Scientists at the University of Oulu, Finland, and at the Helmholtz Center Berlin (HZB) have shown the way to new directions in drug development against African sleeping sickness and other tropical parasitic infections. This was based on the structural analysis of the enzyme thiolase, which plays a central role in lipid metabolism in the parasite that causes sleeping sickness. The researchers examined the biomolecule’s structure at the MX beamline of the electron storage ring, BESSY II, at the HZB. The results were published online on August 2, 2013 in the Biochemical Journal. Sleeping sicknesses – african trypanosomiasis, kala-azar, indian leishmaniasis – are infections caused by tropical parasites. Millions get sick from them each year and thousands end up dying. Anti-parasitic drugs are expensive and often have a host of unwanted side effects. In decades, there have been no new effective therapies. This is reason enough for the World Health Organization (WHO) to consider research, which can lead to the development of new anti-parasitic drugs, a top priority. Now, Professor Rik Wierenga and his team at Oulu University have paved the way for this type of research by shedding light on the structure of the enzyme thiolase. Thiolase figures prominently in parasitic lipid metabolism. According to Dr. Wierenga, “key is knowing the geometry of the enzyme’s active site. This is the place where lipids that play a central role in parasitic metabolism attach and where chemical reactions that convert lipids into other substances take place.” This is why it’s important to investigate the active site’s structure and function: “It enables us to develop lipid-like substances that firmly attach to the active site and block it.” The molecules that are involved represent the ideal starting points for new drug development.
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