In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen
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DOI：
10.1073/pnas.0802982105
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发表时间：
2008-07-01
影响因子：
11.1
通讯作者：
Winzeler, Elizabeth A.
中科院分区：
文献类型：
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作者：
Plouffe, David;Brinker, Achim;Winzeler, Elizabeth A.
对目前一线抗疟药物的抗药性日益增加，是一项重大的健康挑战。为了促进新的抗疟药物的发现，我们已经实施了一种基于红细胞中恶性疟原虫（Pf）增殖的高效和稳健的高通量基于细胞的筛选（1，536孔格式）。从大约170万种化合物的筛选中，我们鉴定了大约6,000种小分子的多样化集合，这些小分子由>530种不同的支架组成，所有这些都显示出有效的抗疟疾活性（
The growing resistance to current first-line antimalarial drugs represents a major health challenge. To facilitate the discovery of new antimalarials, we have implemented an efficient and robust high-throughput cell-based screen (1,536-well format) based on proliferation of Plasmodium falciparum (Pf) in erythrocytes. From a screen of approximate to 1.7 million compounds, we identified a diverse collection of approximate to 6,000 small molecules comprised of >530 distinct scaffolds, all of which show potent antimalarial activity (