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本文引用的文献

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Extracting SAR Information from a Large Collection of Anti-Malarial Screening Hits by NSG-SPT Analysis.通过NSG-SPT分析从大量抗疟筛选命中物中提取SAR信息。
ACS Med Chem Lett. 2011 Jan 5;2(3):201-6. doi: 10.1021/ml100240z. eCollection 2011 Mar 10.
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β-Branched acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase.β-支链无环核苷类似物作为恶性疟原虫 dUTP 酶的抑制剂。
Bioorg Med Chem. 2011 Apr 1;19(7):2378-91. doi: 10.1016/j.bmc.2011.02.012. Epub 2011 Feb 17.
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Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.利用新型微型高通量基于荧光素酶的检测法发现有效的抗多药耐药恶性疟原虫的小分子抑制剂。
Antimicrob Agents Chemother. 2010 Sep;54(9):3597-604. doi: 10.1128/AAC.00431-10. Epub 2010 Jun 14.
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Chemical genetics of Plasmodium falciparum.恶性疟原虫的化学遗传学
Nature. 2010 May 20;465(7296):311-5. doi: 10.1038/nature09099.
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Thousands of chemical starting points for antimalarial lead identification.数以千计的抗疟药物先导化合物化学起始点。
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The pathophysiology of vivax malaria.间日疟的病理生理学。
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In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.计算机模拟活性谱分析揭示了在高通量筛选中发现的抗疟药物的作用机制。
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Drugging the Plasmodium kinome: the benefits of academia-industry synergy.靶向疟原虫激酶组：学术界与产业界协同合作的益处。
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The influence of drug-like concepts on decision-making in medicinal chemistry.类药概念对药物化学决策的影响。
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疟疾药物研发中的开放式创新邀请：来自TCAMS的47个优质起点

An Invitation to Open Innovation in Malaria Drug Discovery: 47 Quality Starting Points from the TCAMS.

作者信息

Calderón Félix, Barros David, Bueno José María, Coterón José Miguel, Fernández Esther, Gamo Francisco Javier, Lavandera José Luís, León María Luisa, Macdonald Simon J F, Mallo Araceli, Manzano Pilar, Porras Esther, Fiandor José María, Castro Julia

机构信息

Tres Cantos Medicines Development Campus, DDW, GlaxoSmithKline , Severo Ochoa 2, 28760 Tres Cantos, Spain.

Medicines for Malaria Venture (MMV) , 20, route de Pré-Bois-PO Box 1826, 1215 Geneva 15, Switzerland.

出版信息

ACS Med Chem Lett. 2011 Aug 3;2(10):741-6. doi: 10.1021/ml200135p. eCollection 2011 Oct 13.

DOI:10.1021/ml200135p
PMID:24900261
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4018116/
Abstract

In 2010, GlaxoSmithKline published the structures of 13533 chemical starting points for antimalarial lead identification. By using an agglomerative structural clustering technique followed by computational filters such as antimalarial activity, physicochemical properties, and dissimilarity to known antimalarial structures, we have identified 47 starting points for lead optimization. Their structures are provided. We invite potential collaborators to work with us to discover new clinical candidates.

摘要

2010年，葛兰素史克公司公布了13533个用于抗疟先导化合物识别的化学起始点的结构。通过使用凝聚结构聚类技术，再结合抗疟活性、物理化学性质以及与已知抗疟结构的差异等计算筛选方法，我们确定了47个用于先导化合物优化的起始点。文中提供了它们的结构。我们邀请潜在的合作伙伴与我们共同努力，发现新的临床候选药物。