Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models
Lücking, Ulrich, Wortmann, Lars, Wengner, Antje M, Lefranc, Julien, Lienau, Philip, Briem, Hans, Siemeister, Gerhard, Bömer, Ulf, Denner, Karsten, Schäfer, Martina, Koppitz, Marcus, Eis, Knut, Bartels, Florian, Bader, Benjamin, Bone, Wilhelm, Moosmayer, Dieter, Holton, Simon J, Eberspächer, Uwe, Grudzinska-Goebel, Joanna, Schatz, Christoph, Deeg, Gesa, Mumberg, Dominik, von Nussbaum, Franz
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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Journal Article
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2‑d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5
Nguyen, Duy, Lemos, Clara, Wortmann, Lars, Eis, Knut, Holton, Simon J, Boemer, Ulf, Moosmayer, Dieter, Eberspaecher, Uwe, Weiske, Joerg, Lechner, Christian, Prechtl, Stefan, Suelzle, Detlev, Siegel, Franziska, Prinz, Florian, Lesche, Ralf, Nicke, Barbara, Nowak-Reppel, Katrin, Himmel, Herbert, Mumberg, Dominik, von Nussbaum, Franz, Nising, Carl F, Bauser, Marcus, Haegebarth, Andrea
Published in Journal of medicinal chemistry (24.01.2019)
Published in Journal of medicinal chemistry (24.01.2019)
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Journal Article
Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors In Vitro and In Vivo
Siemeister, Gerhard, Mengel, Anne, Fernández-Montalván, Amaury E, Bone, Wilhelm, Schröder, Jens, Zitzmann-Kolbe, Sabine, Briem, Hans, Prechtl, Stefan, Holton, Simon J, Mönning, Ursula, von Ahsen, Oliver, Johanssen, Sandra, Cleve, Arwed, Pütter, Vera, Hitchcock, Marion, von Nussbaum, Franz, Brands, Michael, Ziegelbauer, Karl, Mumberg, Dominik
Published in Clinical cancer research (15.02.2019)
Published in Clinical cancer research (15.02.2019)
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Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer
Dieter, Sebastian M., Siegl, Christine, Codó, Paula L., Huerta, Mario, Ostermann-Parucha, Anna L., Schulz, Erik, Zowada, Martina K., Martin, Sylvia, Laaber, Karin, Nowrouzi, Ali, Blatter, Mona, Kreth, Sina, Westermann, Frank, Benner, Axel, Uhrig, Ulrike, Putzker, Kerstin, Lewis, Joe, Haegebarth, Andrea, Mumberg, Dominik, Holton, Simon J., Weiske, Joerg, Toepper, Lena-Marit, Scheib, Ulrike, Siemeister, Gerhard, Ball, Claudia R., Kuster, Bernhard, Stoehr, Gabriele, Hahne, Hannes, Johannes, Sarah, Lange, Martin, Herbst, Friederike, Glimm, Hanno
Published in Cell reports (Cambridge) (20.07.2021)
Published in Cell reports (Cambridge) (20.07.2021)
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Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase
Schulze, Volker K, Klar, Ulrich, Kosemund, Dirk, Wengner, Antje M, Siemeister, Gerhard, Stöckigt, Detlef, Neuhaus, Roland, Lienau, Philip, Bader, Benjamin, Prechtl, Stefan, Holton, Simon J, Briem, Hans, Marquardt, Tobias, Schirok, Hartmut, Jautelat, Rolf, Bohlmann, Rolf, Nguyen, Duy, Fernández-Montalván, Amaury E, Bömer, Ulf, Eberspaecher, Uwe, Brüning, Michael, Döhr, Olaf, Raschke, Marian, Kreft, Bertolt, Mumberg, Dominik, Ziegelbauer, Karl, Brands, Michael, von Nussbaum, Franz, Koppitz, Marcus
Published in Journal of medicinal chemistry (13.08.2020)
Published in Journal of medicinal chemistry (13.08.2020)
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Journal Article
ATAD2 is an epigenetic reader of newly synthesized histone marks during DNA replication
Koo, Seong Joo, Fernández-Montalván, Amaury E, Badock, Volker, Ott, Christopher J, Holton, Simon J, von Ahsen, Oliver, Toedling, Joern, Vittori, Sarah, Bradner, James E, Gorjánácz, Mátyás
Published in Oncotarget (25.10.2016)
Published in Oncotarget (25.10.2016)
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Journal Article
Discovery and Characterization of the Potent and Highly Selective 1,7-Naphthyridine-Based Inhibitors BAY-091 and BAY-297 of the Kinase PIP4K2A
Wortmann, Lars, Bräuer, Nico, Holton, Simon J, Irlbacher, Horst, Weiske, Jörg, Lechner, Christian, Meier, Robin, Karén, Jakob, Siöberg, Catrine Berthold, Pütter, Vera, Christ, Clara D, ter Laak, Antonius, Lienau, Philip, Lesche, Ralf, Nicke, Barbara, Cheung, Shing-Hu, Bauser, Marcus, Haegebarth, Andrea, von Nussbaum, Franz, Mumberg, Dominik, Lemos, Clara
Published in Journal of medicinal chemistry (11.11.2021)
Published in Journal of medicinal chemistry (11.11.2021)
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Coordination of Di-Acetylated Histone Ligands by the ATAD2 Bromodomain
