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Page 1
Covalent Lipid Pocket Ligands Targeting p38α MAPK Mutants.
Bührmann M, Hardick J, Weisner J, Quambusch L, Rauh D. Bührmann M, et al. Among authors: quambusch l. 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
Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity.
Quambusch L, Landel I, Depta L, Weisner J, Uhlenbrock N, Müller MP, Glanemann F, Althoff K, Siveke JT, Rauh D. Quambusch L, et al. Angew Chem Int Ed Engl. 2019 Dec 19;58(52):18823-18829. doi: 10.1002/anie.201909857. Epub 2019 Nov 8. Angew Chem Int Ed Engl. 2019. PMID: 31584233 Free PMC article.
An Unusual Intramolecular Halogen Bond Guides Conformational Selection.
Tesch R, Becker C, Müller MP, Beck ME, Quambusch L, Getlik M, Lategahn J, Uhlenbrock N, Costa FN, Polêto MD, Pinheiro PSM, Rodrigues DA, Sant'Anna CMR, Ferreira FF, Verli H, Fraga CAM, Rauh D. Tesch R, et al. Among authors: quambusch l. Angew Chem Int Ed Engl. 2018 Jul 26;57(31):9970-9975. doi: 10.1002/anie.201804917. Epub 2018 Jul 9. Angew Chem Int Ed Engl. 2018. PMID: 29873877
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: quambusch l. 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.
Cellular model system to dissect the isoform-selectivity of Akt inhibitors.
Quambusch L, Depta L, Landel I, Lubeck M, Kirschner T, Nabert J, Uhlenbrock N, Weisner J, Kostka M, Levy LM, Schultz-Fademrecht C, Glanemann F, Althoff K, Müller MP, Siveke JT, Rauh D. Quambusch L, et al. Nat Commun. 2021 Sep 6;12(1):5297. doi: 10.1038/s41467-021-25512-8. Nat Commun. 2021. PMID: 34489430 Free PMC article.
Covalent Allosteric Inhibitors of Akt Generated Using a Click Fragment Approach.
van der Westhuizen L, Weisner J, Taher A, Landel I, Quambusch L, Lindemann M, Uhlenbrock N, Müller MP, Green IR, Pelly SC, Rauh D, van Otterlo WAL. van der Westhuizen L, et al. Among authors: quambusch l. ChemMedChem. 2022 May 18;17(10):e202100776. doi: 10.1002/cmdc.202100776. Epub 2022 Mar 9. ChemMedChem. 2022. PMID: 35170857 Free PMC article.
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: quambusch l. 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
Spotlight on AKT: Current Therapeutic Challenges.
Landel I, Quambusch L, Depta L, Rauh D. Landel I, et al. Among authors: quambusch l. ACS Med Chem Lett. 2020 Mar 12;11(3):225-227. doi: 10.1021/acsmedchemlett.9b00548. eCollection 2020 Mar 12. ACS Med Chem Lett. 2020. PMID: 32184947 Free PMC article.