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Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
Ong HW, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin M, Galal KA, Willis C, Krämer A, Liu S, Knapp S, Derbyshire ER, Zutshi R, Drewry DH. Ong HW, et al. Among authors: kramer a. Eur J Med Chem. 2023 Mar 5;249:115043. doi: 10.1016/j.ejmech.2022.115043. Epub 2022 Dec 30. Eur J Med Chem. 2023. PMID: 36736152 Free PMC article.
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity in Vivo Mouse Model.
Fromont C, Atzori A, Kaur D, Hashmi L, Greco G, Cabanillas A, Nguyen HV, Jones DH, Garzón M, Varela A, Stevenson B, Iacobini GP, Lenoir M, Rajesh S, Box C, Kumar J, Grant P, Novitskaya V, Morgan J, Sorrell FJ, Redondo C, Kramer A, Harris CJ, Leighton B, Vickers SP, Cheetham SC, Kenyon C, Grabowska AM, Overduin M, Berditchevski F, Weston CJ, Knapp S, Fischer PM, Butterworth S. Fromont C, et al. Among authors: kramer a. J Med Chem. 2020 Jul 9;63(13):6784-6801. doi: 10.1021/acs.jmedchem.9b01803. Epub 2020 Jun 22. J Med Chem. 2020. PMID: 32433887 Free PMC article.
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: kramer a. 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
Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis.
Wanior M, Preuss F, Ni X, Krämer A, Mathea S, Göbel T, Heidenreich D, Simonyi S, Kahnt AS, Joerger AC, Knapp S. Wanior M, et al. Among authors: kramer a. J Med Chem. 2020 Dec 10;63(23):14680-14699. doi: 10.1021/acs.jmedchem.0c01242. Epub 2020 Nov 20. J Med Chem. 2020. PMID: 33216538
Development of a potent and selective chemical probe for the pleiotropic kinase CK2.
Wells CI, Drewry DH, Pickett JE, Tjaden A, Krämer A, Müller S, Gyenis L, Menyhart D, Litchfield DW, Knapp S, Axtman AD. Wells CI, et al. Among authors: kramer a. Cell Chem Biol. 2021 Apr 15;28(4):546-558.e10. doi: 10.1016/j.chembiol.2020.12.013. Epub 2021 Jan 22. Cell Chem Biol. 2021. PMID: 33484635 Free PMC article.
Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders.
Dölle A, Adhikari B, Krämer A, Weckesser J, Berner N, Berger LM, Diebold M, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Gebel J, Löhr F, Dötsch V, Eilers M, Heinzlmeir S, Kuster B, Sotriffer C, Wolf E, Knapp S. Dölle A, et al. Among authors: kramer a. J Med Chem. 2021 Aug 12;64(15):10682-10710. doi: 10.1021/acs.jmedchem.1c00146. Epub 2021 May 13. J Med Chem. 2021. PMID: 33980013
3,088 results