Evans, Chiara M, Phillips, Margaret, Malone, Kiera L, Tonelli, Marco, Cornilescu, Gabriel, Cornilescu, Claudia, Holton, Simon J, Gorjánácz, Mátyás, Wang, Liping, Carlson, Samuel, Gay, Jamie C, Nix, Jay C, Demeler, Borries, Markley, John L, Glass, Karen C
Published in International journal of molecular sciences (24.08.2021)
Published in International journal of molecular sciences (24.08.2021)
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Journal Article
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains
Bouché, Léa, Christ, Clara D, Siegel, Stephan, Fernández-Montalván, Amaury E, Holton, Simon J, Fedorov, Oleg, ter Laak, Antonius, Sugawara, Tatsuo, Stöckigt, Detlef, Tallant, Cynthia, Bennett, James, Monteiro, Octovia, Díaz-Sáez, Laura, Siejka, Paulina, Meier, Julia, Pütter, Vera, Weiske, Jörg, Müller, Susanne, Huber, Kilian V. M, Hartung, Ingo V, Haendler, Bernard
Published in Journal of medicinal chemistry (11.05.2017)
Published in Journal of medicinal chemistry (11.05.2017)
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Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists
Orsi, Douglas L., Ferrara, Steven J., Siegel, Stephan, Friberg, Anders, Bouché, Léa, Pook, Elisabeth, Lienau, Philip, Bluck, Joseph P., Lemke, Christopher T., Akcay, Gizem, Stellfeld, Timo, Meyer, Hanna, Pütter, Vera, Holton, Simon J., Korr, Daniel, Jerchel-Furau, Isabel, Pantelidou, Constantia, Strathdee, Craig A., Meyerson, Matthew, Eis, Knut, Goldstein, Jonathan T.
Published in Bioorganic & medicinal chemistry (15.01.2023)
Published in Bioorganic & medicinal chemistry (15.01.2023)
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Journal Article
Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action
Fernández-Montalván, Amaury E, Berger, Markus, Kuropka, Benno, Koo, Seong Joo, Badock, Volker, Weiske, Joerg, Puetter, Vera, Holton, Simon J, Stöckigt, Detlef, ter Laak, Antonius, Centrella, Paolo A, Clark, Matthew A, Dumelin, Christoph E, Sigel, Eric A, Soutter, Holly H, Troast, Dawn M, Zhang, Ying, Cuozzo, John W, Keefe, Anthony D, Roche, Didier, Rodeschini, Vincent, Chaikuad, Apirat, Díaz-Sáez, Laura, Bennett, James M, Fedorov, Oleg, Huber, Kilian V. M, Hübner, Jan, Weinmann, Hilmar, Hartung, Ingo V, Gorjánácz, Mátyás
Published in ACS chemical biology (17.11.2017)
Published in ACS chemical biology (17.11.2017)
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Functional and Structural Characterization of Bub3·BubR1 Interactions Required for Spindle Assembly Checkpoint Signaling in Human Cells
Prinz, Florian, Puetter, Vera, Holton, Simon J., Andres, Dorothee, Stegmann, Christian M., Kwiatkowski, Dennis, Prechtl, Stefan, Petersen, Kirstin, Beckmann, Georg, Kreft, Bertolt, Mumberg, Dominik, Fernández-Montalván, Amaury
Published in The Journal of biological chemistry (20.05.2016)
Published in The Journal of biological chemistry (20.05.2016)
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Journal Article
The peroxisomal receptor Pex19p forms a helical mPTS recognition domain
Schueller, Nicole, Holton, Simon J, Fodor, Krisztian, Milewski, Morlin, Konarev, Petr, Stanley, Will A, Wolf, Janina, Erdmann, Ralf, Schliebs, Wolfgang, Song, Young-Hwa, Wilmanns, Matthias
Published in The EMBO journal (04.08.2010)
Published in The EMBO journal (04.08.2010)
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Journal Article
The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models
Lemos, Clara, Schulze, Volker K., Baumgart, Simon J., Nevedomskaya, Ekaterina, Heinrich, Tobias, Lefranc, Julien, Bader, Benjamin, Christ, Clara D., Briem, Hans, Kuhnke, Lara P., Holton, Simon J., Bömer, Ulf, Lienau, Philip, von Nussbaum, Franz, Nising, Carl F., Bauser, Marcus, Hägebarth, Andrea, Mumberg, Dominik, Haendler, Bernard
Published in Cellular oncology (Dordrecht) (01.06.2021)
Published in Cellular oncology (Dordrecht) (01.06.2021)
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Expression, purification, characterization and structure of Pseudomonas aeruginosa arylamine N-acetyltransferase
Westwood, Isaac M, Holton, Simon J, Rodrigues-Lima, Fernando, Dupret, Jean-Marie, Bhakta, Sanjib, Noble, Martin E M, Sim, Edith
Published in Biochemical journal (15.01.2005)
Published in Biochemical journal (15.01.2005)
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Journal Article
Investigation of the catalytic triad of arylamine N-acetyltransferases: essential residues required for acetyl transfer to arylamines
Sandy, James, Mushtaq, Adeel, Holton, Simon J, Schartau, Pamela, Noble, Martin E M, Sim, Edith
Published in Biochemical journal (15.08.2005)
Published in Biochemical journal (15.08.2005)
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