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Phenotypic Discovery of Triazolo[1,5-c]quinazolines as a First-In-Class Bone Morphogenetic Protein Amplifier Chemotype.
Wesseler F, Lohmann S, Riege D, Halver J, Roth A, Pichlo C, Weber S, Takamiya M, Müller E, Ketzel J, Flegel J, Gihring A, Rastegar S, Bertrand J, Baumann U, Knippschild U, Peifer C, Sievers S, Waldmann H, Schade D. Wesseler F, et al. Among authors: sievers s. J Med Chem. 2022 Nov 24;65(22):15263-15281. doi: 10.1021/acs.jmedchem.2c01199. Epub 2022 Nov 8. J Med Chem. 2022. PMID: 36346705
Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA.
Teuber A, Schulz T, Fletcher BS, Gontla R, Mühlenberg T, Zischinsky ML, Niggenaber J, Weisner J, Kleinbölting SB, Lategahn J, Sievers S, Müller MP, Bauer S, Rauh D. Teuber A, et al. Among authors: sievers s. Nat Commun. 2024 Jan 2;15(1):63. doi: 10.1038/s41467-023-44376-8. Nat Commun. 2024. PMID: 38167404 Free PMC article.
KIT ATP-Binding Pocket/Activation Loop Mutations in GI Stromal Tumor: Emerging Mechanisms of Kinase Inhibitor Escape.
Mühlenberg T, Falkenhorst J, Schulz T, Fletcher BS, Teuber A, Krzeciesa D, Klooster I, Lundberg M, Wilson L, Lategahn J, von Mehren M, Grunewald S, Tüns AI, Wardelmann E, Sicklick JK, Brahmi M, Serrano C, Schildhaus HU, Sievers S, Treckmann J, Heinrich MC, Raut CP, Ou WB, Marino-Enriquez A, George S, Rauh D, Fletcher JA, Bauer S. Mühlenberg T, et al. Among authors: sievers s. J Clin Oncol. 2024 Apr 20;42(12):1439-1449. doi: 10.1200/JCO.23.01197. Epub 2024 Feb 26. J Clin Oncol. 2024. PMID: 38408285
Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator.
Dötsch L, Davies C, Hennes E, Schönfeld J, Kumar A, Guita CDCL, Ehrler JHM, Hiesinger K, Thavam S, Janning P, Sievers S, Knapp S, Proschak E, Ziegler S, Waldmann H. Dötsch L, et al. Among authors: sievers s. J Med Chem. 2024 Mar 28;67(6):4691-4706. doi: 10.1021/acs.jmedchem.3c02245. Epub 2024 Mar 12. J Med Chem. 2024. PMID: 38470246 Free PMC article.
Illuminating Dark Chemical Matter Using the Cell Painting Assay.
Pahl A, Liu J, Patil S, Rezaei Adariani S, Schölermann B, Warmers J, Bonowski J, Koska S, Akbulut Y, Seitz C, Sievers S, Ziegler S, Waldmann H. Pahl A, et al. Among authors: sievers s. J Med Chem. 2024 Apr 30. doi: 10.1021/acs.jmedchem.4c00160. Online ahead of print. J Med Chem. 2024. PMID: 38687818
185 results