N-Myristoyl Transferase as a drug target for anti-malarial therapy

疟疾是全球最重要的传染病之一，每年折磨着数亿人，因此有必要开发新的药物来治疗疟疾。我们已经找到了一种杀死导致疟疾的寄生虫的方法，使用化合物来阻止寄生虫酶的作用，这种酶在允许寄生虫在血液中生长并通过蚊子从一个人传播到另一个人方面发挥着重要作用。我们现在计划做的是制造新的化合物，更有效地杀死寄生虫，这样它们就可以成为开发抗疟疾新药的基础。为了实现这种改进，我们将寻找以同样方式起作用的全新化合物，并对我们已经拥有的化合物的大小和形状进行微小的改变，以提高它们阻止酶工作的能力。为了最有效地进行这项改进工作，我们需要知道酶的形状和结构，以及这些化合物是否能进入寄生虫细胞杀死它。通过了解停止酶的作用是如何杀死寄生虫的，我们可以利用这些知识开发更好的方法，在试管和血液中测试这些潜在的治疗方法。因此，该项目的目标是确认可以开发出新的、更好的化合物，更有效地阻止这种酶的作用，从而杀死导致疟疾的寄生虫。这些化合物中的一种或多种可能构成与制药工业合作开发治疗药物的进一步计划的基础。

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.