Global S&T Development Trend Analysis Platform of Resources and Environment
DOI | 10.1126/science.aaf8675 |
A multistage antimalarial targets the plasmepsins IX and X essential for invasion and egress | |
Pino, Paco1; Caldelari, Reto2; Mukherjee, Budhaditya1; Vahokoski, Juha3; Klages, Natacha1; Maco, Bohumil1; Collins, Christine R.4; Blackman, Michael J.4,5; Kursula, Inari3,6,7; Heussler, Volker2; Brochet, Mathieu1; Soldati-Favre, Dominique1 | |
2017-10-27 | |
发表期刊 | SCIENCE |
ISSN | 0036-8075 |
EISSN | 1095-9203 |
出版年 | 2017 |
卷号 | 358期号:6362页码:522-+ |
文章类型 | Article |
语种 | 英语 |
国家 | Switzerland; Norway; England; Finland |
英文摘要 | Regulated exocytosis by secretory organelles is important for malaria parasite invasion and egress. Many parasite effector proteins, including perforins, adhesins, and proteases, are extensively proteolytically processed both pre-and postexocytosis. Here we report the multistage antiplasmodial activity of the aspartic protease inhibitor hydroxyl-ethyl-amine-based scaffold compound 49c. This scaffold inhibits the preexocytosis processing of several secreted rhoptry and microneme proteins by targeting the corresponding maturases plasmepsins IX (PMIX) and X (PMX), respectively. Conditional excision of PMIX revealed its crucial role in invasion, and recombinantly active PMIX and PMX cleave egress and invasion factors in a 49c-sensitive manner. |
领域 | 地球科学 ; 气候变化 ; 资源环境 |
收录类别 | SCI-E |
WOS记录号 | WOS:000413757500045 |
WOS关键词 | APICAL MEMBRANE ANTIGEN-1 ; MEROZOITE SURFACE PROTEIN ; PLASMODIUM-FALCIPARUM ; MALARIA PARASITE ; ERYTHROCYTE INVASION ; HOST HEPATOCYTES ; SERINE-PROTEASE ; INHIBITORS ; RELEASE ; COMPLEX |
WOS类目 | Multidisciplinary Sciences |
WOS研究方向 | Science & Technology - Other Topics |
URL | 查看原文 |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | http://119.78.100.173/C666/handle/2XK7JSWQ/197208 |
专题 | 地球科学 资源环境科学 气候变化 |
作者单位 | 1.Univ Geneva, CMU, Fac Med, Dept Microbiol & Mol Med, CH-1211 Geneva, Switzerland; 2.Univ Bern, Inst Cell Biol, CH-3012 Bern, Switzerland; 3.Univ Bergen, Dept Biomed, Jonas Lies Vei 91, N-5009 Bergen, Norway; 4.Francis Crick Inst, Malaria Biochem Lab, Mill Hill, London NW1 1AT, England; 5.London Sch Hyg & Trop Med, Dept Pathogen Mol Biol, London WC1E 7HT, England; 6.Univ Oulu, Bioctr Oulu, Aapistie 7, SF-90220 Oulu, Finland; 7.Univ Oulu, Fac Biochem & Mol Med, Aapistie 7, SF-90220 Oulu, Finland |
推荐引用方式 GB/T 7714 | Pino, Paco,Caldelari, Reto,Mukherjee, Budhaditya,et al. A multistage antimalarial targets the plasmepsins IX and X essential for invasion and egress[J]. SCIENCE,2017,358(6362):522-+. |
APA | Pino, Paco.,Caldelari, Reto.,Mukherjee, Budhaditya.,Vahokoski, Juha.,Klages, Natacha.,...&Soldati-Favre, Dominique.(2017).A multistage antimalarial targets the plasmepsins IX and X essential for invasion and egress.SCIENCE,358(6362),522-+. |
MLA | Pino, Paco,et al."A multistage antimalarial targets the plasmepsins IX and X essential for invasion and egress".SCIENCE 358.6362(2017):522-+. |
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