Design, synthesis, and evaluation of WD-repeat-containing protein 5 (WDR5) degraders A Dölle, B Adhikari, A Krämer, J Weckesser, N Berner, LM Berger, ... Journal of medicinal chemistry 64 (15), 10682-10710, 2021 | 62 | 2021 |
Structure-based design of selective salt-inducible kinase inhibitors R Tesch, M Rak, M Raab, LM Berger, T Kronenberger, AC Joerger, ... Journal of Medicinal Chemistry 64 (12), 8142-8160, 2021 | 30 | 2021 |
Inhibitors of the Hippo pathway kinases STK3/MST2 and STK4/MST1 have utility for the treatment of acute myeloid leukemia N Bata, A Chaikuad, NA Bakas, AS Limpert, LJ Lambert, DJ Sheffler, ... Journal of medicinal chemistry 65 (2), 1352-1369, 2021 | 26 | 2021 |
Design of a “two-in-one” mutant-selective epidermal growth factor receptor inhibitor that spans the orthosteric and allosteric sites F Wittlinger, DE Heppner, C To, M Günther, BH Shin, JK Rana, ... Journal of medicinal chemistry 65 (2), 1370-1383, 2021 | 21 | 2021 |
Single tracer-based protocol for broad-spectrum kinase profiling in live cells with NanoBRET MB Robers, JM Wilkinson, JD Vasta, LM Berger, BT Berger, S Knapp STAR protocols 2 (4), 100822, 2021 | 20 | 2021 |
A highly selective chemical probe for activin receptor-like kinases ALK4 and ALK5 T Hanke, JF Wong, BT Berger, I Abdi, LM Berger, R Tesch, C Tredup, ... ACS Chemical Biology 15 (4), 862-870, 2020 | 18 | 2020 |
A toolbox for the generation of chemical probes for baculovirus IAP repeat containing proteins MP Schwalm, LM Berger, MN Meuter, JD Vasta, CR Corona, S Röhm, ... Frontiers in cell and developmental biology 10, 886537, 2022 | 15 | 2022 |
Solution structures and biophysical analysis of full-length group A PAKs reveal they are monomeric and auto-inhibited in cis FJ Sorrell, LM Kilian, JM Elkins Biochemical Journal 476 (7), 1037-1051, 2019 | 14 | 2019 |
Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-a]pyrimidine-Based Macrocycles CG Kurz, F Preuss, A Tjaden, M Cusack, JA Amrhein, D Chatterjee, ... Journal of Medicinal Chemistry 65 (11), 7799-7817, 2022 | 12 | 2022 |
Shifting the selectivity of pyrido [2, 3-d] pyrimidin-7 (8H)-one inhibitors towards the salt-inducible kinase (SIK) subfamily M Rak, R Tesch, LM Berger, E Shevchenko, M Raab, A Tjaden, R Zhubi, ... European Journal of Medicinal Chemistry 254, 115347, 2023 | 8 | 2023 |
Design and Synthesis of Pyrazole-Based Macrocyclic Kinase Inhibitors Targeting BMPR2 JA Amrhein, G Wang, BT Berger, LM Berger, AD Kalampaliki, A Krämer, ... ACS Medicinal Chemistry Letters 14 (6), 833-840, 2023 | 7 | 2023 |
Development of potent dual BET/HDAC inhibitors via pharmacophore merging and structure-guided optimization N Bauer, DI Balourdas, JR Schneider, X Zhang, LM Berger, BT Berger, ... ACS chemical biology 19 (2), 266-279, 2024 | 6 | 2024 |
Discovery of 3-Amino-1H-pyrazole-Based Kinase Inhibitors to Illuminate the Understudied PCTAIRE Family JA Amrhein, LM Berger, A Tjaden, A Krämer, L Elson, T Tolvanen, ... International Journal of Molecular Sciences 23 (23), 14834, 2022 | 6 | 2022 |
Pharmacokinetic Optimization of Small Molecule Janus Kinase 3 Inhibitors to Target Immune Cells J Laux, M Forster, L Riexinger, A Schwamborn, J Guezguez, C Pokoj, ... ACS Pharmacology & Translational Science 5 (8), 573-602, 2022 | 6 | 2022 |
C81‐evoked inhibition of the TNFR1‐NFκB pathway during inflammatory processes for stabilization of the impaired vascular endothelial barrier for leukocytes GM Krishnathas, B Strödke, L Mittmann, T Zech, LM Berger, CA Reichel, ... The FASEB Journal 35 (6), e21656, 2021 | 5 | 2021 |
Deep Annotation of Donated Chemical Probes (DCP) in Organotypic Human Liver Cultures and Patient-Derived Organoids from Tumor and Normal Colorectum C Tredup, B Ndreshkjana, NS Schneider, A Tjaden, AM Kemas, ... ACS Chemical Biology 18 (4), 822-836, 2023 | 3 | 2023 |
Development of Selective Pyrido[2,3-d]pyrimidin-7(8H)-one-Based Mammalian STE20-Like (MST3/4) Kinase Inhibitors M Rak, A Menge, R Tesch, LM Berger, DI Balourdas, E Shevchenko, ... Journal of Medicinal Chemistry 67 (5), 3813-3842, 2024 | 2 | 2024 |
Synthesis of pyrazole-based macrocycles leads to a highly selective inhibitor for MST3 JA Amrhein, LM Berger, DI Balourdas, AC Joerger, A Menge, A Krämer, ... Journal of Medicinal Chemistry 67 (1), 674-690, 2023 | 2 | 2023 |
Back-pocket optimization of 2-aminopyrimidine-based macrocycles leads to potent EPHA2/GAK kinase inhibitors J Gerninghaus, R Zhubi, A Krämer, M Karim, DHN Tran, AC Joerger, ... Journal of Medicinal Chemistry 67 (15), 12534-12552, 2024 | 1 | 2024 |
Back-pocket optimization of 2-aminopyrimidine-based macrocycles leads to potent dual EPHA2/GAK kinase inhibitors with antiviral activity J Gerninghaus, R Zhubi, A Krämer, M Karim, AC Joerger, C Schreiber, ... bioRxiv, 2024 | | 2024 |