Inhibitor of lipid kinase PI3KC2α identified as potential new treatment of thrombosis
How can one interfere with thrombosis and cancer cell migration by small molecules?
The lipid kinase PI3KC2a is a potential pharmacological target for the treatment of thrombosis and, possibly, cancer. Work published in Nature Chemical Biology now reports highly specific inhibitors of its activity. Screening a compound library of more than 30,000 chemical compounds combined with medicinal chemistry approaches and previous work on the structure of PI3KC2a led to the identification of compounds termed PITCOINs that were highly selective toward PI3KC2a. The researchers were able to show in cells that PITCOINs impair endocytic membrane uptake and platelet aggregation and interfere with breast cancer cell spreading. The findings could open new possibilities for the treatment of thrombosis and cancer.