Scientific Journals and Books

2024

Understanding the Cytomegalovirus Cyclin-Dependent Kinase Ortholog pUL97 as a Multifaceted Regulator and an Antiviral Drug Target

Marschall M, Schutz M, Wild M, Socher E, Wangen C, Dhotre K, Rawlinson W D and Sticht H. Cells. 2024; 13 (16): doi: 10.3390/cells13161338

Inhibition of mammalian mtDNA transcription acts paradoxically to reverse diet-induced hepatosteatosis and obesity

Jiang S, Yuan T, Rosenberger F A, Mourier A, Dragano N R V, Kremer L S, Rubalcava-Gracia D, Hansen F M, Borg M, Mennuni M, Filograna R, Alsina D, Misic J, Koolmeister C, Papadea P, de Angelis M H, Ren L, Andersson O, Unger A, Bergbrede T, Di Lucrezia R, Wibom R, Zierath J R, Krook A, Giavalisco P, Mann M and Larsson N G. Nat Metab. 2024; 6 (6): 1024-1035. doi: 10.1038/s42255-024-01038-3

Fragment-Based Interrogation of the 14-3-3/TAZ Protein-Protein Interaction

Andlovic B, Valenti D, Centorrino F, Picarazzi F, Hristeva S, Hiltmann M, Wolf A, Cantrelle F X, Mori M, Landrieu I, Levy L M, Klebl B, Tzalis D, Genski T, Eickhoff J and Ottmann C. Biochemistry. 2024; 63 (17): 2196-2206. doi: 10.1021/acs.biochem.4c00248

An Antiherpesviral Host-Directed Strategy Based on CDK7 Covalently Binding Drugs: Target-Selective, Picomolar-Dose, Cross-Virus Reactivity

Yu D, Wagner S, Schutz M, Jeon Y, Seo M, Kim J, Bruckner N, Kicuntod J, Tillmanns J, Wangen C, Hahn F, Kaufer B B, Neipel F, Eickhoff J, Klebl B, Nam K and Marschall M. Pharmaceutics. 2024; 16 (2): doi: 10.3390/pharmaceutics16020158

Profiling of ERBB receptors and downstream pathways reveals selectivity and hidden properties of ERBB4 antagonists

Popović L, Wintgens J P, Wu Y, Brankatschk B, Menninger S, Degenhart C, Jensen N, Wichert S P, Klebl B, Rossner M J and Wehr M C. iScience. 2024; doi: 10.1016/j.isci.2024.108839

Pyrrolopyrimidine based CSF1R inhibitors: Attempted departure from Flatland

Bjornstad F, Havik S, Aarhus T I, Mahdi I, Unger A, Habenberger P, Degenhart C, Eickhoff J, Klebl B M, Sundby E and Hoff B H. Eur J Med Chem. 2024; 265 116053. doi: 10.1016/j.ejmech.2023.116053

Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA

Teuber A, Schulz T, Fletcher B S, Gontla R, Muhlenberg T, Zischinsky M L, Niggenaber J, Weisner J, Kleinbolting S B, Lategahn J, Sievers S, Muller M P, Bauer S and Rauh D. Nat Commun. 2024; 15 (1): 63. doi: 10.1038/s41467-023-44376-8

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

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