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The proteasome as a target for protozoan parasites

机译：蛋白酶作为原生动物寄生虫的靶标

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ABSTRACT Introduction: The proteasome is a multi-subunit enzyme complex responsible for the turnover of shortlived, abnormal or damaged proteins in eukaryotic cells. As organisms that undergo rapid growth and cell division, protozoan parasites exist on the knife-edge of proteotoxic catastrophe and thus rely heavily on their protein quality control machinery for survival. Because of this, the proteasome has recently emerged as a desirable drug target. Area covered: This review focuses on efforts to identify protozoan parasite-specific proteasome inhibitors using substrate profiling, library screening, and in vitro evolution of resistance approaches to inform medicinal chemistry. Targeting the parasite's 20S proteasome chymotrypsin-like ((35) activity and selectively inhibiting protein turnover in parasites compared to human cells are critical properties of potent, selective inhibitors. Expert opinion: Proteasome inhibitors have the potential for rapid action against all stages, all species and all strains of plasmodium and kinetoplastid parasites. Given the high level of conservation of proteasome active sites in eukaryotes, an important challenge is achieving inhibitors that show sufficient selectivity while maintaining properties consistent with drug development.
机译：摘要介绍：蛋白酶体是一种多亚基酶复合物，其负责真核细胞中短术，异常或受损蛋白质的转口。作为经过快速生长和细胞分裂的生物，原生动物寄生虫存在于蛋白毒素灾难的刀刃上，因此依赖于他们的蛋白质质量控​​制机械的存活。因此，蛋白酶最近被赋予了理想的药物靶标。涵盖了地区：本综述致力于使用基材分析，文库筛选和抗性方法的体外演变来识别原生动物寄生虫特异性蛋白酶体抑制剂的努力。靶向寄生虫20S蛋白酶体胰蛋白酶样蛋白样（（35）活性和与人类细胞相比，寄生虫中的蛋白质转运是有效的选择性抑制剂的关键性质。专家意见：蛋白酶体抑制剂具有对所有阶段的快速行动的可能性，所有物种和所有疟原虫和酮孢子苷寄生虫的菌株。鉴于真核生物中蛋白酶体活性位点的高水平保护，重要的挑战是实现抑制剂，其表现出足够的选择性，同时保持与药物发育一致的性质。

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