Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand with terminal hydroxyl ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Zoppi et al (2019) Iterative design and optimization of initially inactive Proteolysis Targeting Chimeras (PROTACs) identify VZ185 as a potent, fast, and selective Von Hippel-Lindau (VHL) based dual degrader probe of BRD9 and BRD7. J.Med.Chem. 62 699 PMID:30540463 |Girardini et al (2019) Cereblon versus VHL: hijacking E3 ligases against each other using PROTACs. Bioorg.Med.Chem. 27 2466 PMID:30826187 |Farnaby et al (2019) BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design. Nat.Chem.Biol. 15 672 PMID:31178587 |Maniaci et al (2017) Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation. Nat.Commun. 8 830 PMID:29018234