A fragment-based screening approach to identify, develop, and characterise novel highly potent and efficacious inhibitors against the malaria parasite uridine diphosphate galactose transporter (UGT)

Malaria is a deadly disease that kills over 400,000 people each year and affects an estimated 229 million people worldwide. Vaccines developed against malaria do not offer full protection, and the current antimalarial drugs face the continual threat of drug resistance. Thus, there is an urgent need to discover new drugs to treat malaria. The parasite depends on a sugar moiety called uridine-diphosphate galactose (UDP-Gal) for survival. It captures this sugar from human cells by transporting it through a small door-like protein called the uridine-diphosphate galactose transporter (UGT). I aim to determine the detailed structure of UGT at a high resolution. This will enable me to identify small molecules that bind to UGT and may block UDP-Gal entry into the parasite. Closing this door will kill the parasite by depriving it of essential nutrients. Such molecules could then be developed as novel drugs against malaria.