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Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S.
Lategahn J, Keul M, Klövekorn P, Tumbrink HL, Niggenaber J, Müller MP, Hodson L, Flaßhoff M, Hardick J, Grabe T, Engel J, Schultz-Fademrecht C, Baumann M, Ketzer J, Mühlenberg T, Hiller W, Günther G, Unger A, Müller H, Heimsoeth A, Golz C, Blank-Landeshammer B, Kollipara L, Zahedi RP, Strohmann C, Hengstler JG, van Otterlo WAL, Bauer S, Rauh D. Lategahn J, et al. Among authors: hardick j. Chem Sci. 2019 Oct 4;10(46):10789-10801. doi: 10.1039/c9sc03445e. eCollection 2019 Dec 14. Chem Sci. 2019. PMID: 31857889 Free PMC article.
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.
Kaitsiotou H, Keul M, Hardick J, Mühlenberg T, Ketzer J, Ehrt C, Krüll J, Medda F, Koch O, Giordanetto F, Bauer S, Rauh D. Kaitsiotou H, et al. Among authors: hardick j. J Med Chem. 2017 Nov 9;60(21):8801-8815. doi: 10.1021/acs.jmedchem.7b00841. Epub 2017 Oct 24. J Med Chem. 2017. PMID: 28991465
Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.
Uhlenbrock N, Smith S, Weisner J, Landel I, Lindemann M, Le TA, Hardick J, Gontla R, Scheinpflug R, Czodrowski P, Janning P, Depta L, Quambusch L, Müller MP, Engels B, Rauh D. Uhlenbrock N, et al. Among authors: hardick j. Chem Sci. 2019 Feb 13;10(12):3573-3585. doi: 10.1039/c8sc05212c. eCollection 2019 Mar 28. Chem Sci. 2019. PMID: 30996949 Free PMC article.
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
Lategahn J, Hardick J, Grabe T, Niggenaber J, Jeyakumar K, Keul M, Tumbrink HL, Becker C, Hodson L, Kirschner T, Klövekorn P, Ketzer J, Baumann M, Terheyden S, Unger A, Weisner J, Müller MP, van Otterlo WAL, Bauer S, Rauh D. Lategahn J, et al. Among authors: hardick j. J Med Chem. 2020 Oct 22;63(20):11725-11755. doi: 10.1021/acs.jmedchem.0c00870. Epub 2020 Sep 30. J Med Chem. 2020. PMID: 32931277
Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in KRAS-Mutant Pancreatic and Colorectal Cancer.
Weisner J, Landel I, Reintjes C, Uhlenbrock N, Trajkovic-Arsic M, Dienstbier N, Hardick J, Ladigan S, Lindemann M, Smith S, Quambusch L, Scheinpflug R, Depta L, Gontla R, Unger A, Müller H, Baumann M, Schultz-Fademrecht C, Günther G, Maghnouj A, Müller MP, Pohl M, Teschendorf C, Wolters H, Viebahn R, Tannapfel A, Uhl W, Hengstler JG, Hahn SA, Siveke JT, Rauh D. Weisner J, et al. Among authors: hardick j. Cancer Res. 2019 May 1;79(9):2367-2378. doi: 10.1158/0008-5472.CAN-18-2861. Epub 2019 Mar 11. Cancer Res. 2019. PMID: 30858154
Covalent Lipid Pocket Ligands Targeting p38α MAPK Mutants.
Bührmann M, Hardick J, Weisner J, Quambusch L, Rauh D. Bührmann M, et al. Among authors: hardick j. Angew Chem Int Ed Engl. 2017 Oct 16;56(43):13232-13236. doi: 10.1002/anie.201706345. Epub 2017 Sep 22. Angew Chem Int Ed Engl. 2017. PMID: 28834017
Optimization of Covalent MKK7 Inhibitors via Crude Nanomole-Scale Libraries.
Gehrtz P, Marom S, Bührmann M, Hardick J, Kleinbölting S, Shraga A, Dubiella C, Gabizon R, Wiese JN, Müller MP, Cohen G, Babaev I, Shurrush K, Avram L, Resnick E, Barr H, Rauh D, London N. Gehrtz P, et al. Among authors: hardick j. J Med Chem. 2022 Aug 11;65(15):10341-10356. doi: 10.1021/acs.jmedchem.1c02206. Epub 2022 Jul 30. J Med Chem. 2022. PMID: 35912476 Free PMC article.
99 results