Scientific Journals and Books

2021
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

IMI European Lead Factory – democratizing access to high-throughput screening

Jones P S, Boucharens S, McElroy S P, Morrison A, Honarnejad S, Boeckel Sv, van de Hurk H, Basting D, Hüser J, Jaroch S, Ottow E, Benningshof J, Folmer R H A, Leemhuis F, Patricia M 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, Dömling A, Kühnert S M, Roevens P W M, van Vlijmen H, van Wanrooij E J A , Verbruggen C, Nussbaumer P, Ovaa H, van der Stelt M, Baek Simonsen K B, Tagmose L, Waldmann H, Duffy J, Finsinger D, Jurzak M, Burgess-Brown N A, Lee W H, Rutjes F P J T, Haag H, Kallus C, Mors H, