Trypanocidal drugs targeting PFK and PYK

点击翻译按钮获取中文摘要

Protozoan parasites are the cause of serious diseases of the developing world where literally millions of people are at risk and tens of thousands die annually. Current treatments are poor and use very toxic drugs. The parasites have a rather unique biochemical pathway for metabolising sugar. We have characterised two proteins involved in this pathway and have used this information to design and synthesise libraries of drug-like molecules that block the pathway. Our initial trials also show that some of these compounds kill the parasite and show specificity against the parasite compared to mammalian cells. These results provide an excellent starting point for developing more potent and specific molecular families that can be tested as potential drugs. Our approach will lead to two complementary drug families that may provide the basis of a combination therapy that would not only be more potent, but also minimise the risk of the development of resistance in the parasite population.