Foote S J, Cowman A F
Whitehead Institute for Biomedical Research, Cambridge, MA 01242.
Acta Trop. 1994 Mar;56(2-3):157-71. doi: 10.1016/0001-706x(94)90061-2.
The mechanism of action of the antifolate and quinoline antimalarials has been investigated over the last few decades, and recent advances should aid the development of new drugs to combat the increasingly refractile parasite. The molecular description of resistance to the antifolates has been well characterised and is due to structural changes in the target enzymes, but the factors involved in the parasite's ability to circumvent the action of the quinoline antimalarials have yet to be fully elucidated. This review discusses the mode of action of these drugs and the means used by the parasite to defeat our therapeutic ingenuity.
在过去几十年中，人们对抗叶酸和喹啉类抗疟药物的作用机制进行了研究，最近的进展应有助于开发新药以对抗日益耐药的疟原虫。对叶酸拮抗剂耐药性的分子描述已得到充分表征，这是由于靶酶的结构变化所致，但疟原虫规避喹啉类抗疟药物作用的相关因素尚未完全阐明。本综述讨论了这些药物的作用方式以及疟原虫战胜我们治疗策略的手段。
