Global Phenotypic Screening for Antimalarials

被引:103
作者
Guiguemde, W. Armand [1 ]
Shelat, Anang A. [1 ]
Garcia-Bustos, Jose F. [2 ]
Diagana, Thierry T. [3 ]
Gamo, Francisco-Javier [4 ]
Guy, R. Kiplin [1 ]
机构
[1] St Jude Childrens Res Hosp, Dept Chem Biol & Therapeut, Memphis, TN 38105 USA
[2] Univ Otago, Dept Biochem, Dunedin 9054, New Zealand
[3] Novartis Inst Trop Dis, Drug Discovery Unit, Singapore 138670, Singapore
[4] GlaxoSmithKline, Dis Dev World, Madrid, Spain
来源
CHEMISTRY & BIOLOGY | 2012年 / 19卷 / 01期
关键词
CARRIER PROTEIN REDUCTASE; FALCIPARUM DIHYDROOROTATE DEHYDROGENASE; MITOCHONDRIAL ELECTRON-TRANSPORT; MALARIA DRUG DISCOVERY; HIGH-THROUGHPUT SCREEN; PLASMODIUM-FALCIPARUM; LACTATE-DEHYDROGENASE; ARTEMISININ RESISTANCE; STRUCTURAL GENOMICS; STARTING POINTS;
D O I
10.1016/j.chembiol.2012.01.004
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Malaria, a devastating infectious disease caused by Plasmodium spp., leads to roughly 655,000 deaths per year, mostly of African children. To compound the problem, drug resistance has emerged to all classical antimalarials and may be emerging for artemisinin-based combination therapies. To address the need for new antimalarials with novel mechanisms, several groups carried out phenotypic screening campaigns to identify compounds inhibiting growth of the blood stages of Plasmodium falciparum. In this review, we describe the characterization of these compounds, explore currently ongoing strategies to develop lead molecules, and endorse the concept of a "malaria box" of publicly accessible active compounds.
引用
收藏
页码:116 / 129
页数:14
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