Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3 ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug discovery paradigm which has been widely used as biological tools and medicinal molecules with the potential of clinical application value. Currently, ARV-110, an orally small molecule PROTAC was designed to specifically target Androgen receptor (AR), firstly enters clinical phase I trials for the treatment of metastatic castration-resistant prostate cancer, which turns a new avenue for the development of PROTAC. We herein provide a detail summary on the latest one year progress of PROTAC target various proteins and elucidate the advantages of PROTAC technology. Finally, the potential challenges of this vibrant field are also discussed.

靶向嵌合体（PROTAC）的蛋白水解，劫持目标蛋白（POI）并募集E3连接酶以通过以下途径降解靶标泛素-蛋白酶体途径是一种新的药物发现范例，已被广泛用作生物学工具和药用分子，具有潜在的临床应用价值。目前，口服小分子PROTAC ARV-110被设计为专门针对雄激素受体（AR），首先进入I期临床试验以治疗转移性去势抵抗性前列腺癌，这为PROTAC的发展开辟了新途径。我们在此提供有关PROTAC靶向各种蛋白质的最新进展的详细摘要，并阐明PROTAC技术的优势。最后，还讨论了这个充满活力的领域的潜在挑战。