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Back-pocket optimization of 2-aminopyrimidine-based macrocycles leads to potent dual EPHA2/GAK kinase inhibitors with antiviral activity.
Gerninghaus J, Zhubi R, Krämer A, Karim M, Tran DHN, Joerger AC, Schreiber C, Berger LM, Berger BT, Ehret TAL, Elson L, Lenz C, Saxena K, Müller S, Einav S, Knapp S, Hanke T. Gerninghaus J, et al. Among authors: berger bt. bioRxiv [Preprint]. 2024 Feb 18:2024.02.18.580805. doi: 10.1101/2024.02.18.580805. bioRxiv. 2024. Update in: J Med Chem. 2024 Aug 8;67(15):12534-12552. doi: 10.1021/acs.jmedchem.4c00411. PMID: 38405908 Free PMC article. Updated. Preprint.
Selective targeting of the αC and DFG-out pocket in p38 MAPK.
Röhm S, Schröder M, Dwyer JE, Widdowson CS, Chaikuad A, Berger BT, Joerger AC, Krämer A, Harbig J, Dauch D, Kudolo M, Laufer S, Bagley MC, Knapp S. Röhm S, et al. Among authors: berger bt. Eur J Med Chem. 2020 Dec 15;208:112721. doi: 10.1016/j.ejmech.2020.112721. Epub 2020 Aug 20. Eur J Med Chem. 2020. PMID: 33035818
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
Tesch R, Rak M, Raab M, Berger LM, Kronenberger T, Joerger AC, Berger BT, Abdi I, Hanke T, Poso A, Strebhardt K, Sanhaji M, Knapp S. Tesch R, et al. Among authors: berger lm, berger bt. J Med Chem. 2021 Jun 24;64(12):8142-8160. doi: 10.1021/acs.jmedchem.0c02144. Epub 2021 Jun 4. J Med Chem. 2021. PMID: 34086472
Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe.
Röhm S, Berger BT, Schröder M, Chatterjee D, Mathea S, Joerger AC, Pinkas DM, Bufton JC, Tjaden A, Kovooru L, Kudolo M, Pohl C, Bullock AN, Müller S, Laufer S, Knapp S. Röhm S, et al. Among authors: berger bt. J Med Chem. 2021 Sep 23;64(18):13451-13474. doi: 10.1021/acs.jmedchem.1c00868. Epub 2021 Sep 10. J Med Chem. 2021. PMID: 34506142
Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-a]pyrimidine-Based Macrocycles.
Kurz CG, Preuss F, Tjaden A, Cusack M, Amrhein JA, Chatterjee D, Mathea S, Berger LM, Berger BT, Krämer A, Weller M, Weiss T, Müller S, Knapp S, Hanke T. Kurz CG, et al. Among authors: berger lm, berger bt. J Med Chem. 2022 Jun 9;65(11):7799-7817. doi: 10.1021/acs.jmedchem.2c00173. Epub 2022 May 24. J Med Chem. 2022. PMID: 35608370
A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins.
Schwalm MP, Berger LM, Meuter MN, Vasta JD, Corona CR, Röhm S, Berger BT, Farges F, Beinert SM, Preuss F, Morasch V, Rogov VV, Mathea S, Saxena K, Robers MB, Müller S, Knapp S. Schwalm MP, et al. Among authors: berger lm, berger bt. Front Cell Dev Biol. 2022 May 26;10:886537. doi: 10.3389/fcell.2022.886537. eCollection 2022. Front Cell Dev Biol. 2022. PMID: 35721509 Free PMC article.
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