Scientific Journals and Books

2025

Highly potent quinoxalinediones inhibit alpha-hemolysin and ameliorate Staphylococcus aureus lung infections

Shekhar A, Di Lucrezia R, Jerye K, Korotkov V S, Harmrolfs K, Rox K, Weich H A, Ghai I, Delhommel F, Becher I, Degenhart C, Fansa E, Unger A, Habenberger P, Klebl B, Lukat P, Schmelz S, Henke S, Borgert S, Lang J C, Sasse F, Diestel R, Richter C, Schneider-Daum N, Hinkelmann B, Niemz J, Lehr C M, Jansch L, Huehn J, Alm R, Savitski M, Welte T, Hesterkamp T, Sattler M, Winterhalter M, Blankenfeldt W, Medina E, Bilitewski U, Dinkel K and Bronstrup M. Cell Host Microbe. 2025; 33 (4): 560-572 e521. doi: 10.1016/j.chom.2025.03.006

The P2X7R-antagonist AFC-5128 ameliorates chronic experimental autoimmune encephalomyelitis in a preventive and therapeutic paradigm

Hoffrogge R, Karachunskaya A, Heitmann N, Pedreiturria X, Kloster K, Bader V, Winklhofer K F, Hamacher M, Klebl B, Gold R, Dinkel K, Kleiter I and Faissner S. Front Immunol. 2025; 16 1554999. doi: 10.3389/fimmu.2025.1554999

Design and Synthesis of Pyridine-Based Pyrrolo[2,3-d]pyrimidine Analogs as CSF1R Inhibitors: Molecular Hybridization and Scaffold Hopping Approach

Cherukupalli S, Degenhart C, Habenberger P, Unger A, Eickhoff J, Hoff B H and Sundby E. Pharmaceuticals. 2025; 18 (6): doi: 10.3390/ph18060814

RECQL4 affects MHC class II-mediated signalling and favours an immune-evasive signature that limits response to immune checkpoint inhibitor therapy in patients with malignant melanoma

Egea-Rodriguez S, Varaljai R, Nordmann T M, Lubis R, Philip M, Rambow F, Roesch A, Flaig M, Horn S, Stoll R, Zhao F, Paschen A, Klebl B, Hickson I D, Schadendorf D, Mann M and Helfrich I. Clin Transl Med. 2025; 15 (1): e70094. doi: 10.1002/ctm2.70094

P2X7R antagonism suppresses long-lasting hyperexcitability following traumatic brain injury in mice

Alves M, de Diego-Garcia L, Vegliante G, Moreno O, Gil B, Ramos-Cabrer P, Mitra M, Fernandez Martin A, Menendez Mendez A, Wang Y, Ryzwesky Strogulsky N, Sun M, Melia C, Conte G, Plaza-Garcia S, Khalin I, Teng X, Plesnila N, Klebl B, Dinkel K, Hamacher M, Bhattarcharya A, Ceusters M, Palmer J, Loane D, Llop J, Henshall D and Engel T. Theranostics. 2025; 15 (4): 1399-1419. doi: 10.7150/thno.97254

2019

Kinase Chemodiversity from the Arctic: The Breitfussins

Hansen 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 PI4KIIIß

Kremer 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/C797S

Lategahn 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 Cells

Garivet 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 Assays

Ghosh 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 Action

Bongard 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 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, 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 Inhibitors

Wolle 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 vivo

Reinhardt 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 pain

Falk 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 model

Sonntag 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

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