摘要
疟疾是一种具有破坏性的人类寄生虫病,由于对传统药物耐药性的出现,疟疾又得到了更为广泛的关注。因此,寻找新的分子靶点是一个主要的目标。PfAM 是一种由William H. Welch1897年从恶性疟原虫中发现的氨肽酶,归属于金属蛋白酶M1家族, 这是一个有前途的阻挡疟原虫红细胞内期的抑制剂靶点。从1998年它被鉴别开始,人们做了很多努力来验证PfAM1作为一个合适的抗疟药物的靶标。目前的工作是对PfAM1的主要结构,功能和动力学特征的一个关键性的概述,也是关键的抑制剂在分子和细胞水平上作用的一个总结。实验结果的系统化应该有助于更好的理解PfAM1作为抗疟药物靶点的属性,并促进集中于PfAM1抑制剂发展的研究项目。
关键词: 抗疟疾药,生长抑制,M1家族,金属氨肽酶,恶性疟原虫,蛋白酶抑制剂
Current Drug Targets
Title:Plasmodium falciparum M1-Aminopeptidase: A Promising Target for the Development of Antimalarials
Volume: 15 Issue: 12
Author(s): Jorge Gonzalez-Bacerio, Rafael Fando, Alberto del Monte-Martinez, Jean-Louis Charli and Maria de los A. Chavez
Affiliation:
关键词: 抗疟疾药,生长抑制,M1家族,金属氨肽酶,恶性疟原虫,蛋白酶抑制剂
摘要: Malaria is a devastating human parasitic disease that receives enhanced attention due to the emergence of resistance to traditional drugs. Thus, the search for new molecular targets is a major goal. PfAM1 is an aminopeptidase from Plasmodium falciparum, William H. Welch 1897, belonging to the M1 family of metalloproteases, which is a promising target of inhibitors to block the intra-erythrocytic stages of the parasite. Since its identification in 1998, many efforts have been done to validate PfAM1 as an appropriate target of antimalarials. The present work is a critical review of the main structural, functional and kinetic characteristics of PfAM1, as well as a summary of the effects of key inhibitors at molecular and cellular levels. The systematization of experimental results should contribute to a better understanding of the properties of PfAM1 as a target of antimalarials and promote research projects focused on the development of PfAM1 inhibitors.
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Gonzalez-Bacerio Jorge, Fando Rafael, Monte-Martinez del Alberto, Charli Jean-Louis and Chavez de los A. Maria, Plasmodium falciparum M1-Aminopeptidase: A Promising Target for the Development of Antimalarials, Current Drug Targets 2014; 15 (12) . https://dx.doi.org/10.2174/1389450115666141024115641
DOI https://dx.doi.org/10.2174/1389450115666141024115641 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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