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布氏锥虫EIF4AI翻译起始因子在类eIF4F复合物中的不同相互作用模式及对RocA抑制剂的敏感性。

Distinct modes of interaction within eIF4F-like complexes and susceptibility to the RocA inhibitor for the Trypanosoma brucei EIF4AI translation initiation factor.

作者信息

Moura Danielle M N, Soares Amanda L, da Silva Adalúcia, Ribeiro João L A B, Sunter Jack D, Assis Ludmila A, Carrington Mark, de Melo Neto Osvaldo P

机构信息

Aggeu Magalhães Institute, Oswaldo Cruz Foundation (Fiocruz), Recife, Pernambuco, Brazil.

Department of Biological and Medical Sciences, Oxford Brookes University, Oxford, United Kingdom.

出版信息

PLoS One. 2025 May 9;20(5):e0322812. doi: 10.1371/journal.pone.0322812. eCollection 2025.

Abstract

Trypanosomatids are parasitic protozoa responsible for major human diseases which are characterized by unique gene expression mechanisms. mRNA translation in these parasites is associated with multiple eIF4F-like complexes, required for mRNA recruitment and ribosome binding. The eukaryotic eIF4F is generally known to require the action of eIF4A, an ATP-dependent RNA helicase, in order to function properly, but not all trypanosomatid eIF4F complexes might require EIF4AI, their single eIF4A homologue. In mammals, eIF4A is known to be targeted by specific inhibitors and can thus be considered a potential target for a selective inhibition of translation in these parasites. Here, aiming to better define the EIF4AI functionality, we started by investigating its interactome in Trypanosoma brucei, confirming a strong interaction with only one of five eIF4F-like complexes found in trypanosomatids, based on the EIF4E4/EIF4G3 subunits. Nevertheless, when the interactome of a mutant EIF4AI (DEAD/DQAD), known to be impacted on its ATPase activity, was investigated, the only eIF4F-like complex found was based on the EIF4E3/EIF4G4 pair, with many translation-related and other proteins also found with the mutant protein. When both wild-type and mutant proteins were also investigated through a fluorescent-based tethering assay, a stimulatory effect on mRNA expression was confirmed for EIF4AI, but not for the mutant protein. Sensitivity to the Rocaglamide A (RocA) inhibitor, which targets the mammalian eIF4A, was also investigated, with the inhibitor blocking the stimulation seen on the tethering assay. Parasite susceptibility to RocA was further assessed in T. brucei and Leishmania infantum, with both, and specially T. brucei, being much less susceptible to the drug than mammalian cells. This phenotype correlates with changes in EIF4AI within the RocA binding pocket where, in comparison with the mammalian eIF4A, a phenylalanine to valine substitution in the T. brucei EIF4AI likely impairs RocA binding. Our results help better define the EIF4AI mode of action in T. brucei and provide relevant data which might support future searches for specific EIF4AI inhibitors.

摘要

锥虫是导致主要人类疾病的寄生原生动物,其特征在于独特的基因表达机制。这些寄生虫中的mRNA翻译与多种eIF4F样复合物相关,这些复合物是mRNA募集和核糖体结合所必需的。真核生物的eIF4F通常需要eIF4A(一种ATP依赖性RNA解旋酶)的作用才能正常发挥功能,但并非所有锥虫的eIF4F复合物都需要EIF4AI(它们唯一的eIF4A同源物)。在哺乳动物中,已知eIF4A会被特定抑制剂靶向,因此可被视为选择性抑制这些寄生虫翻译的潜在靶点。在此,为了更好地定义EIF4AI的功能,我们首先研究了它在布氏锥虫中的相互作用组,基于EIF4E4/EIF4G3亚基,证实它仅与锥虫中发现的五种eIF4F样复合物之一有强烈相互作用。然而,当研究已知其ATP酶活性受到影响的突变型EIF4AI(DEAD/DQAD)的相互作用组时,发现的唯一eIF4F样复合物是基于EIF4E3/EIF4G4对,同时还发现许多与翻译相关的蛋白质和其他蛋白质与突变蛋白有关。当通过基于荧光的拴系试验对野生型和突变型蛋白进行研究时,证实EIF4AI对mRNA表达有刺激作用,而突变蛋白则没有。还研究了对靶向哺乳动物eIF4A的罗卡酰胺A(RocA)抑制剂的敏感性,该抑制剂阻断了拴系试验中观察到的刺激作用。在布氏锥虫和婴儿利什曼原虫中进一步评估了寄生虫对RocA的敏感性,两者,特别是布氏锥虫,对该药物的敏感性远低于哺乳动物细胞。这种表型与RocA结合口袋内EIF4AI的变化相关,与哺乳动物的eIF4A相比,布氏锥虫EIF4AI中苯丙氨酸到缬氨酸的取代可能会损害RocA的结合。我们的结果有助于更好地定义布氏锥虫中EIF4AI的作用模式,并提供可能支持未来寻找特定EIF4AI抑制剂的相关数据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb53/12063893/aa28e977c5ed/pone.0322812.g001.jpg

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