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Non-PEG Linkers for Designing Proteolysis Targeting Chimera Molecules
Proteolysis targeting chimera molecules are bifunctional small molecules which consist of a ubiquitin E3 ligase ligand and a protein of interest (POI) ligand covalently bonded via a linker. The chimera molecules that induce the degradation of POI, while conventional molecules cannot, are regarded as a new drug modality. Although PEG linkers are typically used as linkers, the drug-like structures using non-PEG linkers with shorter linker length have been recently reported.1,2) Non-PEG linkers, 1-Boc-4-(piperidin-4-ylmethyl)piperazine (1) and 1-Boc-4-(piperazin-1-ylmethyl)piperidine (2) can bind to various ligands. The proteolysis targeting chimera molecules derivatized from 1 or 2 are studied as potential oral drugs.
Related Products
Product Category Pages
- Homobifunctional Cross-Linkers
- Heterobifunctional Cross-Linkers
- Proteolysis Targeting Chimera Research Reagents
References
- 1) Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer
- 2) Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation
