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Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action.
Fernández-Montalván AE, Berger M, Kuropka B, Koo SJ, Badock V, Weiske J, Puetter V, Holton SJ, Stöckigt D, Ter Laak A, Centrella PA, Clark MA, Dumelin CE, Sigel EA, Soutter HH, Troast DM, Zhang Y, Cuozzo JW, Keefe AD, Roche D, Rodeschini V, Chaikuad A, Díaz-Sáez L, Bennett JM, Fedorov O, Huber KVM, Hübner J, Weinmann H, Hartung IV, Gorjánácz M. Fernández-Montalván AE, et al. Among authors: badock v. ACS Chem Biol. 2017 Nov 17;12(11):2730-2736. doi: 10.1021/acschembio.7b00708. Epub 2017 Oct 24. ACS Chem Biol. 2017. PMID: 29043777 Free PMC article.
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.
Eggert E, Hillig RC, Koehr S, Stöckigt D, Weiske J, Barak N, Mowat J, Brumby T, Christ CD, Ter Laak A, Lang T, Fernandez-Montalvan AE, Badock V, Weinmann H, Hartung IV, Barsyte-Lovejoy D, Szewczyk M, Kennedy S, Li F, Vedadi M, Brown PJ, Santhakumar V, Arrowsmith CH, Stellfeld T, Stresemann C. Eggert E, et al. Among authors: badock v. J Med Chem. 2016 May 26;59(10):4578-600. doi: 10.1021/acs.jmedchem.5b01890. Epub 2016 May 3. J Med Chem. 2016. PMID: 27075367 Free PMC article.
Structural analysis of human KDM5B guides histone demethylase inhibitor development.
Johansson C, Velupillai S, Tumber A, Szykowska A, Hookway ES, Nowak RP, Strain-Damerell C, Gileadi C, Philpott M, Burgess-Brown N, Wu N, Kopec J, Nuzzi A, Steuber H, Egner U, Badock V, Munro S, LaThangue NB, Westaway S, Brown J, Athanasou N, Prinjha R, Brennan PE, Oppermann U. Johansson C, et al. Among authors: badock v. Nat Chem Biol. 2016 Jul;12(7):539-45. doi: 10.1038/nchembio.2087. Epub 2016 May 23. Nat Chem Biol. 2016. PMID: 27214403
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.
Hillig RC, Sautier B, Schroeder J, Moosmayer D, Hilpmann A, Stegmann CM, Werbeck ND, Briem H, Boemer U, Weiske J, Badock V, Mastouri J, Petersen K, Siemeister G, Kahmann JD, Wegener D, Böhnke N, Eis K, Graham K, Wortmann L, von Nussbaum F, Bader B. Hillig RC, et al. Among authors: badock v. Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2551-2560. doi: 10.1073/pnas.1812963116. Epub 2019 Jan 25. Proc Natl Acad Sci U S A. 2019. PMID: 30683722 Free PMC article.
Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles.
Eaton JK, Furst L, Ruberto RA, Moosmayer D, Hilpmann A, Ryan MJ, Zimmermann K, Cai LL, Niehues M, Badock V, Kramm A, Chen S, Hillig RC, Clemons PA, Gradl S, Montagnon C, Lazarski KE, Christian S, Bajrami B, Neuhaus R, Eheim AL, Viswanathan VS, Schreiber SL. Eaton JK, et al. Among authors: badock v. Nat Chem Biol. 2020 May;16(5):497-506. doi: 10.1038/s41589-020-0501-5. Epub 2020 Mar 30. Nat Chem Biol. 2020. PMID: 32231343 Free PMC article.
Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening.
Gradl S, Steuber H, Weiske J, Szewczyk MM, Schmees N, Siegel S, Stoeckigt D, Christ CD, Li F, Organ S, Abbey M, Kennedy S, Chau I, Trush V, Barsyte-Lovejoy D, Brown PJ, Vedadi M, Arrowsmith C, Husemann M, Badock V, Bauser M, Haegebarth A, Hartung IV, Stresemann C. Gradl S, et al. Among authors: badock v. SLAS Discov. 2021 Sep;26(8):947-960. doi: 10.1177/24725552211019409. Epub 2021 Jun 21. SLAS Discov. 2021. PMID: 34154424 Free article.
A miniaturized mode-of-action profiling platform enables high throughput characterization of the molecular and cellular dynamics of EZH2 inhibition.
Falkenstern L, Georgi V, Bunse S, Badock V, Husemann M, Roehn U, Stellfeld T, Fitzgerald M, Ferrara S, Stöckigt D, Stresemann C, Hartung IV, Fernández-Montalván A. Falkenstern L, et al. Among authors: badock v. Sci Rep. 2024 Jan 19;14(1):1739. doi: 10.1038/s41598-023-50964-x. Sci Rep. 2024. PMID: 38242973 Free PMC article.
23 results