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受体介导的内吞作用在非洲锥虫药物传递中的应用:实现保罗·埃尔利希的化疗愿景。

Receptor-mediated endocytosis for drug delivery in African trypanosomes: fulfilling Paul Ehrlich's vision of chemotherapy.

机构信息

Department of Pathogen Molecular Biology, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK.

出版信息

Trends Parasitol. 2013 May;29(5):207-12. doi: 10.1016/j.pt.2013.03.004. Epub 2013 Apr 17.

DOI:10.1016/j.pt.2013.03.004
PMID:23601931
Abstract

Bloodstream-form cells of Trypanosoma brucei exhibit massively increased endocytic activity relative to the insect midgut stage, enabling rapid recycling of variant surface glycoprotein and antibody clearance from the surface. In addition, recent advances have identified a role for receptor-mediated endocytosis in the uptake of the antitrypanosomal drug, suramin, via invariant surface glycoprotein 75, and in the uptake of trypanosome lytic factor 1 via haptoglobin-haemoglobin receptor. Here, we argue that receptor-mediated endocytosis represents both a validated drug target and a promising route for the delivery of novel therapeutics into trypanosomes.

摘要

bloodstream-form 细胞的布氏锥虫表现出相对于昆虫中肠阶段大大增加的内吞活性,使变体表面糖蛋白快速回收和抗体从表面清除。此外,最近的进展确定了受体介导的内吞作用在摄取抗锥虫药物苏拉明中的作用,通过不变表面糖蛋白 75 摄取,以及通过触珠蛋白-血红蛋白受体摄取锥虫溶解因子 1。在这里,我们认为受体介导的内吞作用不仅代表了一个经过验证的药物靶点,也是将新型治疗药物输送到锥虫中的有前途的途径。

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