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.

Increased expression of the ATP-gated P2X7 receptor reduces responsiveness to anti-convulsants during status epilepticus in mice
Beamer E, Morgan J, Alves M, Méndez A M, Morris G, Zimmer B, Conte G, de Diego-Garcia L, Alarcón-Vila C, Ka Yiu Ng N, Madden S, Calzaferri F, de Los Ríos C, García A G, Hamacher M, Dinkel K, Pelegrín P, Henshall D C, Nicke A, Engel T. Br J Pharmacol. 2021 Dec 27;10.1111/bph.15785

Transient P2X7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy
Beamer E, Morgan J, Alves M, Menendez Mendez M, Morris G, Zimmer B, Conte G, de Diego-Garcia L, Ka Yiu Ng N, Madden S, Calzaferri F, de los Rios C, Garcia A, Hamacher M, Dinkel K, Pelegrin P, Henshall D, Nicke A, Engel T. Authorea. 2021 Sep 25;

Sequence-Selective Covalent CaaX-Box Receptors Prevent Farnesylation of Oncogenic Ras Proteins and Impact MAPK/PI3 K Signaling
Franz M, Mörchen B, Degenhart C, Gülden D, Shkura O, Wolters D, Koch U, Klebl B, Stoll R, Helfrich I, Scherkenbeck J. ChemMedChem. 2021 Aug 19;16(16):2504-2514.

Structure-Activity Relationship Studies of Trisubstituted Isoxazoles as Selective Allosteric Ligands for the Retinoic-Acid-Receptor-Related Orphan Receptor γt.
Meijer FA, Saris AOWM, Doveston RG, Oerlemans GJM, de Vries RMJM, Somsen BA, Unger A, Klebl B, Ottmann C, Cossar PJ, Brunsveld L. J Med Chem. 2021 Jul 8;64(13):9238-9258.

Combinatorial Drug Treatments Reveal Promising Anticytomegaloviral Profiles for Clinically Relevant Pharmaceutical Kinase Inhibitors (PKIs)
Wild M, Kicuntod J, Seyler L, Wangen C, Bertzbach LD, Conradie AM, Kaufer BB, Wagner S, Michel D, Eickhoff J, Tsogoeva SB, Bäuerle T, Hahn F, Marschall M. Int J Mol Sci. 2021 Jan 8;22(2):575.