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筛选策略,以鉴定用于治疗动基体感染的药物开发的新化学多样性。

Screening strategies to identify new chemical diversity for drug development to treat kinetoplastid infections.

机构信息

Drugs for Neglected Diseases initiative, 15 Chemin Louis-Dunant, 1202 Geneva, Switzerland.

出版信息

Parasitology. 2014 Jan;141(1):140-6. doi: 10.1017/S003118201300142X. Epub 2013 Aug 28.

Abstract

The Drugs for Neglected Diseases initiative (DNDi) has defined and implemented an early discovery strategy over the last few years, in fitting with its virtual R&D business model. This strategy relies on a medium- to high-throughput phenotypic assay platform to expedite the screening of compound libraries accessed through its collaborations with partners from the pharmaceutical industry. We review the pragmatic approaches used to select compound libraries for screening against kinetoplastids, taking into account screening capacity. The advantages, limitations and current achievements in identifying new quality series for further development into preclinical candidates are critically discussed, together with attractive new approaches currently under investigation.

摘要

国际药品采购机制(DNDi)在过去几年中根据其虚拟研发业务模式制定并实施了早期发现战略。该战略依赖于一种中高通量表型测定平台,以加快通过与制药行业合作伙伴合作获得的化合物库的筛选。我们回顾了用于针对动质体筛选的化合物库选择的实用方法,同时考虑了筛选能力。批判性地讨论了在确定具有进一步开发为临床前候选药物的新质量系列方面的优势、限制和当前成就,以及目前正在研究的有吸引力的新方法。

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