Dysregulated androgen receptor (AR) signalling is a hallmark of advanced prostate cancer. This study showed that disrupting an interaction between the AR and a co-regulator protein could be beneficial. The authors structurally designed a peptidomimetic that disrupted the interaction between the scaffold protein PELP1 (proline-, glutamic acid- and leucine-rich protein 1) and the AR by targeting the LXXLLL motif. In cells, the compound prevented nuclear translocation of the AR and inhibited androgen-induced proliferation, and it inhibited tumour growth in a mouse xenograft model of prostate cancer.
References
Ravindranathan, P. et al. Peptidomimetic targeting of critical androgen receptor–coregulator interactions in prostate cancer. Nature Comm. 4, 1923 (2013)
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Charlotte, H. Targeting receptor–regulator interactions. Nat Rev Drug Discov 12, 580 (2013). https://doi.org/10.1038/nrd4092
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DOI: https://doi.org/10.1038/nrd4092