Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles
Eaton, John K., Furst, Laura, Ruberto, Richard A., Moosmayer, Dieter, Hilpmann, André, Ryan, Matthew J., Zimmermann, Katja, Cai, Luke L., Niehues, Michael, Badock, Volker, Kramm, Anneke, Chen, Sixun, Hillig, Roman C., Clemons, Paul A., Gradl, Stefan, Montagnon, Claire, Lazarski, Kiel E., Christian, Sven, Bajrami, Besnik, Neuhaus, Roland, Eheim, Ashley L., Viswanathan, Vasanthi S., Schreiber, Stuart L.
Published in Nature chemical biology (01.05.2020)
Published in Nature chemical biology (01.05.2020)
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Journal Article
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction
Hillig, Roman C., Sautier, Brice, Schroeder, Jens, Moosmayer, Dieter, Hilpmann, André, Stegmanna, Christian M., Werbeck, Nicolas D., Briem, Hans, Boemer, Ulf, Weiske, Joerg, Badock, Volker, Mastouri, Julia, Petersen, Kirstin, Siemeister, Gerhard, Kahmann, Jan D., Wegener, Dennis, Böhnke, Niels, Eis, Knut, Graham, Keith, Wortmann, Lars, von Nussbaum, Franz, Bader, Benjamin
Published in Proceedings of the National Academy of Sciences - PNAS (12.02.2019)
Published in Proceedings of the National Academy of Sciences - PNAS (12.02.2019)
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Journal Article
Mechanism of inhibition of human glucose transporter GLUT1 is conserved between cytochalasin B and phenylalanine amides
Kapoor, Khyati, Finer-Moore, Janet S., Pedersen, Bjørn P., Caboni, Laura, Waight, Andrew, Hillig, Roman C., Bringmann, Peter, Heisler, Iring, Müller, Thomas, Siebeneicher, Holger, Stroud, Robert M.
Published in Proceedings of the National Academy of Sciences - PNAS (26.04.2016)
Published in Proceedings of the National Academy of Sciences - PNAS (26.04.2016)
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Journal Article
Crystal structures of the selenoprotein glutathione peroxidase 4 in its apo form and in complex with the covalently bound inhibitor ML162
Moosmayer, Dieter, Hilpmann, André, Hoffmann, Jutta, Schnirch, Lennart, Zimmermann, Katja, Badock, Volker, Furst, Laura, Eaton, John K., Viswanathan, Vasanthi S., Schreiber, Stuart L., Gradl, Stefan, Hillig, Roman C.
Published in Acta crystallographica. Section D, Biological crystallography. (01.02.2021)
Published in Acta crystallographica. Section D, Biological crystallography. (01.02.2021)
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Journal Article
Pan-mutant IDH1 inhibitor BAY 1436032 for effective treatment of IDH1 mutant astrocytoma in vivo
Pusch, Stefan, Krausert, Sonja, Fischer, Viktoria, Balss, Jörg, Ott, Martina, Schrimpf, Daniel, Capper, David, Sahm, Felix, Eisel, Jessica, Beck, Ann-Christin, Jugold, Manfred, Eichwald, Viktoria, Kaulfuss, Stefan, Panknin, Olaf, Rehwinkel, Hartmut, Zimmermann, Katja, Hillig, Roman C., Guenther, Judith, Toschi, Luisella, Neuhaus, Roland, Haegebart, Andrea, Hess-Stumpp, Holger, Bauser, Markus, Wick, Wolfgang, Unterberg, Andreas, Herold-Mende, Christel, Platten, Michael, von Deimling, Andreas
Published in Acta neuropathologica (01.04.2017)
Published in Acta neuropathologica (01.04.2017)
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Journal Article
Discovery and Characterization of the Potent and Selective P2X4 Inhibitor N‑[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile
