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Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.
Chan KH, Zengerle M, Testa A, Ciulli A. Chan KH, et al. Among authors: testa a. J Med Chem. 2018 Jan 25;61(2):504-513. doi: 10.1021/acs.jmedchem.6b01912. Epub 2017 Jun 22. J Med Chem. 2018. PMID: 28595007 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: testa a. 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.
1,052 results