Scientific Journals and Books

2022
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 Jan 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 Nov 9;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
Brüggenthies J B, Fiore A, Russier M, Bitsina C, Brötzmann J, Kordes S, Menninger S, Wolf A, Conti E, Eickhoff Jan E, Murray Peter J J Biol Chem. 2022 Oct 20;102629. doi: 10.1016/j.jbc.2022.102629.
OCT4 interprets and enhances nucleosome flexibility
MacCarthy Caitlin M, Huertas J, Ortmeier C, Vom Bruch H, Tan Daisylyn S, Reinke D, Sander A, Bergbrede T, Jauch R, Schöler Hans R, Cojocaru V Nucleic Acids Res. 2022 Oct 14;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 Bert M Cancers (Basel). 2022 Sep 9;14(18):4386. doi: 10.3390/cancers14184386.
Synthesis, Biological Evaluation, and Binding Mode of a New Class of Oncogenic K-Ras4b Inhibitors
Jeuken S, Shkura O, Röger M, Brickau V, Choidas A, Degenhart C , Gülden D, Klebl B, Koch U, Stoll R, Scherkenbeck J ChemMedChem. 2022 Aug 18;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, Peña D, Farias A, Morin V, Baumann M, Klebl B M, Pincheira R, Castro A F Front Pharmacol. 2022 Jun 23;13:912688. doi: 10.3389/fphar.2022.912688. eCollection 2022.
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, Müller F, Lorenz C, Brägelmann J, Spille I, Grabe T, P Müller M, Heuckmann J M, Klebl Bert M, Nussbaumer P, Sos M L, Rauh D J Med Chem. 2022 Apr 29. 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 NS, Grigalunas M, Krzyzanowski A, Abegg D, Shuster A, Potowski M, Karatas H, Karageorgis G, Mosaddeghzadeh N, Zischinsky M, Merten C, Golz C, Brieger L, Strohmann C, Antonchick SP, Janning P, Adibekian A, Goody RS, Ahmadian MR, Ziegler S, Waldmann H. Angew Chem Int Ed Engl. 2022 Apr 25;61(18):e202112193.
IMI European Lead Factory – democratizing access to high-throughput screening
Jones PS, Boucharens S, McElroy SP, Morrison A, Honarnejad S, van Boeckel S, van den Hurk S, Basting D, Hüser J, Jaroch S, Ottow E, Benningshof J, Folmer RHA, Leemhuis F, Kramer-Verhulst PM, Nies VJM, Orrling KM, Rijnders T, Pfander C, Engkvist O, Pairaudeau G, Simpson PB, Ortholand J, Roche D, Dömling A, Kühnert SM, Roevens PWM, van Vlijmen H, van Wanrooij EJA, Verbruggen C, Nussbaumer P, Ovaa H, van der Stelt M, Simonsen KB, Tagmose L, Waldmann H, Duffy J, Finsinger D, Jurzak M, Burgess-Brown NA, Lee WH, Rutjes FPJT, Haag H, Kallus C, Mors H, Dorval T, Lesur B, Olayo FR, Hamza D, Jones G, Pearce C, Piechot A, Tzalis D, Clausen MH, Davis J, Derouane D, Vermeiren C, Kaiser M, Stockman RA, Barrault DV, Pannifer AD, Swedlow JR, Nelson AS, Orru RVA, Ruijter E, van Helden SP, Li VM, Vries T, de Vlieger JSB. Nat Rev Drug Discov. 2022 Apr;21(4):245-246.
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 Mar;41(3):e2100151.
2018
In vivo proof-of-concept for two experimental antiviral drugs, both directed to cellular targets, using a murine cytomegalovirus model
Sonntag E, Hahn F, Bertzbach LD, Seyler L, Wangen C, Müller R, Tannig P, Grau B, Baumann M, Zent E, Zischinsky G, Eickhoff J, Kaufer BB, Bäuerle T, Tsogoeva SB, Marschall M. Antiviral Res. 2018 Nov 17; 161:63-69. PMID: 30452929.
Wege zu neuen Medikamenten
Nussbaumer P, Klebl B. Nachrichten der Chemie 2018, 66, 976-978
Gasdermin D plays a vital role in the generation of neutrophil extracellular traps
Sollberger G, Choidas A, Burn GL, Habenberger P, Di Lucrezia R, Kordes S, Menninger S, Eickhoff J, Nussbaumer P, Klebl B, Krüger R, Herzig A, Zychlinsky A. Science Immunology 2018, 3, eaar6689.
TRPC4/TRPC5 channels mediate adverse reaction to the cancer cell cytotoxic agent (-)-Englerin A
Cheung SY, Henrot M, Al-Saad M, Baumann M, Muller H, Unger A, Rubaiy HN, Mathar I, Dinkel K, Nussbaumer P, Klebl B, Freichel M, Rode B, Trainor S, Clapcote SJ, Christmann M, Waldmann H, Abbas SK, Beech DJ, Vasudev NS. Oncotarget 2018, 9 (51), 29634-29643.
Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as novel AXL kinase inhibitors
Szabadkai I, Torka R, Garamvölgyi R, Baska F, Gyulavári P, Boros S, Illyés E, Choidas A, Ullrich A, Őrfi L. J Med Chem. 2018 Jul 26;61(14):6277-6292.
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
Göthert JR, Imsak R, Möllmann M, Kesper S, Göbel M, Dührsen U, Scholz A, Lücking U, Baumann M, Unger A, Schultz-Fademrecht C, Klebl B, Eickhoff J, Choidas A, Dürig J. Oncotarget. 2018 May 29;9(41):26353-26369.
Modulators of 14-3-3 protein-protein interactions
Stevers LM, Sijbesma E, Botta M, MacKintosh C, Obsil T, Landrieu I, Cau Y, Wilson AJ, Karawajczyk A, Eickhoff J, Davis J, Hann M, O’Mahony G, Doveston RG, Brunsveld L, Ottmann C. J Med Chem. 2018 May 10;61(9):3755-3778.
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 AR, Wask L, Gravenstein I, Pardo M, Pietzke M, Gurumurthy RK, Angermann J, Laudeley R, Glage S, Meyer M, Chumduri C, Kempa S, Dinkel K, Unger A, Klebl B, Klos A, Meyer TF. Cell Host Microbe. 2018 May 9;23(5):661-671.e8.
Identification of non-catalytic lysine residues from allosteric circuits via covalent probes
Bongard J, Lorenz M, Vetter IR, Stege P, Porfetye AT, Schmitz AL, Kaschani F, Wolf A, Koch U, Nussbaumer P, Klebl B, Kaiser M, Ehrmann M. ACS Chem. Biol. 2018, 13 (5), 1307-1312.