PROteolysis TArgeting Chimeras (PROTACs) offer new opportunities in modern medicine by targeting proteins that are intractable to classic inhibitors. Heterobifunctional in nature, PROTACs are small molecules that offer a unique mechanism of protein degradation by hijacking the ubiquitin-mediated protein degradation pathway, known as the ubiquitin–proteasome system. Herein, we present an analysis on the structural characteristics of this novel chemical modality. Furthermore, we review and discuss the formulation opportunities to overcome the oral delivery challenges of PROTACs in drug discovery.

中文翻译：

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早期评估口服 PROTAC 克服分子挑战的机会

蛋白水解靶向嵌合体 (PROTAC) 通过靶向经典抑制剂难以处理的蛋白质，为现代医学提供了新的机遇。PROTAC 本质上是异双功能的小分子，通过劫持泛素介导的蛋白质降解途径（称为泛素-蛋白酶体系统）来提供独特的蛋白质降解机制。在这里，我们对这种新型化学形态的结构特征进行了分析。此外，我们回顾并讨论了药物发现中克服 PROTAC 口服给药挑战的制剂机会。