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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: bauser m. SLAS Discov. 2021 Sep;26(8):947-960. doi: 10.1177/24725552211019409. Epub 2021 Jun 21. SLAS Discov. 2021. PMID: 34154424 Free 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 D, Lemos C, Wortmann L, Eis K, Holton SJ, Boemer U, Moosmayer D, Eberspaecher U, Weiske J, Lechner C, Prechtl S, Suelzle D, Siegel F, Prinz F, Lesche R, Nicke B, Nowak-Reppel K, Himmel H, Mumberg D, von Nussbaum F, Nising CF, Bauser M, Haegebarth A. Nguyen D, et al. Among authors: bauser m. J Med Chem. 2019 Jan 24;62(2):928-940. doi: 10.1021/acs.jmedchem.8b01606. Epub 2019 Jan 9. J Med Chem. 2019. PMID: 30563338
Computationally Empowered Workflow Identifies Novel Covalent Allosteric Binders for KRASG12C.
Mortier J, Friberg A, Badock V, Moosmayer D, Schroeder J, Steigemann P, Siegel F, Gradl S, Bauser M, Hillig RC, Briem H, Eis K, Bader B, Nguyen D, Christ CD. Mortier J, et al. Among authors: bauser m. ChemMedChem. 2020 May 19;15(10):827-832. doi: 10.1002/cmdc.201900727. Epub 2020 Apr 1. ChemMedChem. 2020. PMID: 32237114 Free PMC 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 L, Bräuer N, Holton SJ, Irlbacher H, Weiske J, Lechner C, Meier R, Karén J, Siöberg CB, Pütter V, Christ CD, Ter Laak A, Lienau P, Lesche R, Nicke B, Cheung SH, Bauser M, Haegebarth A, von Nussbaum F, Mumberg D, Lemos C. Wortmann L, et al. Among authors: bauser m. J Med Chem. 2021 Nov 11;64(21):15883-15911. doi: 10.1021/acs.jmedchem.1c01245. Epub 2021 Oct 26. J Med Chem. 2021. PMID: 34699202 Free article.
The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models.
Lemos C, Schulze VK, Baumgart SJ, Nevedomskaya E, Heinrich T, Lefranc J, Bader B, Christ CD, Briem H, Kuhnke LP, Holton SJ, Bömer U, Lienau P, von Nussbaum F, Nising CF, Bauser M, Hägebarth A, Mumberg D, Haendler B. Lemos C, et al. Among authors: bauser m. Cell Oncol (Dordr). 2021 Jun;44(3):581-594. doi: 10.1007/s13402-020-00584-8. Epub 2021 Jan 25. Cell Oncol (Dordr). 2021. PMID: 33492659
The novel dihydroorotate dehydrogenase (DHODH) inhibitor BAY 2402234 triggers differentiation and is effective in the treatment of myeloid malignancies.
Christian S, Merz C, Evans L, Gradl S, Seidel H, Friberg A, Eheim A, Lejeune P, Brzezinka K, Zimmermann K, Ferrara S, Meyer H, Lesche R, Stoeckigt D, Bauser M, Haegebarth A, Sykes DB, Scadden DT, Losman JA, Janzer A. Christian S, et al. Among authors: bauser m. Leukemia. 2019 Oct;33(10):2403-2415. doi: 10.1038/s41375-019-0461-5. Epub 2019 Apr 2. Leukemia. 2019. PMID: 30940908
Donated chemical probes for open science.
Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A. Müller S, et al. Among authors: bauser m. Elife. 2018 Apr 20;7:e34311. doi: 10.7554/eLife.34311. Elife. 2018. PMID: 29676732 Free PMC article.
Novel Class of Potent and Cellularly Active Inhibitors Devalidates MTH1 as Broad-Spectrum Cancer Target.
Ellermann M, Eheim A, Rahm F, Viklund J, Guenther J, Andersson M, Ericsson U, Forsblom R, Ginman T, Lindström J, Silvander C, Trésaugues L, Giese A, Bunse S, Neuhaus R, Weiske J, Quanz M, Glasauer A, Nowak-Reppel K, Bader B, Irlbacher H, Meyer H, Queisser N, Bauser M, Haegebarth A, Gorjánácz M. Ellermann M, et al. Among authors: bauser m. ACS Chem Biol. 2017 Aug 18;12(8):1986-1992. doi: 10.1021/acschembio.7b00370. Epub 2017 Jul 12. ACS Chem Biol. 2017. PMID: 28679043 Free article.
Creation of a Novel Class of Potent and Selective MutT Homologue 1 (MTH1) Inhibitors Using Fragment-Based Screening and Structure-Based Drug Design.
Rahm F, Viklund J, Trésaugues L, Ellermann M, Giese A, Ericsson U, Forsblom R, Ginman T, Günther J, Hallberg K, Lindström J, Persson LB, Silvander C, Talagas A, Díaz-Sáez L, Fedorov O, Huber KVM, Panagakou I, Siejka P, Gorjánácz M, Bauser M, Andersson M. Rahm F, et al. Among authors: bauser m. J Med Chem. 2018 Mar 22;61(6):2533-2551. doi: 10.1021/acs.jmedchem.7b01884. Epub 2018 Mar 7. J Med Chem. 2018. PMID: 29485874
31 results