Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 210, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112981
Keywords
PROTAC; Small molecule; Target protein degradation; Undruggable target; Drug resistance; Drug discovery
Categories
Funding
- Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province [2019E10021]
- Health Commission of Zhejiang Province [WJKZJ-1918, 2020KY526]
- Youth Foundation of Zhejiang Academy of Medical Sciences [C11905Q-04]
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PROTAC is a novel drug discovery paradigm that targets proteins for degradation. ARV-110, an orally small molecule PROTAC designed for Androgen receptor, has entered clinical trials, marking a new avenue for PROTAC development.
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. (C) 2020 Elsevier Masson SAS. All rights reserved.
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