Werner, Stefan, Mesch, Stefanie, Hillig, Roman C, ter Laak, Antonius, Klint, Julie, Neagoe, Ioana, Laux-Biehlmann, Alexis, Dahllöf, Henrik, Bräuer, Nico, Puetter, Vera, Nubbemeyer, Reinhard, Schulz, Simone, Bairlein, Michaela, Zollner, Thomas M, Steinmeyer, Andreas
Published in Journal of medicinal chemistry (26.12.2019)
Published in Journal of medicinal chemistry (26.12.2019)
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Journal Article
BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe
Günther, Judith, Hillig, Roman C., Zimmermann, Katja, Kaulfuss, Stefan, Lemos, Clara, Nguyen, Duy, Rehwinkel, Hartmut, Habgood, Matthew, Lechner, Christian, Neuhaus, Roland, Ganzer, Ursula, Drewes, Mark, Chai, Jijie, Bouché, Léa
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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Journal Article
Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics
Hillisch, Alexander, Gericke, Kersten M, Allerheiligen, Swen, Roehrig, Susanne, Schaefer, Martina, Tersteegen, Adrian, Schulz, Simone, Lienau, Philip, Gnoth, Mark, Puetter, Vera, Hillig, Roman C, Heitmeier, Stefan
Published in Journal of medicinal chemistry (12.11.2020)
Published in Journal of medicinal chemistry (12.11.2020)
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Journal Article
Discovery and Characterization of BAY-184: A New Potent and Selective Acylsulfonamide-Benzofuran In Vivo -Active KAT6AB Inhibitor
Ter Laak, Antonius, Hillig, Roman C, Ferrara, Steven J, Korr, Daniel, Barak, Naomi, Lienau, Philip, Herbert, Simon, Fernández-Montalván, Amaury Ernesto, Neuhaus, Roland, Gorjánácz, Mátyás, Puetter, Vera, Badock, Volker, Bone, Wilhelm, Strathdee, Craig, Siegel, Franziska, Schatz, Christoph, Nowak-Reppel, Katrin, Doehr, Olaf, Gradl, Stefan, Hartung, Ingo V, Meyerson, Matthew, Bouché, Léa
Published in Journal of medicinal chemistry (25.10.2024)
Published in Journal of medicinal chemistry (25.10.2024)
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Journal Article
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2
Eggert, Erik, Hillig, Roman C, Koehr, Silke, Stöckigt, Detlef, Weiske, Jörg, Barak, Naomi, Mowat, Jeffrey, Brumby, Thomas, Christ, Clara D, ter Laak, Antonius, Lang, Tina, Fernandez-Montalvan, Amaury E, Badock, Volker, Weinmann, Hilmar, Hartung, Ingo V, Barsyte-Lovejoy, Dalia, Szewczyk, Magdalena, Kennedy, Steven, Li, Fengling, Vedadi, Masoud, Brown, Peter J, Santhakumar, Vijayaratnam, Arrowsmith, Cheryl H, Stellfeld, Timo, Stresemann, Carlo
Published in Journal of medicinal chemistry (26.05.2016)
Published in Journal of medicinal chemistry (26.05.2016)
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Journal Article
A Novel NAMPT Inhibitor-Based Antibody–Drug Conjugate Payload Class for Cancer Therapy
Böhnke, Niels, Berger, Markus, Griebenow, Nils, Rottmann, Antje, Erkelenz, Michael, Hammer, Stefanie, Berndt, Sandra, Günther, Judith, Wengner, Antje M., Stelte-Ludwig, Beatrix, Mahlert, Christoph, Greven, Simone, Dietz, Lisa, Jörißen, Hannah, Barak, Naomi, Bömer, Ulf, Hillig, Roman C., Eberspaecher, Uwe, Weiske, Jörg, Giese, Anja, Mumberg, Dominik, Nising, Carl Friedrich, Weinmann, Hilmar, Sommer, Anette
Published in Bioconjugate chemistry (15.06.2022)
Published in Bioconjugate chemistry (15.06.2022)
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Journal Article
Identification of the Highly Active, Species Cross-Reactive Complex I Inhibitor BAY-179
