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Prioritization of Molecular Targets for Antimalarial Drug Discovery
ACS Infectious Diseases ( IF 5.3 ) Pub Date : 2021-09-15 , DOI: 10.1021/acsinfecdis.1c00322
Barbara Forte 1 , Sabine Ottilie 2 , Andrew Plater 1 , Brice Campo 3 , Koen J Dechering 4 , Francisco Javier Gamo 5 , Daniel E Goldberg 6 , Eva S Istvan 6 , Marcus Lee 7 , Amanda K Lukens 8, 9 , Case W McNamara 10 , Jacquin C Niles 11 , John Okombo 12 , Charisse Flerida A Pasaje 11 , Miles G Siegel 13 , Dyann Wirth 8, 9 , Susan Wyllie 1 , David A Fidock 12, 14 , Beatriz Baragaña 1 , Elizabeth A Winzeler 2 , Ian H Gilbert 1
Affiliation  

There is a shift in antimalarial drug discovery from phenotypic screening toward target-based approaches, as more potential drug targets are being validated in Plasmodium species. Given the high attrition rate and high cost of drug discovery, it is important to select the targets most likely to deliver progressible drug candidates. In this paper, we describe the criteria that we consider important for selecting targets for antimalarial drug discovery. We describe the analysis of a number of drug targets in the Malaria Drug Accelerator (MalDA) pipeline, which has allowed us to prioritize targets that are ready to enter the drug discovery process. This selection process has also highlighted where additional data are required to inform target progression or deprioritization of other targets. Finally, we comment on how additional drug targets may be identified.

中文翻译:

抗疟药物发现的分子靶点的优先级

随着更多潜在的药物靶点在疟原虫中得到验证,抗疟药物发现正在从表型筛选转向基于靶点的方法物种。鉴于药物发现的高损耗率和高成本,选择最有可能提供可进展候选药物的目标非常重要。在本文中,我们描述了我们认为对于选择抗疟药物发现目标很重要的标准。我们描述了对疟疾药物加速器 (MalDA) 管道中的一些药物靶点的分析,这使我们能够优先考虑准备好进入药物发现过程的靶点。这一选择过程还强调了哪些地方需要额外的数据来告知目标进展或其他目标的优先级。最后,我们评论了如何识别其他药物靶点。
更新日期:2021-10-08
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