Novel, dual-targeted small molecule inhibitor of PKC and Aurora A kinase against cancer
A small molecule inhibitor of protein kinase c and aurora a kinase in cancer models has been produced at McGill University.
In cancer progression, tumors alter a number of cellular functions such as mobility, cell death, and proliferation. Two proteins that are commonly associated with some of these cellular pathways in tumor progression are aurora A kinase and protein kinase C. Aurora A kinase controls cell cycle progression and mitosis by interacting with different proteins. Protein kinase C regulates multiple features of tumor growth, including proliferation, survival, differentiation, and motility. Since even combination therapy often develops drug resistance, there is a great need for an inhibitor that targets multiple pathways.
This technology is a small molecule inhibitor that is able to selectively target both Protein kinase C and Aurora A kinase in low nanomolar ranges. In pre-clinical studies, this inhibitor was found to have broad in vitro anti-proliferative and anti-invasive activities in human and mouse cancer models. These orally available molecules have proven effective in breast, pancreatic, and renal cancer models. Based on genome-wide profiling studies and functional assays, this drug has also been shown to have a unique mechanism affecting cancer cell differentiation.
- Molecules are oral therapeutic agents
- Target 2 common metastatic kinases
- Could be good for combination therapy since it has a unique mechanism affecting cancer cell differentiation