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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. 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. 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.
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Bouché L, Christ CD, Siegel S, Fernández-Montalván AE, Holton SJ, Fedorov O, Ter Laak A, Sugawara T, Stöckigt D, Tallant C, Bennett J, Monteiro O, Díaz-Sáez L, Siejka P, Meier J, Pütter V, Weiske J, Müller S, Huber KVM, Hartung IV, Haendler B. Bouché L, et al. Among authors: fernandez montalvan ae. J Med Chem. 2017 May 11;60(9):4002-4022. doi: 10.1021/acs.jmedchem.7b00306. Epub 2017 May 1. J Med Chem. 2017. PMID: 28402630 Free PMC article.
Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times.
Heroven C, Georgi V, Ganotra GK, Brennan P, Wolfreys F, Wade RC, Fernández-Montalván AE, Chaikuad A, Knapp S. Heroven C, et al. Among authors: fernandez montalvan ae. Angew Chem Int Ed Engl. 2018 Jun 11;57(24):7220-7224. doi: 10.1002/anie.201801666. Epub 2018 May 9. Angew Chem Int Ed Engl. 2018. PMID: 29601130 Free PMC article.
Binding Kinetics Survey of the Drugged Kinome.
Georgi V, Schiele F, Berger BT, Steffen A, Marin Zapata PA, Briem H, Menz S, Preusse C, Vasta JD, Robers MB, Brands M, Knapp S, Fernández-Montalván A. Georgi V, et al. J Am Chem Soc. 2018 Nov 21;140(46):15774-15782. doi: 10.1021/jacs.8b08048. Epub 2018 Nov 6. J Am Chem Soc. 2018. PMID: 30362749
36 results