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Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors.
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: ehret tal. J Med Chem. 2024 Aug 8;67(15):12534-12552. doi: 10.1021/acs.jmedchem.4c00411. Epub 2024 Jul 19. J Med Chem. 2024. PMID: 39028937
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: ehret tal. 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.
Structural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition.
Kücükdisli M, Bel-Abed H, Cirillo D, Lo WT, Efrém NL, Horatscheck A, Perepelittchenko L, Prokofeva P, Ehret TAL, Radetzki S, Neuenschwander M, Specker E, Médard G, Müller S, Wilhelm S, Kuster B, von Kries JP, Haucke V, Nazaré M. Kücükdisli M, et al. Among authors: ehret tal. J Med Chem. 2023 Oct 26;66(20):14278-14302. doi: 10.1021/acs.jmedchem.3c01319. Epub 2023 Oct 11. J Med Chem. 2023. PMID: 37819647 Free PMC article.