Targeted protein degradation in cancers: Orthodox PROTACs and beyond
|Corresponding Author||Lu，Aiping; Liang，Chao|
|Joint first author||Li，Jin; Chen，Xinxin|
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology can be used to target proteins by hijacking the ubiquitin-proteasome system. Conceptually, PROTAC aims to target the “undruggable” majority of proteins in the human proteome. Through constant exploration and optimization of PROTACs and the exploitation of other TPD strategies over two decades, TPD has expanded from theoretical studies to clinical strategies, with practical applications in oncological, immunological, and other diseases. In this review, we introduce the mechanisms, features, and molecular targets of orthodox PROTACs and summarize the PROTAC drugs under study as cancer therapeutics in clinical trials. We also discuss PROTAC derivatives and other TPD strategies, such as lysosome-targeting chimeras, autophagy-targeting chimeras, and molecular glue strategies. Collectively, the studies summarized herein support the full potential of TPD in the biomedical industry.
First ; 共同第一 ; Corresponding
Department of Education of Guangdong Province[2021KTSCX104] ; Basic and Applied Basic Research Foundation of Guangdong Province[2022A1515012164] ; National Natural Science Foundation of China ; National Natural Science Foundation of China
|WOS Research Area|
Science & Technology - Other Topics
|WOS Accession No|
Cited Times [WOS]:0
|Document Type||Journal Article|
|Department||Department of Biology|
1.Department of Biology,School of Life Sciences,Southern University of Science and Technology,Shenzhen,518055,China
2.Institute of Integrated Bioinfomedicine and Translational Science (IBTS),School of Chinese Medicine,Hong Kong Baptist University,Hong Kong SAR,999077,Hong Kong
3.State Key Laboratory of Proteomics,National Center for Protein Sciences (Beijing),Beijing Institute of Lifeomics,Beijing,100850,China
4.Guangdong–Hong Kong–Macau Joint Lab on Chinese Medicine and Immune Disease Research,Guangzhou,510006,China
|First Author Affilication||Department of Biology; School of Life Sciences|
|Corresponding Author Affilication||Department of Biology; School of Life Sciences|
|First Author's First Affilication||Department of Biology; School of Life Sciences|
Li，Jin,Chen，Xinxin,Lu，Aiping,et al. Targeted protein degradation in cancers: Orthodox PROTACs and beyond[J]. Innovation,2023,4(3).
Li，Jin,Chen，Xinxin,Lu，Aiping,&Liang，Chao.(2023).Targeted protein degradation in cancers: Orthodox PROTACs and beyond.Innovation,4(3).
Li，Jin,et al."Targeted protein degradation in cancers: Orthodox PROTACs and beyond".Innovation 4.3(2023).
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