2. Academic Validation
  3. Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

  • Eur J Med Chem. 2021 Jan 15:210:112981. doi: 10.1016/j.ejmech.2020.112981.
Shenxin Zeng 1,  Wenhai Huang 1,  Xiaoliang Zheng 2,  Liyan Cheng 2,  Zhimin Zhang 3,  Jian Wang 4,  Zhengrong Shen 5
Affiliations

Affiliations

  • 1 Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province, Institute of Materia Medica, Hangzhou Medical College, Hangzhou, 310013, PR China; School of Pharmacy, Hangzhou Medical College, Hangzhou, 310013, PR China.
  • 2 Center for Molecular Medicine, Hangzhou Medical College, Hangzhou, 310013, PR China.
  • 3 Department of Drug Platform of Small Molecules, HangZhou ZhongMei HuaDong Pharmaceutical CO, LTD, 866 Moganshan Road, Hangzhou, 310011, PR China.
  • 4 School of Pharmacy, Hangzhou Medical College, Hangzhou, 310013, PR China.
  • 5 Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province, Institute of Materia Medica, Hangzhou Medical College, Hangzhou, 310013, PR China; School of Pharmacy, Hangzhou Medical College, Hangzhou, 310013, PR China. Electronic address: Shenzr601@163.com.
PMID: 33160761 DOI: 10.1016/j.ejmech.2020.112981
Abstract

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.

Keywords

Drug discovery; Drug resistance; PROTAC; Small molecule; Target protein degradation; Undruggable target.

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