Scientific Journals and Books

2019
Chronic high dose P2X7 receptor inhibition exacerbates cancer-induced bone pain

Falk S, Appel CK, Bennedbæk HB, Al-Dihaissy T, Unger A, Dinkel K, Heegaard AM. Eur J Pharmacol. 2019 Feb 15;845:48-55

Chemical Validation of DegS As a Target for the Development of Antibiotics with a Novel Mode of Action

Bongard J, Schmitz AL, 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 Jun 5;14(11):1074-1078.

Kinase Chemodiversity from the Arctic: The Breitfussins

Hansen KØ, Andersen JH, Bayer A, Pandey SK, Lorentzen M, Jørgensen KB, Sydnes MO, Guttormsen Y, Baumann M, Koch U, Klebl B, Eickhoff J, Haug BE, Isaksson J, Hansen EH. J Med Chem. 2019 Nov 27;62(22):10167-10181.

Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß

Kremer L, Hennes E, Brause A, Ursu A, Robke L, Matsubayashi HT, Nihongaki Y, Flegel J, Mejdrová I, Eickhoff J, Baumann M, Nencka R, Janning , Kordes S, Schöler HR, Sterneckert J, Inoue T, Ziegler S, Waldmann H. Angew Chem Int Ed Engl. 2019 Nov 11;58(46):16617-16628.

In vivo proof-of-concept for two experimental antiviral drugs, both directed to cellular targets, using a murine cytomegalovirus model

Sonntag E, Hahn F, Bertzbach LD, Seyler L, Wangen C, Müller R, Tannig P, Grau B, Baumann M, Zent E, Zischinsky G, Eickhoff J, Kaufer BB, Bäuerle T, Tsogoeva SB, Marschall M. Antiviral Res. 2019 Jan;161:63-69.

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. Chem Sci. 2019 Oct 4;10(46):10789-10801.

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 J, Hahn SA, Siveke JT, Rauh D. Cancer Res. 2019 May 1;79(9):2367-2378.

Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors

Wolle P, Hardick J, Cronin SJF, Engel J, Baumann M, Lategahn J, Penninger JM, Rauh D. J Med Chem. 2019 Mar 14;62(5):2843-2848.

Small-Molecule Inhibition of the UNC-Src Interaction Impairs Dynamic Src Localization in Cells

Garivet G, Hofer W, Konitsiotis A, Klein C, Kaiser N, Mejuch T, Fansa E, Alsaabi R, Wittinghofer A, Bastiaens PIH, Waldmann H. Cell Chem Biol. 2019 Jun 20;26(6):842-851.

Analysis and Modelling of False Positives in GPCR Assays

Ghosh D, Tetko I, Klebl B, Nussbaumer P, Koch U. International Conference on Artificial Neural Networks 2019, 764-770.

2018
In vivo proof-of-concept for two experimental antiviral drugs, both directed to cellular targets, using a murine cytomegalovirus model

Sonntag E, Hahn F, Bertzbach LD, Seyler L, Wangen C, Müller R, Tannig P, Grau B, Baumann M, Zent E, Zischinsky G, Eickhoff J, Kaufer BB, Bäuerle T, Tsogoeva SB, Marschall M. Antiviral Res. 2018 Nov 17; 161:63-69.

PMID: 30452929.

Wege zu neuen Medikamenten

Nussbaumer P, Klebl B.

Nachrichten der Chemie 2018, 66, 976-978

Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as novel AXL kinase inhibitors

Szabadkai I, Torka R, Garamvölgyi R, Baska F, Gyulavári P, Boros S, Illyés E, Choidas A, Ullrich A, Őrfi L. J Med Chem. 2018 Jul 26;61(14):6277-6292.

Gasdermin D plays a vital role in the generation of neutrophil extracellular traps

Sollberger G, Choidas A, Burn GL, Habenberger P, Di Lucrezia R, Kordes S, Menninger S, Eickhoff J, Nussbaumer P, Klebl B, Krüger R, Herzig A, Zychlinsky A. Science Immunology 2018, 3, eaar6689.

TRPC4/TRPC5 channels mediate adverse reaction to the cancer cell cytotoxic agent (-)-Englerin A

Cheung SY, Henrot M, Al-Saad M, Baumann M, Muller H, Unger A, Rubaiy HN, Mathar I, Dinkel K, Nussbaumer P, Klebl B, Freichel M, Rode B, Trainor S, Clapcote SJ, Christmann M, Waldmann H, Abbas SK, Beech DJ, Vasudev NS.

Oncotarget 2018, 9 (51), 29634-29643.

Link to publication

Potent anti-leukemic activity of a specific cyclin-dependent kinase 9 inhibitor in mouse models of chronic lymphocytic leukemia

Göthert JR, Imsak R, Möllmann M, Kesper S, Göbel M, Dührsen U, Scholz A, Lücking U, Baumann M, Unger A, Schultz-Fademrecht C, Klebl B, Eickhoff J, Choidas A, Dürig J. Oncotarget. 2018 May 29;9(41):26353-26369.

Link to publication

Modulators of 14-3-3 protein-protein interactions

Stevers LM, Sijbesma E, Botta M, MacKintosh C, Obsil T, Landrieu I, Cau Y, Wilson AJ, Karawajczyk A, Eickhoff J, Davis J, Hann M, O’Mahony G, Doveston RG, Brunsveld L, Ottmann C. J Med Chem.

2018 May 10;61(9):3755-3778.
Link to publication

Combined human genome-wide RNAi and metabolite analyses identify IMPDH as a host-directed target against chlamydia infection

Rother M, Gonzalez E, Teixeira da Costa AR, Wask L, Gravenstein I, Pardo M, Pietzke M, Gurumurthy RK, Angermann J, Laudeley R, Glage S, Meyer M, Chumduri C, Kempa S, Dinkel K, Unger A, Klebl B, Klos A, Meyer TF.

Cell Host Microbe. 2018 May 9;23(5):661-671.e8.

Challenging Medicinal Chemistry: Ups and Downs in a Drug Discovery Project

Nussbaumer P.

Chemical Monthly 2018, 149 (7), 1191–1197

Identification of non-catalytic lysine residues from allosteric circuits via covalent probes

Bongard J, Lorenz M, Vetter IR, Stege P, Porfetye AT, Schmitz AL, Kaschani F, Wolf A, Koch U, Nussbaumer P, Klebl B, Kaiser M, Ehrmann M.

ACS Chem. Biol. 2018, 13 (5), 1307-1312.