Context matters: E3 ligase–ligand pairing strategies for optimized PROTAC performance
Luyao Yin, Pengcheng Shu, Xiaozhong Peng · 2025
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Description
Drugs that hijack the cell's shredder to destroy a chosen protein live or die by their matchmaking. Luyao Yin, Pengcheng Shu, and Xiaozhong Peng argue the shredder's handle matters as much as the grip on the target. Their perspective surveys how pairing each PROTAC with the right E3 ligase, the enzyme that tags proteins for destruction, changes results across cancers and tissues.
Head-to-head comparisons show no universal champion. One ligase family leads in blood cancers, another in certain solid tumours, and fresh ligase options promise escape from resistance. Tissue distribution and the chemistry of the three-way complex explain the patchwork. The authors' refrain: context dictates strategy. They also peek at degrading non-protein targets and using these molecules as laboratory knockdown tools.
Catalog record
| CREATOR | Luyao Yin, Pengcheng Shu, Xiaozhong Peng |
|---|---|
| YEAR | 2025 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 60 KB |
| VERSION | 1.0 |
| LICENSE | CC BY 4.0 |
| RIGHTS | CC BY |
| SOURCE | Europe PMC |