“超越五规则”化学空间中的蛋白酶靶向嵌合体（PROTACs）：近期进展与未来挑战
Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five' chemical space: Recent progress and future challenges.
作者信息
Edmondson Scott D, Yang Bin, Fallan Charlene
机构信息
Medicinal Chemistry, Oncology, IMED Biotech Unit, AstraZeneca, Boston, MA, USA.
Medicinal Chemistry, Oncology, IMED Biotech Unit, AstraZeneca, Boston, MA, USA.
出版信息
Bioorg Med Chem Lett. 2019 Jul 1;29(13):1555-1564. doi: 10.1016/j.bmcl.2019.04.030. Epub 2019 Apr 20.
Proteolysis targeting chimeras (PROTACs) are heterobifunctional compounds with molecular weights and other properties that lie outside the classic 'rule-of-five' space. Consequently, PROTACs have unique challenges associated with their development as potential therapeutic agents. This review summarizes and analyzes a representative set of recent PROTACs and highlights some of the potential future challenges facing this promising modality.
蛋白酶靶向嵌合体（PROTACs）是一类异双功能化合物，其分子量和其他性质超出了经典的“五规则”范围。因此，PROTACs作为潜在治疗药物的开发面临着独特的挑战。本综述总结并分析了一组具有代表性的近期PROTACs，并强调了这种有前景的药物形式未来可能面临的一些挑战。
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