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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. Copyright © 2020 Elsevier Masson SAS. All rights reserved.


Shenxin Zeng, Wenhai Huang, Xiaoliang Zheng, Liyan Cheng, Zhimin Zhang, Jian Wang, Zhengrong Shen. Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges. European journal of medicinal chemistry. 2021 Jan 15;210:112981

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PMID: 33160761

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