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Antimalarial drugs inhibiting hemozoin (beta-hematin) formation: a mechanistic update.

机译:抗疟疾药物抑制hezozoin(β-hematin)的形成:机械更新。

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摘要

Digestion of hemoglobin in the food vacuole of the malaria parasite produces very high quantities of redox active toxic free heme. Hemozoin (beta-hematin) formation is a unique process adopted by Plasmodium sp. to detoxify free heme. Hemozoin formation is a validated target for most of the well-known existing antimalarial drugs and considered to be a suitable target to develop new antimalarials. Here we discuss the possible mechanisms of free heme detoxification in the malaria parasite and the mechanistic details of compounds, which offer antimalarial activity by inhibiting hemozoin formation. The chemical nature of new antimalarial compounds showing antimalarial activity through the inhibition of hemozoin formation has also been incorporated, which may help to design future antimalarials with therapeutic potential against multi-drug resistant malaria.
机译:疟原虫食物液泡中的血红蛋白消化会产生大量的氧化还原活性无毒血红素。血红素(β-血红素)的形成是疟原虫sp。sp。采用的独特过程。排毒免费的血红素。血红素的形成是大多数已知的现有抗疟药的有效靶标,并且被认为是开发新抗疟药的合适靶标。在这里,我们讨论了疟原虫中游离血红素解毒的可能机制,以及化合物的机械细节,这些化合物通过抑制血zo素的形成提供抗疟疾活性。还已经纳入了新的抗疟疾化合物的化学性质,该化合物通过抑制血腥素的形成而具有抗疟疾活性,这可能有助于设计未来的抗疟疾药物,对多种药物具有抗药性。

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