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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: hillig rc. 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.
A Novel NAMPT Inhibitor-Based Antibody-Drug Conjugate Payload Class for Cancer Therapy.
Böhnke N, Berger M, Griebenow N, Rottmann A, Erkelenz M, Hammer S, Berndt S, Günther J, Wengner AM, Stelte-Ludwig B, Mahlert C, Greven S, Dietz L, Jörißen H, Barak N, Bömer U, Hillig RC, Eberspaecher U, Weiske J, Giese A, Mumberg D, Nising CF, Weinmann H, Sommer A. Böhnke N, et al. Among authors: hillig rc. Bioconjug Chem. 2022 Jun 15;33(6):1210-1221. doi: 10.1021/acs.bioconjchem.2c00178. Epub 2022 Jun 3. Bioconjug Chem. 2022. PMID: 35658441 Free PMC article.
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.
Hillig RC, Sautier B, Schroeder J, Moosmayer D, Hilpmann A, Stegmann CM, Werbeck ND, Briem H, Boemer U, Weiske J, Badock V, Mastouri J, Petersen K, Siemeister G, Kahmann JD, Wegener D, Böhnke N, Eis K, Graham K, Wortmann L, von Nussbaum F, Bader B. Hillig RC, et al. Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2551-2560. doi: 10.1073/pnas.1812963116. Epub 2019 Jan 25. Proc Natl Acad Sci U S A. 2019. PMID: 30683722 Free PMC article.
BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe.
Günther J, Hillig RC, Zimmermann K, Kaulfuss S, Lemos C, Nguyen D, Rehwinkel H, Habgood M, Lechner C, Neuhaus R, Ganzer U, Drewes M, Chai J, Bouché L. Günther J, et al. Among authors: hillig rc. J Med Chem. 2022 Nov 10;65(21):14366-14390. doi: 10.1021/acs.jmedchem.2c00441. Epub 2022 Oct 19. J Med Chem. 2022. PMID: 36261130 Free PMC article.
Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles.
Eaton JK, Furst L, Ruberto RA, Moosmayer D, Hilpmann A, Ryan MJ, Zimmermann K, Cai LL, Niehues M, Badock V, Kramm A, Chen S, Hillig RC, Clemons PA, Gradl S, Montagnon C, Lazarski KE, Christian S, Bajrami B, Neuhaus R, Eheim AL, Viswanathan VS, Schreiber SL. Eaton JK, et al. Among authors: hillig rc. Nat Chem Biol. 2020 May;16(5):497-506. doi: 10.1038/s41589-020-0501-5. Epub 2020 Mar 30. Nat Chem Biol. 2020. PMID: 32231343 Free PMC article.
Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics.
Hillisch A, Gericke KM, Allerheiligen S, Roehrig S, Schaefer M, Tersteegen A, Schulz S, Lienau P, Gnoth M, Puetter V, Hillig RC, Heitmeier S. Hillisch A, et al. Among authors: hillig rc. J Med Chem. 2020 Nov 12;63(21):12574-12594. doi: 10.1021/acs.jmedchem.0c01035. Epub 2020 Oct 27. J Med Chem. 2020. PMID: 33108181 Free article.
Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor.
Lefranc J, Schulze VK, Hillig RC, Briem H, Prinz F, Mengel A, Heinrich T, Balint J, Rengachari S, Irlbacher H, Stöckigt D, Bömer U, Bader B, Gradl SN, Nising CF, von Nussbaum F, Mumberg D, Panne D, Wengner AM. Lefranc J, et al. Among authors: hillig rc. J Med Chem. 2020 Jan 23;63(2):601-612. doi: 10.1021/acs.jmedchem.9b01460. Epub 2020 Jan 10. J Med Chem. 2020. PMID: 31859507
35 results