BioCentury
ARTICLE | Distillery Therapeutics

Cancer

September 26, 2018 5:33 PM UTC

In vitro and mouse studies identified an amiloride-based PLAU inhibitor that could help treat metastatic fibrosarcoma and pancreatic cancers. Chemical synthesis and in vitro testing of amiloride analogs in enzyme activity assays yielded two compounds that inhibited PLAU with Ki values of 53 and 183 nM. In a mouse model of metastatic fibrosarcoma, the compounds decreased metastasis to the lung compared with vehicle. In a xenograft mouse model of metastatic pancreatic cancer, the two compounds decreased tumor volume and one of the compounds decreased metastasis to the liver. Next steps could include optimizing and testing the compounds in the models...