Publikationen

2025
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

2022
Increased expression of the ATP-gated P2X7 receptor reduces responsiveness to anti-convulsants during status epilepticus in mice

Beamer E, Morgan J, Alves M, Menendez Mendez A, Morris G, Zimmer B, Conte G, de Diego-Garcia L, Alarcon-Vila C, Yiu Ng N K, Madden S, Calzaferri F, de Los Rios C, Garcia A G, Hamacher M, Dinkel K, Pelegrin P, Henshall D C, Nicke A, Engel T. Br J Pharmacol. 2022; 179 (12): 2986-3006. doi: 10.1111/bph.15785

A bead-based GPCR phosphorylation immunoassay for high-throughput ligand profiling and GRK inhibitor screening

Kaufmann J, Blum N K, Nagel F, Schuler A, Drube J, Degenhart C, Engel J, Eickhoff J E, Dasgupta P, Fritzwanker S, Guastadisegni M, Schulte C, Miess-Tanneberg E, Maric H M, Spetea M, Kliewer A, Baumann M, Klebl B, Reinscheid R K, Hoffmann C, Schulz S. Commun Biol. 2022; 5 (1): 1206. doi: 10.1038/s42003-022-04135-9

A cell-based chemical-genetic screen for amino acid stress response inhibitors reveals torins reverse stress kinase GCN2 signaling

Bruggenthies J B, Fiore A, Russier M, Bitsina C, Brotzmann J, Kordes S, Menninger S, Wolf A, Conti E, Eickhoff J E, Murray P J. J Biol Chem. 2022; 298 (12): 102629. doi: 10.1016/j.jbc.2022.102629

OCT4 interprets and enhances nucleosome flexibility

MacCarthy C M, Huertas J, Ortmeier C, Vom Bruch H, Tan D S, Reinke D, Sander A, Bergbrede T, Jauch R, Scholer H R, Cojocaru V. Nucleic Acids Res. 2022; 50 (18): 10311-10327. doi: 10.1093/nar/gkac755

White Paper: Mimetics of Class 2 Tumor Suppressor Proteins as Novel Drug Candidates for Personalized Cancer Therapy

Dahl E, Villwock S, Habenberger P, Choidas A, Rose M, Klebl B M. Cancers (Basel). 2022; 14 (18): doi: 10.3390/cancers14184386

Synthesis, Biological Evaluation, and Binding Mode of a New Class of Oncogenic K-Ras4b Inhibitors

Jeuken S, Shkura O, Roger M, Brickau V, Choidas A, Degenhart C, Gulden D, Klebl B, Koch U, Stoll R, Scherkenbeck J. ChemMedChem. 2022; 17 (22): e202200392. doi: 10.1002/cmdc.202200392

Blocking the Farnesyl Pocket of PDEδ Reduces Rheb-Dependent mTORC1 Activation and Survival of Tsc2-Null Cells

Armijo M E, Escalona E, Pena D, Farias A, Morin V, Baumann M, Klebl B M, Pincheira R, Castro A F. Front Pharmacol. 2022; 13 912688. doi: 10.3389/fphar.2022.912688

Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors

Lategahn J, Tumbrink H L, Schultz-Fademrecht C, Heimsoeth A, Werr L, Niggenaber J, Keul M, Parmaksiz F, Baumann M, Menninger S, Zent E, Landel I, Weisner J, Jeyakumar K, Heyden L, Russ N, Muller F, Lorenz C, Bragelmann J, Spille I, Grabe T, Muller M P, Heuckmann J M, Klebl B M, Nussbaumer P, Sos M L, Rauh D. J Med Chem. 2022; 65 (9): 6643-6655. doi: 10.1021/acs.jmedchem.1c02080

The Pseudo-Natural Product Rhonin Targets RHOGDI

Akbarzadeh M, Flegel J, Patil S, Shang E, Narayan R, Buchholzer M, Kazemein Jasemi N S, Grigalunas M, Krzyzanowski A, Abegg D, Shuster A, Potowski M, Karatas H, Karageorgis G, Mosaddeghzadeh N, Zischinsky M L, Merten C, Golz C, Brieger L, Strohmann C, Antonchick A P, Janning P, Adibekian A, Goody R S, Ahmadian M R, Ziegler S, Waldmann H. Angew Chem Int Ed Engl. 2022; 61 (18): e202115193. doi: 10.1002/anie.202115193

IMI European Lead Factory – democratizing access to high-throughput screening

Jones P S, Boucharens S, McElroy S P, Morrison A, Honarnejad S, van Boeckel S, van den Hurk H, Basting D, Huser J, Jaroch S, Ottow E, Benningshof J, Folmer R H A, Leemhuis F, Kramer-Verhulst P M, Nies V J M, Orrling K M, Rijnders T, Pfander C, Engkvist O, Pairaudeau G, Simpson P B, Ortholand J Y, Roche D, Domling A, Kuhnert S M, Roevens P W M, van Vlijmen H, van Wanrooij E J A, Verbruggen C, Nussbaumer P, Ovaa H, van der Stelt M, Simonsen K B, Tagmose L, Waldmann H, Duffy J, Finsinger D, Jurzak M, Burgess-Brown N A, Lee W H, Rutjes F, Haag H, Kallus C, Mors H, Dorval T, Lesur B, Ramon Olayo F, Hamza D, Jones G, Pearce C, Piechot A, Tzalis D, Clausen M H, Davis J, Derouane D, Vermeiren C, Kaiser M, Stockman R A, Barrault D V, Pannifer A D, Swedlow J R, Nelson A S, Orru R V A, Ruijter E, van Helden S P, Li V M, Vries T, de Vlieger J S B. Nat Rev Drug Discov. 2022; 21 (4): 245-246. doi: 10.1038/d41573-021-00196-3

Highly Accurate Filters to Flag Frequent Hitters in AlphaScreen Assays by Suggesting their Mechanism

Ghosh D, Koch U, Hadian K, Sattler M, Tetko I V. Mol Inform. 2022; 41 (3): e2100151. doi: 10.1002/minf.202100151