Researchers at The University of Texas Southwestern Medical Center (UTSMC) in Dallas, Texas, have developed a class of drugs known as peptidomimetics, which disrupt androgen receptor activity in a unique way, according to a UTSMC statement. The findings have been published online by Nature Communications.

Most men with advanced prostate cancer receive drugs that block androgen production or block the receptor at which the androgen binds, but such therapy ultimately fails, and androgen receptor signaling is still active and promoting tumor growth when the patient dies. The new agents, known as peptidomimetics, prevent prostate cancer cells from receiving the signal to proliferate even when the androgen receptor is activated.

As explained in the UTSMC statement, peptidomimetics consist of an engineered protein-like chain designed to mimic the peptides that are critical to androgen receptor function. These agents block the activity of the androgen receptor even in the presence of androgen by attacking the protein at a different site from that where the androgen binds.


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In mouse models and human-tissue models, peptidomimetics prevented androgen receptor signaling in cancer cells. In addition, these drugs were nontoxic.

“We are hopeful that this novel class of drugs will shut down androgen receptor signaling and lead to added options and increase longevity for men with advanced prostate cancer,” noted study leader and UTSMC urologist Ganesh V. Raj, MD, PhD, in the UTSMC statement.