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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: christ cd. 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 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. Among authors: christ cd. 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: christ cd. 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.
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: christ cd. 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: christ cd. 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: christ cd. 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
Discovery of a hidden transient state in all bromodomain families.
Raich L, Meier K, Günther J, Christ CD, Noé F, Olsson S. Raich L, et al. Among authors: christ cd. Proc Natl Acad Sci U S A. 2021 Jan 26;118(4):e2017427118. doi: 10.1073/pnas.2017427118. Proc Natl Acad Sci U S A. 2021. PMID: 33468647 Free PMC article.
24 results