Dr. Stephen L. Bearne, Ph.D., M.D.C.M.
Professor, Department of Biochemistry & Molecular Biology, cross-appointed to the Department of Chemistry
Dalhousie University Faculty of Medicine, Dalhousie University Faculty of Science
enzymology, enzyme inhibitor design, chemical biology, proteomics
Inhibiting Enzymes to Fight Cancer
Understanding how enzymes catalyze reactions and the precise interactions that occur between enzymes and molecules provides us with knowledge to guide drug development. The enzyme cytidine 5?-triphosphate (CTP) synthase promotes the formation of CTP and is a recognized target for anti-cancer drugs. CTP is utilized for many functions, including the manufacture of genetic material and cell membranes, especially in rapidly proliferating cells such as cancer cells. Indeed, inhibition of CTP synthase has been shown to lead to selective killing of cancer cells and augmentation of the beneficial effects of current chemotherapy drugs. Unfortunately, only one inhibitor of CTP synthase has made it to clinical trails and it exhibited toxic side effects to the heart. Dr. Bearne’s research focuses on developing new strategies to inhibit CTP synthase activity and guide future drug development.