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Combining experimental strategies for successful target deconvolution
Drug Discovery Today ( IF 6.5 ) Pub Date : 2020-09-21 , DOI: 10.1016/j.drudis.2020.09.016
Isabel V L Wilkinson 1 , Georg C Terstappen 2 , Angela J Russell 3
Affiliation  

Investment in phenotypic drug discovery has led to increased demand for rapid and robust target deconvolution to aid successful drug development. Although methods for target identification and mechanism of action (MoA) discovery are flourishing, they typically lead to lists of putative targets. Validating which target(s) are involved in the therapeutic mechanism of a compound poses a significant challenge, requiring direct binding, target engagement, and functional studies in relevant physiological contexts. A combination of orthogonal approaches can allow target identification beyond the proteome as well as aid prioritisation for resource-intensive target validation studies.



中文翻译:


结合成功目标反卷积的实验策略



对表型药物发现的投资导致了对快速、强大的靶标解卷积的需求增加,以帮助成功的药物开发。尽管目标识别和作用机制 (MoA) 发现的方法正在蓬勃发展,但它们通常会导致推定目标列表。验证哪些靶点参与化合物的治疗机制是一项重大挑战,需要在相关生理背景下进行直接结合、靶点参与和功能研究。正交方法的组合可以实现蛋白质组之外的目标识别,并有助于资源密集型目标验证研究的优先级排序。

更新日期:2020-11-15
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