Cited by 286Protein Degradation and InhibitorsUbiquitin and proteasome pathwaysChemical Synthesis and Analysis

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

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He, Ming, Cao, Chaoguo, Ni, Zhihao, Liu, Yongbo, Song, Peilu, Hao, Shuang, He, Yuna, Sun, Xiuyun +1 more·2022·Signal Transduction and Targeted Therapy

Abstract

PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-degradation strategy that has emerged in recent years. It uses bifunctional small molecules to induce the ubiquitination and degradation of target proteins through the ubiquitin–proteasome system. PROTACs can not only be used as potential clinical treatments for diseases such as cancer, immune disorders, viral infections, and neurodegenerative diseases, but also provide unique chemical knockdown tools for biological research in a catalytic, reversible, and rapid manner. In 2019, our group published a review article “PROTACs: great opportunities for academia and industry” in the journal, summarizing the representative compounds of PROTACs reported before the end of 2019. In the past 2 years, the entire field of protein degradation has experienced rapid development, including not only a large increase in the number of research papers on protein-degradation technology but also a rapid increase in the number of small-molecule degraders that have entered the clinical and will enter the clinical stage. In addition to PROTAC and molecular glue technology, other new degradation technologies are also developing rapidly. In this article, we mainly summarize and review the representative PROTACs of related targets published in 2020–2021 to present to researchers the exciting developments in the field of protein degradation. The problems that need to be solved in this field will also be briefly introduced.

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  1. [203]Georg EW Phthalimide conjugation as a strategy for in vivo target protein degradation Science 2015 348 1376 1381 10.1126/science.aab1433 25999370 PMC4937790 · DOI · Paper page
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Authors
He, M., Cao, C., Ni, Z., Liu, Y., Song, P., Hao, S., He, Y., Sun, X., & Rao, Y.
Affiliations
  • Tsinghua University (CN)
  • Zhengzhou University (CN)
Corresponding author
Rao, Yu
Venue
Signal Transduction and Targeted Therapy
Published
2022-06-09
Volume
7
Issue
1
Pages
181-181
ISSN
2059-3635 (ISSN-L)
OpenAlex
W4281795388
Cited by
283
References
559
Citations by year
2026: 50 · 2025: 82 · 2024: 84 · 2023: 50 · 2022: 17
FWCI
6.14
Type
journal article
Language
en
Open access
Locations
  • Signal Transduction and Targeted Therapy (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion)
Funders
  • National Natural Science Foundation of China (#82125034, #81773567, 2021YFA1302100, 2020YFE0202200)
  • China Postdoctoral Science Foundation
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ubiquitin and proteasome pathways
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
Keywords
PROTACs, protein degradation, bifunctional small molecules, ubiquitination, ubiquitin-proteasome system, molecular glues, small-molecule degraders, clinical development, cancer therapy
MeSH terms
Ubiquitin-Protein Ligases, Proteasome Endopeptidase Complex, Proteolysis

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