BioCentury
ARTICLE | Distillery Therapeutics

Cancer

February 5, 2019 4:04 PM UTC

Cell culture and mouse studies identified an aryloxytetramethylcyclobutane-based degrader of androgen receptor that could help treat prostate cancer. Chemical synthesis and testing in three prostate cancer cells lines of analogs of a tool compound androgen receptor antagonist linked to a vHL ligand yielded an aryloxytetramethylcyclobutane-based compound that induced androgen receptor degradation with IC50 values of 0.25, 34 and 183 nM, respectively. In a xenograft mouse model of prostate cancer, the compound decreased androgen receptor activity in tumors compared with no treatment. Next steps by Oncopia Therapeutics LLC could include testing the compound in additional animal models of prostate cancers.

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