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Target 2035 - update on the quest for a probe for every protein.
Müller S, Ackloo S, Al Chawaf A, Al-Lazikani B, Antolin A, Baell JB, Beck H, Beedie S, Betz UAK, Bezerra GA, Brennan PE, Brown D, Brown PJ, Bullock AN, Carter AJ, Chaikuad A, Chaineau M, Ciulli A, Collins I, Dreher J, Drewry D, Edfeldt K, Edwards AM, Egner U, Frye SV, Fuchs SM, Hall MD, Hartung IV, Hillisch A, Hitchcock SH, Homan E, Kannan N, Kiefer JR, Knapp S, Kostic M, Kubicek S, Leach AR, Lindemann S, Marsden BD, Matsui H, Meier JL, Merk D, Michel M, Morgan MR, Mueller-Fahrnow A, Owen DR, Perry BG, Rosenberg SH, Saikatendu KS, Schapira M, Scholten C, Sharma S, Simeonov A, Sundström M, Superti-Furga G, Todd MH, Tredup C, Vedadi M, von Delft F, Willson TM, Winter GE, Workman P, Arrowsmith CH. Müller S, et al. Among authors: ciulli a. RSC Med Chem. 2021 Dec 3;13(1):13-21. doi: 10.1039/d1md00228g. eCollection 2022 Jan 27. RSC Med Chem. 2021. PMID: 35211674 Free PMC article.
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: ciulli 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.
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298).
Soares P, Gadd MS, Frost J, Galdeano C, Ellis L, Epemolu O, Rocha S, Read KD, Ciulli A. Soares P, et al. Among authors: ciulli a. J Med Chem. 2018 Jan 25;61(2):599-618. doi: 10.1021/acs.jmedchem.7b00675. Epub 2017 Sep 18. J Med Chem. 2018. PMID: 28853884 Free PMC article.
Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions.
Popow J, Arnhof H, Bader G, Berger H, Ciulli A, Covini D, Dank C, Gmaschitz T, Greb P, Karolyi-Özguer J, Koegl M, McConnell DB, Pearson M, Rieger M, Rinnenthal J, Roessler V, Schrenk A, Spina M, Steurer S, Trainor N, Traxler E, Wieshofer C, Zoephel A, Ettmayer P. Popow J, et al. Among authors: ciulli a. J Med Chem. 2019 Mar 14;62(5):2508-2520. doi: 10.1021/acs.jmedchem.8b01826. Epub 2019 Feb 22. J Med Chem. 2019. PMID: 30739444
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