Malaria parasites die when a chemical compound jams a specific enzyme that they need to survive inside human blood cells and inside mosquitoes. This matters because malaria still infects hundreds of millions of people every year, and the parasites are becoming resistant to existing drugs. The enzyme, called N-myristoyl transferase, is essential for the parasite’s growth and transmission. The research team has already found compounds that block this enzyme and kill the parasite. Now they need to make those compounds more effective. The project will search for entirely new compounds that hit the same target, and will also tweak the shape and size of existing compounds to improve their ability to stop the enzyme. To guide these improvements, the team will determine the enzyme’s three-dimensional structure and test whether the compounds can actually enter the parasite cell. If this succeeds, one or more of the improved compounds could become the basis for a drug development programme in partnership with the pharmaceutical industry. The goal is a new class of antimalarial drugs that work by a mechanism different from current treatments, potentially bypassing existing resistance.
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There is a need to develop new drugs to treat malaria, which is one of the most important global infectious diseases, afflicting hundreds of millions of people each year. We have identified a way to kill the parasite causing malaria using chemical compounds that stop the action of a parasite enzyme that has an important role in allowing the parasite to grow in the blood stream and in passing from one individual to another through the mosquito. What we now plan to do is to make new compounds that are even more effective at killing the parasite so that they can form the basis of the development of new drugs against malaria. To make such improvements we will both look for completely new chemical compounds that work in the same way, and make small changes in the size and shape of the compounds we already have to improve their ability to stop the enzyme from working. To do this improvement work most effectively we need to know the shape and structure of the enzyme and whether or not the compounds can get into the parasite cell to kill it. By understanding how stopping the action of the enzyme kills the parasite we can use the knowledge to develop better ways of testing these potential therapeutics against the parasite in the test tube and within the blood stream. The goal of the project is therefore to confirm that new and better chemical compounds can be developed that are more effective in stopping the action of this enzyme and therefore in killing the parasite that causes malaria. One or more of these compounds may form the basis of a further programme in collaboration with pharmaceutical industry to develop therapeutic drugs.
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