{Ravindranathan2013PeptidomimeticTO,
  title={Peptidomimetic targeting of critical androgen receptor-coregulator interactions in prostate cancer.},
  author={Preethi Ravindranathan and T-c. Lee and Lin Yang and Margaret Mary Centenera and Lisa Mathis Butler and Wayne D Tilley and Jer-Tsong Hsieh and Jung Mo Ahn and Ganesh Venkataram Raj},
  journal={Nature communications},
  year={2013},
  volume={4},
  pages={
          1923
        }
}
The growth of advanced prostate cancer depends on androgen receptor signalling, however treatment options are limited. Here we report the disruption of specific protein-protein interactions involving LXXLL motifs in androgen receptor-coregulator proteins such as PELP1 using a novel, small molecule peptidomimetic (D2). D2 is stable, non-toxic and efficiently taken up by prostate cancer cells. Importantly, D2 blocks androgen-induced nuclear uptake and genomic activity of the androgen receptor… CONTINUE READING
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