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恶性疟原虫的丝氨酸蛋白酶:作为抗疟药物靶点的潜力

Serine Proteases of Malaria Parasite Plasmodium falciparum: Potential as Antimalarial Drug Targets.

作者信息

Alam Asrar

机构信息

Department of Biological Sciences, Tata Institute of Fundamental Research, Homi Bhabha Road, Colaba, Mumbai 400005, India.

出版信息

Interdiscip Perspect Infect Dis. 2014;2014:453186. doi: 10.1155/2014/453186. Epub 2014 Mar 11.

DOI:10.1155/2014/453186
PMID:24799897
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3988940/
Abstract

Malaria is a major global parasitic disease and a cause of enormous mortality and morbidity. Widespread drug resistance against currently available antimalarials warrants the identification of novel drug targets and development of new drugs. Malarial proteases are a group of molecules that serve as potential drug targets because of their essentiality for parasite life cycle stages and feasibility of designing specific inhibitors against them. Proteases belonging to various mechanistic classes are found in P. falciparum, of which serine proteases are of particular interest due to their involvement in parasite-specific processes of egress and invasion. In P. falciparum, a number of serine proteases belonging to chymotrypsin, subtilisin, and rhomboid clans are found. This review focuses on the potential of P. falciparum serine proteases as antimalarial drug targets.

摘要

疟疾是一种主要的全球寄生虫病,是造成巨大死亡率和发病率的原因。对目前可用抗疟药的广泛耐药性使得有必要识别新的药物靶点并开发新药。疟疾蛋白酶是一类分子,由于它们对寄生虫生命周期各阶段至关重要,且设计针对它们的特异性抑制剂具有可行性,因此可作为潜在的药物靶点。恶性疟原虫中存在属于各种机制类别的蛋白酶,其中丝氨酸蛋白酶因其参与寄生虫特有的逸出和入侵过程而特别受关注。在恶性疟原虫中,发现了许多属于胰凝乳蛋白酶、枯草杆菌蛋白酶和类菱形蛋白酶家族的丝氨酸蛋白酶。本综述重点关注恶性疟原虫丝氨酸蛋白酶作为抗疟药物靶点的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2fab/3988940/18e6665c9514/IPID2014-453186.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2fab/3988940/18e6665c9514/IPID2014-453186.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2fab/3988940/18e6665c9514/IPID2014-453186.001.jpg

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