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蛋白酶抑制：防治传染病的成熟策略。

Protease Inhibition-An Established Strategy to Combat Infectious Diseases.

机构信息

Biology Centre, Institute of Parasitology, Academy of Sciences of the Czech Republic, Branišovská 1160/31, CZ-37005 České Budějovice, Czech Republic.

Faculty of Science, University of South Bohemia in České Budějovice, Branišovská 1760c, CZ-37005 České Budějovice, Czech Republic.

出版信息

Int J Mol Sci. 2021 May 28;22(11):5762. doi: 10.3390/ijms22115762.

DOI:10.3390/ijms22115762
PMID:34071206
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8197795/
Abstract

Therapeutic agents with novel mechanisms of action are urgently needed to counter the emergence of drug-resistant infections. Several decades of research into proteases of disease agents have revealed enzymes well suited for target-based drug development. Among them are the three recently validated proteolytic targets: proteasomes of the malarial parasite aspartyl proteases of (plasmepsins) and the Sars-CoV-2 viral proteases. Despite some unfulfilled expectations over previous decades, the three reviewed targets clearly demonstrate that selective protease inhibitors provide effective therapeutic solutions for the two most impacting infectious diseases nowadays-malaria and COVID-19.

摘要

急需具有新型作用机制的治疗药物来应对耐药性感染的出现。几十年来对疾病因子蛋白酶的研究揭示了非常适合基于靶标的药物开发的酶。其中包括最近验证的三个蛋白水解靶标：疟原虫的蛋白酶体、（疟原虫的天冬氨酸蛋白酶）和 SARS-CoV-2 病毒蛋白酶。尽管过去几十年的一些期望没有得到满足，但这三个被审查的靶标清楚地表明，选择性蛋白酶抑制剂为当今两个最具影响力的传染病（疟疾和 COVID-19）提供了有效的治疗解决方案。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b86a/8197795/db29f61f584a/ijms-22-05762-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b86a/8197795/1d76157f8061/ijms-22-05762-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b86a/8197795/1474b27fb26b/ijms-22-05762-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b86a/8197795/db29f61f584a/ijms-22-05762-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b86a/8197795/1d76157f8061/ijms-22-05762-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b86a/8197795/1474b27fb26b/ijms-22-05762-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b86a/8197795/db29f61f584a/ijms-22-05762-g003.jpg

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