The PROTAC technology in drug development
Top Cited Papers
Open Access
- 2 January 2019
- journal article
- review article
- Published by Wiley in Cell Biochemistry and Function
- Vol. 37 (1), 21-30
- https://doi.org/10.1002/cbf.3369
Abstract
Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein. During the first decade, three pedigreed groups worked on the development of this technology. To date, this technology has been extended by different groups, aiming to develop new drugs against different diseases including cancers. This review summarizes the contributions of the groups for the development of PROTAC. Significance of the study This review summarized the development of the PROTAC technology for readers and also presented the author's opinions on the application of the technology in tumor therapy.Keywords
Funding Information
- National Natural Science Foundation of China (81572729, 81830092, 81872244)
This publication has 97 references indexed in Scilit:
- Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteinsNature Chemical Biology, 2011
- Development of target protein-selective degradation inducer for protein knockdownBioorganic & Medicinal Chemistry, 2011
- Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target proteinFEBS Letters, 2011
- Protacs for Treatment of CancerPediatric Research, 2010
- Design and Applications of Bifunctional Small Molecules: Why Two Heads Are Better Than OneACS Chemical Biology, 2008
- Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancerOncogene, 2008
- Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomicsBioorganic & Medicinal Chemistry Letters, 2008
- hSef potentiates EGF-mediated MAPK signaling through affecting EGFR trafficking and degradationCellular Signalling, 2008
- Development of an Aryl Hydrocarbon Receptor Antagonist Using the Proteolysis-Targeting Chimeric Molecules Approach: A Potential Tool for ChemopreventionMolecular Pharmacology, 2008
- Chemical Genetic Control of Protein Levels: Selective in Vivo Targeted DegradationJournal of the American Chemical Society, 2004