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Review Article

基于肽的PROTACs：当前的挑战和未来展望

卷 31, 期 2, 2024

发表于: 20 March, 2023

页: [208 - 222] 页: 15

弟呕挨: 10.2174/0929867330666230130121822

价格: $65

摘要

蛋白水解靶向嵌合体 (PROTAC) 是一种针对以前不可成药或耐药突变蛋白的有吸引力的方法。虽然基于小分子的 PROTAC 很稳定并且可以穿过细胞膜，但能够将蛋白质招募到 E3 泛素连接酶进行降解的合适小分子弹头的可用性有限。随着结构生物学和计算机蛋白质结构预测的进步，现在定义适合 PROTAC 设计的高选择性肽变得越来越容易。因此，基于肽的 PROTAC 正在成为针对先前不适合小分子抑制的“不可成药”蛋白质的可行方案。在这篇综述中，我们总结了基于肽的 PROTAC 的设计和应用的最新进展，以及获得 PROTAC 候选肽的几种实用方法。我们还讨论了阻碍基于肽的 PROTAC 从实验室转化为临床的主要障碍，例如它们的递送和生物利用度，目的是激发关于如何在不久的将来最好地加速基于肽的 PROTAC 的临床开发的讨论。

关键词: 基于肽的PROTAC，靶向蛋白质降解，药物递送，不可成药蛋白质，E3泛素，突变蛋白

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