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

2016
Transient P2X7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy

Jimenez-Pacheco A, Diaz-Hernandez M, Arribas-Blazquez M, Sanz-Rodriguez A, Olivos-Ore L A, Artalejo A R, Alves M, Letavic M, Miras-Portugal M T, Conroy R M, Delanty N, Farrell M A, O'Brien D F, Bhattacharya A, Engel T, Henshall D C. J Neurosci. 2016; 36 (22): 5920-5932. doi: 10.1523/JNEUROSCI.4009-15.2016

Design and synthesis of DNA-encoded libraries based on a benzodiazepine and a pyrazolopyrimidine scaffold

Škopić M K, Bugain O, Jung K, Onstein S, Brandherm S, Kalliokoski T, Brunschweiger A. MedChemComm. 2016; 7 (10): 1957-1965. doi: 10.1039/c6md00243a

Characterization of RON protein isoforms in pancreatic cancer: implications for biology and therapeutics

Chakedis J, French R, Babicky M, Jaquish D, Mose E, Cheng P, Holman P, Howard H, Miyamoto J, Porras P, Walterscheid Z, Schultz-Fademrecht C, Esdar C, Schadt O, Eickhoff J, Lowy A M. Oncotarget. 2016; 7 (29): 45959-45975. doi: 10.18632/oncotarget.10009

Critical Evaluation of P2X7 Receptor Antagonists in Selected Seizure Models

Fischer W, Franke H, Krugel U, Muller H, Dinkel K, Lord B, Letavic M A, Henshall D C, Engel T. PLoS One. 2016; 11 (6): e0156468. doi: 10.1371/journal.pone.0156468

Identification of pyrazolopyridazinones as PDEδ inhibitors

Papke B, Murarka S, Vogel H A, Martin-Gago P, Kovacevic M, Truxius D C, Fansa E K, Ismail S, Zimmermann G, Heinelt K, Schultz-Fademrecht C, Al Saabi A, Baumann M, Nussbaumer P, Wittinghofer A, Waldmann H, Bastiaens P I. Nat Commun. 2016; 7 11360. doi: 10.1038/ncomms11360

The Evolving Role of the Medicinal Chemist

Lawton G, Nussbaumer P. Prog Med Chem. 2016; 55 193-226. doi: 10.1016/bs.pmch.2015.11.001