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The PROTACtable genome
Nature Reviews Drug Discovery ( IF 122.7 ) Pub Date : 2021-07-20 , DOI: 10.1038/s41573-021-00245-x
Melanie Schneider 1, 2 , Chris J Radoux 1, 2, 3 , Andrew Hercules 1, 2 , David Ochoa 1, 2 , Ian Dunham 1, 2 , Lykourgos-Panagiotis Zalmas 2, 4 , Gerhard Hessler 5 , Sven Ruf 5 , Veerabahu Shanmugasundaram 6 , Michael M Hann 7 , Pam J Thomas 7 , Markus A Queisser 7 , Andrew B Benowitz 7 , Kris Brown 8, 9 , Andrew R Leach 1, 2
Affiliation  

Proteolysis-targeting chimeras (PROTACs) are an emerging drug modality that may offer new opportunities to circumvent some of the limitations associated with traditional small-molecule therapeutics. By analogy with the concept of the ‘druggable genome’, the question arises as to which potential drug targets might PROTAC-mediated protein degradation be most applicable. Here, we present a systematic approach to the assessment of the PROTAC tractability (PROTACtability) of protein targets using a series of criteria based on data and information from a diverse range of relevant publicly available resources. Our approach could support decision-making on whether or not a particular target may be amenable to modulation using a PROTAC. Using our approach, we identified 1,067 proteins of the human proteome that have not yet been described in the literature as PROTAC targets that offer potential opportunities for future PROTAC-based efforts.



中文翻译:

 PROTACTable 基因组


蛋白水解靶向嵌合体(PROTAC)是一种新兴的药物模式,可能为规避传统小分子疗法的一些局限性提供新的机会。与“可成药基因组”的概念类比,出现了哪些潜在药物靶点可能最适用于 PROTAC 介导的蛋白质降解的问题。在这里,我们提出了一种系统方法,使用基于各种相关公开资源的数据和信息的一系列标准来评估蛋白质靶标的 PROTAC 易处理性 (PROTACtability)。我们的方法可以支持关于特定目标是否适合使用 PROTAC 进行调制的决策。使用我们的方法,我们鉴定了人类蛋白质组中尚未在文献中描述为 PROTAC 靶点的 1,067 种蛋白质,这些蛋白质为未来基于 PROTAC 的工作提供了潜在的机会。

更新日期:2021-07-20
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