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

2018
Wege zu neuen Medikamenten

Nussbaumer P, Klebl B. Nachrichten aus der Chemie. 2018; 66 (10): 976-978. doi: 10.1002/nadc.20184074752

Gasdermin D plays a vital role in the generation of neutrophil extracellular traps

Sollberger G, Choidas A, Burn G L, Habenberger P, Di Lucrezia R, Kordes S, Menninger S, Eickhoff J, Nussbaumer P, Klebl B, Kruger R, Herzig A, Zychlinsky A. Sci Immunol. 2018; 3 (26): doi: 10.1126/sciimmunol.aar6689

TRPC4/TRPC5 channels mediate adverse reaction to the cancer cell cytotoxic agent (-)-Englerin A

Cheung S Y, Henrot M, Al-Saad M, Baumann M, Muller H, Unger A, Rubaiy H N, Mathar I, Dinkel K, Nussbaumer P, Klebl B, Freichel M, Rode B, Trainor S, Clapcote S J, Christmann M, Waldmann H, Abbas S K, Beech D J, Vasudev N S. Oncotarget. 2018; 9 (51): 29634-29643. doi: 10.18632/oncotarget.25659

Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as novel AXL kinase inhibitors

Szabadkai I, Torka R, Garamvolgyi R, Baska F, Gyulavari P, Boros S, Illyes E, Choidas A, Ullrich A, Orfi L. J Med Chem. 2018; 61 (14): 6277-6292. doi: 10.1021/acs.jmedchem.8b00672

Challenging Medicinal Chemistry: Ups and Downs in a Drug Discovery Project

Nussbaumer P. Chemical Monthly. 2018; 149 1191-1197

Potent anti-leukemic activity of a specific cyclin-dependent kinase 9 inhibitor in mouse models of chronic lymphocytic leukemia

Gothert J R, Imsak R, Mollmann M, Kesper S, Gobel M, Duhrsen U, Scholz A, Lucking U, Baumann M, Unger A, Schultz-Fademrecht C, Klebl B, Eickhoff J, Choidas A, Durig J. Oncotarget. 2018; 9 (41): 26353-26369. doi: 10.18632/oncotarget.25293

Modulators of 14-3-3 protein-protein interactions

Stevers L M, Sijbesma E, Botta M, MacKintosh C, Obsil T, Landrieu I, Cau Y, Wilson A J, Karawajczyk A, Eickhoff J, Davis J, Hann M, O'Mahony G, Doveston R G, Brunsveld L, Ottmann C. J Med Chem. 2018; 61 (9): 3755-3778. doi: 10.1021/acs.jmedchem.7b00574

Combined human genome-wide RNAi and metabolite analyses identify IMPDH as a host-directed target against chlamydia infection

Rother M, Gonzalez E, Teixeira da Costa A R, Wask L, Gravenstein I, Pardo M, Pietzke M, Gurumurthy R K, Angermann J, Laudeley R, Glage S, Meyer M, Chumduri C, Kempa S, Dinkel K, Unger A, Klebl B, Klos A, Meyer T F. Cell Host Microbe. 2018; 23 (5): 661-671 e668. doi: 10.1016/j.chom.2018.04.002

Identification of non-catalytic lysine residues from allosteric circuits via covalent probes

Bongard J, Lorenz M, Vetter I R, Stege P, Porfetye A T, Schmitz A L, Kaschani F, Wolf A, Koch U, Nussbaumer P, Klebl B, Kaiser M, Ehrmann M. ACS Chem Biol. 2018; 13 (5): 1307-1312. doi: 10.1021/acschembio.8b00101

Interaction of KRas4B protein with C6-ceramide containing lipid model membranes

Li L, Dwivedi M, Erwin N, Mobitz S, Nussbaumer P, Winter R. Biochim Biophys Acta Biomembr. 2018; 1860 (5): 1008-1014. doi: 10.1016/j.bbamem.2018.01.016

Identification of an (-)-Englerin A analogue which antagonizes (-)-Englerin A at TRPC1/4/5 channels

Rubaiy H N, Seitz T, Hahn S, Choidas A, Habenberger P, Klebl B, Dinkel K, Nussbaumer P, Waldmann H, Christmann M, Beech D J. Br J Pharmacol. 2018; 175 (5): 830-839. doi: 10.1111/bph.14128

Dynarrestin, a Novel Inhibitor of Cytoplasmic Dynein

Hoing S, Yeh T Y, Baumann M, Martinez N E, Habenberger P, Kremer L, Drexler H C A, Kuchler P, Reinhardt P, Choidas A, Zischinsky M L, Zischinsky G, Nandini S, Ledray A P, Ketcham S A, Reinhardt L, Abo-Rady M, Glatza M, King S J, Nussbaumer P, Ziegler S, Klebl B, Schroer T A, Scholer H R, Waldmann H, Sterneckert J. Cell Chem Biol. 2018; 25 (4): 357-369 e356. doi: 10.1016/j.chembiol.2017.12.014

SAMHD1 is recurrently mutated in T-cell prolymphocytic leukemia

Johansson P, Klein-Hitpass L, Choidas A, Habenberger P, Mahboubi B, Kim B, Bergmann A, Scholtysik R, Brauser M, Lollies A, Siebert R, Zenz T, Duhrsen U, Kuppers R, Durig J. Blood Cancer J. 2018; 8 (1): 11. doi: 10.1038/s41408-017-0036-5