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Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity.
Imaide S, Riching KM, Makukhin N, Vetma V, Whitworth C, Hughes SJ, Trainor N, Mahan SD, Murphy N, Cowan AD, Chan KH, Craigon C, Testa A, Maniaci C, Urh M, Daniels DL, Ciulli A. Imaide S, et al. Among authors: hughes sj. Nat Chem Biol. 2021 Nov;17(11):1157-1167. doi: 10.1038/s41589-021-00878-4. Epub 2021 Oct 21. Nat Chem Biol. 2021. PMID: 34675414 Free PMC article.
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.
Zoppi V, Hughes SJ, Maniaci C, Testa A, Gmaschitz T, Wieshofer C, Koegl M, Riching KM, Daniels DL, Spallarossa A, Ciulli A. Zoppi V, et al. Among authors: hughes sj. J Med Chem. 2019 Jan 24;62(2):699-726. doi: 10.1021/acs.jmedchem.8b01413. Epub 2018 Dec 28. J Med Chem. 2019. PMID: 30540463 Free PMC article.
Structure-Based Design of a Macrocyclic PROTAC.
Testa A, Hughes SJ, Lucas X, Wright JE, Ciulli A. Testa A, et al. Among authors: hughes sj. Angew Chem Int Ed Engl. 2020 Jan 20;59(4):1727-1734. doi: 10.1002/anie.201914396. Epub 2019 Dec 12. Angew Chem Int Ed Engl. 2020. PMID: 31746102 Free PMC article.
Understanding and Improving the Membrane Permeability of VH032-Based PROTACs.
Klein VG, Townsend CE, Testa A, Zengerle M, Maniaci C, Hughes SJ, Chan KH, Ciulli A, Lokey RS. Klein VG, et al. Among authors: hughes sj. ACS Med Chem Lett. 2020 Jul 30;11(9):1732-1738. doi: 10.1021/acsmedchemlett.0c00265. eCollection 2020 Sep 10. ACS Med Chem Lett. 2020. PMID: 32939229 Free PMC article.
298 results