2019
Kinase Chemodiversity from the Arctic: The BreitfussinsHansen K O, Andersen J H, Bayer A, Pandey S K, Lorentzen M, Jorgensen K B, Sydnes M O, Guttormsen Y, Baumann M, Koch U, Klebl B, Eickhoff J, Haug B E, Isaksson J, Hansen E H. J Med Chem. 2019; 62 (22): 10167-10181. doi: 10.1021/acs.jmedchem.9b01006
Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIßKremer L, Hennes E, Brause A, Ursu A, Robke L, Matsubayashi H T, Nihongaki Y, Flegel J, Mejdrova I, Eickhoff J, Baumann M, Nencka R, Janning P, Kordes S, Scholer H R, Sterneckert J, Inoue T, Ziegler S, Waldmann H. Angew Chem Int Ed Engl. 2019; 58 (46): 16617-16628. doi: 10.1002/anie.201907632
Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797SLategahn J, Keul M, Klovekorn P, Tumbrink H L, Niggenaber J, Muller M P, Hodson L, Flasshoff M, Hardick J, Grabe T, Engel J, Schultz-Fademrecht C, Baumann M, Ketzer J, Muhlenberg T, Hiller W, Gunther G, Unger A, Muller H, Heimsoeth A, Golz C, Blank-Landeshammer B, Kollipara L, Zahedi R P, Strohmann C, Hengstler J G, van Otterlo W A L, Bauer S, Rauh D. Chem Sci. 2019; 10 (46): 10789-10801. doi: 10.1039/c9sc03445e
Small-Molecule Inhibition of the UNC-Src Interaction Impairs Dynamic Src Localization in CellsGarivet G, Hofer W, Konitsiotis A, Klein C, Kaiser N, Mejuch T, Fansa E, Alsaabi R, Wittinghofer A, Bastiaens P I H, Waldmann H. Cell Chem Biol. 2019; 26 (6): 842-851 e847. doi: 10.1016/j.chembiol.2019.02.019
Analysis and Modelling of False Positives in GPCR AssaysGhosh D, Tetko I, Klebl B, Nussbaumer P, Koch U. ICANN 2019. 2019; 11731 767-770
Chemical Validation of DegS As a Target for the Development of Antibiotics with a Novel Mode of ActionBongard J, Schmitz A L, Wolf A, Zischinsky G, Pieren M, Schellhorn B, Bravo-Rodriguez K, Schillinger J, Koch U, Nussbaumer P, Klebl B, Steinmann J, Buer J, Sanchez-Garcia E, Ehrmann M, Kaiser M. ChemMedChem. 2019; 14 (11): 1074-1078. doi: 10.1002/cmdc.201900193
Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in KRAS-Mutant Pancreatic and Colorectal CancerWeisner 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, Muller H, Baumann M, Schultz-Fademrecht C, Gunther G, Maghnouj A, Muller M P, Pohl M, Teschendorf C, Wolters H, Viebahn R, Tannapfel A, Uhl W, Hengstler J G, Hahn S A, Siveke J T, Rauh D. Cancer Res. 2019; 79 (9): 2367-2378. doi: 10.1158/0008-5472.CAN-18-2861
Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent InhibitorsWolle P, Hardick J, Cronin S J F, Engel J, Baumann M, Lategahn J, Penninger J M, Rauh D. J Med Chem. 2019; 62 (5): 2843-2848. doi: 10.1021/acs.jmedchem.9b00102
Dual inhibition of GSK3β and CDK5 protects the cytoskeleton of neurons from neuroinflammatory-mediated degeneration in vitro and in vivoReinhardt L, Kordes S, Reinhardt P, Glatza M, Baumann M, Drexler H C A, Menninger S, Zischinsky G, Eickhoff J, Frob C, Bhattarai P, Arulmozhivarman G, Marrone L, Janosch A, Adachi K, Stehling M, Anderson E N, Abo-Rady M, Bickle M, Pandey U B, Reimer M M, Kizil C, Scholer H R, Nussbaumer P, Klebl B, Sterneckert J L. Stem Cell Reports. 2019; 12 (3): 502-517. doi: 10.1016/j.stemcr.2019.01.015
Chronic high dose P2X7 receptor inhibition exacerbates cancer-induced bone painFalk S, Appel C K, Bennedbaek H B, Al-Dihaissy T, Unger A, Dinkel K, Heegaard A M. Eur J Pharmacol. 2019; 845 48-55. doi: 10.1016/j.ejphar.2018.12.032
In vivo proof-of-concept for two experimental antiviral drugs, both directed to cellular targets, using a murine cytomegalovirus modelSonntag E, Hahn F, Bertzbach L D, Seyler L, Wangen C, Muller R, Tannig P, Grau B, Baumann M, Zent E, Zischinsky G, Eickhoff J, Kaufer B B, Bauerle T, Tsogoeva S B, Marschall M. Antiviral Res. 2019; 161 63-69. doi: 10.1016/j.antiviral.2018.11.008