Mowat, Jeffrey, Ehrmann, Alexander H. M, Christian, Sven, Sperl, Carolyn, Menz, Stephan, Günther, Judith, Hillig, Roman C, Bauser, Marcus, Schwede, Wolfgang
Published in ACS medicinal chemistry letters (10.03.2022)
Published in ACS medicinal chemistry letters (10.03.2022)
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Journal Article
Computationally Empowered Workflow Identifies Novel Covalent Allosteric Binders for KRAS G12C
Mortier, Jérémie, Friberg, Anders, Badock, Volker, Moosmayer, Dieter, Schroeder, Jens, Steigemann, Patrick, Siegel, Franziska, Gradl, Stefan, Bauser, Marcus, Hillig, Roman C, Briem, Hans, Eis, Knut, Bader, Benjamin, Nguyen, Duy, Christ, Clara D
Published in ChemMedChem (19.05.2020)
Published in ChemMedChem (19.05.2020)
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Journal Article
Computationally Empowered Workflow Identifies Novel Covalent Allosteric Binders for KRASG12C
Mortier, Jérémie, Friberg, Anders, Badock, Volker, Moosmayer, Dieter, Schroeder, Jens, Steigemann, Patrick, Siegel, Franziska, Gradl, Stefan, Bauser, Marcus, Hillig, Roman C., Briem, Hans, Eis, Knut, Bader, Benjamin, Nguyen, Duy, Christ, Clara D.
Published in ChemMedChem (19.05.2020)
Published in ChemMedChem (19.05.2020)
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Journal Article
Optimization of allosteric MEK inhibitors. Part 2: Taming the sulfamide group balances compound distribution properties
Hartung, Ingo V., Hammer, Stefanie, Hitchcock, Marion, Neuhaus, Roland, Scholz, Arne, Siemeister, Gerhard, Bohlmann, Rolf, Hillig, Roman C., Pühler, Florian
Published in Bioorganic & medicinal chemistry letters (01.01.2016)
Published in Bioorganic & medicinal chemistry letters (01.01.2016)
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Journal Article
The complex of Arl2-GTP and PDEδ: from structure to function
Hanzal-Bayer, Michael, Renault, Louis, Roversi, Pietro, Wittinghofer, Alfred, Hillig, Roman C.
Published in The EMBO journal (01.05.2002)
Published in The EMBO journal (01.05.2002)
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Journal Article
Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories
Hartung, Ingo V., Hitchcock, Marion, Pühler, Florian, Neuhaus, Roland, Scholz, Arne, Hammer, Stefanie, Petersen, Kirstin, Siemeister, Gerhard, Brittain, Dominic, Hillig, Roman C.
Published in Bioorganic & medicinal chemistry letters (15.04.2013)
Published in Bioorganic & medicinal chemistry letters (15.04.2013)
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Journal Article
Modular Assembly of Allosteric MEK Inhibitor Structural Elements Unravels Potency and Feedback-Modulation Handles
Hartung, Ingo V., Pühler, Florian, Neuhaus, Roland, Scholz, Arne, Siemeister, Gerhard, Geisler, Jens, Hillig, Roman C., von Ahsen, Oliver, Hitchcock, Marion
Published in ChemMedChem (01.12.2015)
Published in ChemMedChem (01.12.2015)
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Journal Article
Back Cover: Modular Assembly of Allosteric MEK Inhibitor Structural Elements Unravels Potency and Feedback-Modulation Handles (ChemMedChem 12/2015)
Hartung, Ingo V., Pühler, Florian, Neuhaus, Roland, Scholz, Arne, Siemeister, Gerhard, Geisler, Jens, Hillig, Roman C., von Ahsen, Oliver, Hitchcock, Marion
Published in ChemMedChem (01.12.2015)
Published in ChemMedChem (01.12.2015)
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