BioCentury
ARTICLE | Distillery Therapeutics

Cancer

April 25, 2017 3:56 PM UTC

In vitro, cell culture and mouse studies suggest a guanidine-based inhibitor of the σ-1 receptor could help treat prostate cancer. Chemical synthesis and in vitro testing yielded a guanidine analog compound that bound the σ-1 receptor with a Ki of 38 nM. In a human prostate cancer cell line, the compound decreased androgen receptor levels and androgen receptor-induced gene expression compared with vehicle. In a xenograft mouse model of castration-resistant prostate cancer (CRPC), the compound decreased tumor growth compared with vehicle. Next steps by Context Therapeutics include developing a version of the compound to advance to clinical testing...

BCIQ Target Profiles

Sigma-1 receptor