A multistage antimalarial targets the plasmepsins IX and X essential for invasion and egress

doi:10.1126/science.aaf8675

GSTDTAP > 地球科学

DOI	10.1126/science.aaf8675
	A multistage antimalarial targets the plasmepsins IX and X essential for invasion and egress
	Pino, Paco 1; Caldelari, Reto 2; Mukherjee, Budhaditya 1; Vahokoski, Juha 3; Klages, Natacha 1; Maco, Bohumil 1; Collins, Christine R.4; Blackman, Michael J.4,5; Kursula, Inari 3,6,7; Heussler, Volker 2; Brochet, Mathieu 1; Soldati-Favre, Dominique 1
	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
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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-+.