疟原虫蛋白酶：化疗的新靶点
Proteases of malaria parasites: new targets for chemotherapy.
作者信息
Rosenthal P J
机构信息
San Francisco, General Hospital, California, USA.
出版信息
Emerg Infect Dis. 1998 Jan-Mar;4(1):49-57. doi: 10.3201/eid0401.980107.
Abstract
The increasing resistance of malaria parasites to antimalarial drugs is a major contributor to the reemergence of the disease as a major public health problem and its spread in new locations and populations. Among potential targets for new modes of chemotherapy are malarial proteases, which appear to mediate processes within the erythrocytic malarial life cycle, including the rupture and invasion of infected erythrocytes and the degradation of hemoglobin by trophozoites. Cysteine and aspartic protease inhibitors are now under study as potential antimalarials. Lead compounds have blocked in vitro parasite development at nanomolar concentrations and cured malaria-infected mice. This review discusses available antimalarial agents and summarizes experimental results that support development of protease inhibitors as antimalarial drugs.
摘要
疟原虫对抗疟药物的耐药性不断增强，这是该疾病再度成为重大公共卫生问题并在新地区和人群中传播的主要原因之一。疟原虫蛋白酶是新化疗方法的潜在靶点，它们似乎在红细胞内疟原虫生命周期的过程中发挥介导作用，包括受感染红细胞的破裂和入侵以及滋养体对血红蛋白的降解。目前正在研究半胱氨酸和天冬氨酸蛋白酶抑制剂作为潜在的抗疟药物。先导化合物已在纳摩尔浓度下阻断体外寄生虫发育，并治愈了疟疾感染小鼠。本文综述了现有的抗疟药物，并总结了支持将蛋白酶抑制剂开发为抗疟药物的实验结果。
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本文引用的文献
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