Departamento de Bioquímica e Imunologia, Faculdade de Medicina de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, São Paulo, Brasil.
Departamento de Biologia Animal, Instituto de Biologia, Universidade de Campinas, Campinas, São Paulo, Brasil.
Parasitol Res. 2020 Jul;119(7):2159-2176. doi: 10.1007/s00436-020-06686-4. Epub 2020 May 19.
The proteasome is the key player in the cellular protein degradation machinery and is pivotal for protein homeostasis and Schistosoma mansoni (S. mansoni) survival. Our group study provides insights into proteasome inhibitors and reveals that selective schistosomiasis agents represent an interesting branch of proteasome research linked to the development of new drugs for this neglected disease. Here, we explored the phenotypic response of S. mansoni to b-AP15, a bis-benzylidine piperidone that inhibits 26S proteasome deubiquitinases (DUBs), ubiquitin-specific protease 14 (USP14), and ubiquitin carboxyl-terminal hydrolase 5 (UCHL5). b-AP15 induces a modest decrease in egg production in vitro and reduces viability, leading to the death of parasite couples. This inhibitor also induces a twofold increase in the accumulation of polyubiquitinated proteins in S. mansoni adult worms and causes tegument changes such as disintegration, wrinkling, and bubble formation, both throughout the length of the parasite and in the oral sucker. b-AP15 alters the cell organelles of adult S. mansoni worms, and we specifically observed mitochondrial alterations, which are suggestive of proteotoxic stress leading to autophagy. Taken together, these results indicate that the deubiquitinase function of the proteasome is essential for the parasite and support the hypothesis that the proteasome constitutes an interesting drug target for the treatment of schistosomiasis.
蛋白酶体是细胞蛋白降解机制的关键参与者,对蛋白质平衡和曼氏血吸虫(S. mansoni)的生存至关重要。我们的研究小组提供了蛋白酶体抑制剂的深入了解,并揭示了选择性血吸虫病药物代表了与开发这种被忽视疾病的新药相关的蛋白酶体研究的一个有趣分支。在这里,我们研究了 b-AP15 对曼氏血吸虫的表型反应,b-AP15 是一种双苄叉哌啶酮,可抑制 26S 蛋白酶体去泛素酶(DUBs)、泛素特异性蛋白酶 14(USP14)和泛素羧基末端水解酶 5(UCHL5)。b-AP15 在体外适度减少产卵并降低存活率,导致寄生虫对死亡。这种抑制剂还导致曼氏血吸虫成虫中多泛素化蛋白的积累增加两倍,并导致体被变化,如分裂、起皱和形成气泡,无论是在寄生虫的全长还是在口吸盘处。b-AP15 改变了成年 S. mansoni 蠕虫的细胞器官,我们特别观察到线粒体的改变,这表明存在蛋白质毒性应激导致自噬。总之,这些结果表明蛋白酶体的去泛素酶功能对寄生虫至关重要,并支持蛋白酶体是治疗血吸虫病的一个有趣药物靶点的假设。