Scientific Journals and Books

2023
Assessment of Covalently Binding Warhead Compounds in the Validation of the Cytomegalovirus Nuclear Egress Complex as an Antiviral Target

Tillmanns J, Hage S, Borst E M, Wardin J, Eickhoff J, Klebl B, Wagner S, Wangen C, Hahn F, Socher E, Marschall M. Cells. 2023; 12 (8): doi: 10.3390/cells12081162

Cytomegalovirus Cyclin-Dependent Kinase Ortholog Vcdk/Pul97 Undergoes Regulatory Interaction with Human Cyclin H and Cdk7 to Codetermine Viral Replication Efficiency

Schutz M, Wangen C, Sommerer M, Kogler M, Eickhoff J, Degenhart C, Klebl B, Naing Z, Egilmezer E, Hamilton S T, Rawlinson W D, Sticht H, Marschall M. Virus Res. 2023; 335 199200. doi: 10.1016/j.virusres.2023.199200

Characterization of the Antibacterial Activity of Quinone-Based Compounds Originating from the Alnumycin Biosynthetic Gene Cluster of a Streptomyces Isolate

Sagurna L, Heinrich S, Kaufmann L S, Ruckert-Reed C, Busche T, Wolf A, Eickhoff J, Klebl B, Kalinowski J, Bandow J E. Antibiotics (Basel). 2023; 12 (7): doi: 10.3390/antibiotics12071116

A Reinvestigation of the Role of the Sorbic Acid Tail on the Antibacterial and Anti-Tuberculosis Properties of Moiramide B

Kollmorgen I, Bachmann N, Dal Molin M, Degenhart C, Zent E, Pareek V, Koch U, Rybniker J, Metzler-Nolte N, Stoll R, Klebl B, Bandow J E, Scherkenbeck J. ChemMedChem. 2023; 18 (11): e202200631. doi: 10.1002/cmdc.202200631

Functional Expression of the Atp-Gated P2x7 Receptor in Human Ipsc-Derived Astrocytes

Kesavan J, Watters O, de Diego-Garcia L, Mendez A M, Alves M, Dinkel K, Hamacher M, Prehn J H M, Henshall D C, Engel T. Purinergic Signal. 2023; doi: 10.1007/s11302-023-09957-8

Inhibiting the Glycerophosphodiesterase Edi3 in Er-Her2+ Breast Cancer Cells Resistant to Her2-Targeted Therapy Reduces Viability and Tumour Growth

Keller M, Rohlf K, Glotzbach A, Leonhardt G, Luke S, Derksen K, Demirci O, Gocener D, AlWahsh M, Lambert J, Lindskog C, Schmidt M, Brenner W, Baumann M, Zent E, Zischinsky M L, Hellwig B, Madjar K, Rahnenfuhrer J, Overbeck N, Reinders J, Cadenas C, Hengstler J G, Edlund K, Marchan R. J Exp Clin Cancer Res. 2023; 42 (1): 25. doi: 10.1186/s13046-022-02578-w

Ifn-α Primes Cancer Cells for Fusicoccin-Induced Cell Death Via 14-3-3 Ppi Stabilization

Andlovic B, Heilmann G, Ninck S, Andrei S A, Centorrino F, Higuchi Y, Kato N, Brunsveld L, Arkin M, Menninger S, Choidas A, Wolf A, Klebl B, Kaschani F, Kaiser M, Eickhoff J, Ottmann C. Cell Chem Biol. 2023; 30 (6): 573-590 e576. doi: 10.1016/j.chembiol.2023.04.005

Negishi Cross‐Coupling in the Preparation of Benzyl Substituted Pyrrolo[2,3‐D]Pyrimidine Based Csf1r Inhibitors

Aarjus T I, Teksum V, Unger A, Habenberger P, Wolf A, Eickhoff J, Klebl B, Wolowczyk C, Bjorkoy G, Sundby E, Hoff B H. European Journal of Organic Chemistry. 2023; 26 (12): 93-104. doi: 10.1002/ejoc.202300052

A Highly Selective Purine-Based Inhibitor of Csf1r Potently Inhibits Osteoclast Differentiation

Aarhus T I, Eickhoff J, Klebl B, Unger A, Boros J, Choidas A, Zischinsky M L, Wolowczyk C, Bjorkoy G, Sundby E, Hoff B H. Eur J Med Chem. 2023b; 255 115344. doi: 10.1016/j.ejmech.2023.115344

Synthesis and Development of Highly Selective Pyrrolo[2,3-d]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form

Aarhus TI, Bjornstad F, Wolowczyk C, Larsen KU, Rognstad L., Leithaug T., Unger A., Habenberger P, Wolf A, Bjorkoy G, Pridans C, Eickhoff J, Klebl B, Hoff BH, Sundby E. J Med Chem. 2023 May 25; 66(10), 6959-6980. doi: 10.1021/acs.jmedchem.3c00428.

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