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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: karim m. 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: karim m. 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.
PIP4K2C inhibition reverses autophagic flux impairment induced by SARS-CoV-2.
Karim M, Mishra M, Lo CW, Saul S, Cagirici HB, Tran DHN, Agrawal A, Ghita L, Ojha A, East MP, Gammeltoft KA, Sahoo MK, Johnson GL, Das S, Jochmans D, Cohen CA, Gottwein J, Dye J, Neff N, Pinsky BA, Laitinen T, Pantsar T, Poso A, Zanini F, Jonghe S, Asquith CRM, Einav S. Karim M, et al. bioRxiv [Preprint]. 2024 Apr 17:2024.04.15.589676. doi: 10.1101/2024.04.15.589676. bioRxiv. 2024. PMID: 38659941 Free PMC article. Preprint.
Numb-associated kinases are required for SARS-CoV-2 infection and are cellular targets for antiviral strategies.
Karim M, Saul S, Ghita L, Sahoo MK, Ye C, Bhalla N, Lo CW, Jin J, Park JG, Martinez-Gualda B, East MP, Johnson GL, Pinsky BA, Martinez-Sobrido L, Asquith CRM, Narayanan A, De Jonghe S, Einav S. Karim M, et al. Antiviral Res. 2022 Aug;204:105367. doi: 10.1016/j.antiviral.2022.105367. Epub 2022 Jun 20. Antiviral Res. 2022. PMID: 35738348 Free PMC article.
1,798 results