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Glucocorticoid activation by HSD11B1 limits T cell-driven interferon signaling and response to PD-1 blockade in melanoma.
Martins Nascentes Melo L, Herrera-Rios D, Hinze D, Löffek S, Oezel I, Turiello R, Klein J, Leonardelli S, Westedt IV, Al-Matary Y, Egea-Rodriguez S, Brenzel A, Bau M, Sucker A, Hadaschik E, Wirsdörfer F, Hanenberg H, Uhlenbrock N, Rauh D, Poźniak J, Rambow F, Marine JC, Effern M, Glodde N, Schadendorf D, Jablonska J, Hölzel M, Helfrich I. Martins Nascentes Melo L, et al. Among authors: uhlenbrock n. J Immunother Cancer. 2023 Apr 7;11(4):e004150. doi: 10.1136/jitc-2021-004150. J Immunother Cancer. 2023. PMID: 37028818 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: uhlenbrock n. 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
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. Among authors: uhlenbrock n. 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: uhlenbrock n. ChemMedChem. 2022 May 18;17(10):e202100776. doi: 10.1002/cmdc.202100776. Epub 2022 Mar 9. ChemMedChem. 2022. PMID: 35170857 Free PMC article.
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. Among authors: uhlenbrock n. 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.
Inhibition of Tumor VEGFR2 Induces Serine 897 EphA2-Dependent Tumor Cell Invasion and Metastasis in NSCLC.
Volz C, Breid S, Selenz C, Zaplatina A, Golfmann K, Meder L, Dietlein F, Borchmann S, Chatterjee S, Siobal M, Schöttle J, Florin A, Koker M, Nill M, Ozretić L, Uhlenbrock N, Smith S, Büttner R, Miao H, Wang B, Reinhardt HC, Rauh D, Hallek M, Acker-Palmer A, Heukamp LC, Ullrich RT. Volz C, et al. Among authors: uhlenbrock n. Cell Rep. 2020 Apr 28;31(4):107568. doi: 10.1016/j.celrep.2020.107568. Cell Rep. 2020. PMID: 32348765 Free article.
Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.
Engel J, Richters A, Getlik M, Tomassi S, Keul M, Termathe M, Lategahn J, Becker C, Mayer-Wrangowski S, Grütter C, Uhlenbrock N, Krüll J, Schaumann N, Eppmann S, Kibies P, Hoffgaard F, Heil J, Menninger S, Ortiz-Cuaran S, Heuckmann JM, Tinnefeld V, Zahedi RP, Sos ML, Schultz-Fademrecht C, Thomas RK, Kast SM, Rauh D. Engel J, et al. Among authors: uhlenbrock n. J Med Chem. 2015 Sep 10;58(17):6844-63. doi: 10.1021/acs.jmedchem.5b01082. Epub 2015 Aug 31. J Med Chem. 2015. PMID: 26275028
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: uhlenbrock n. 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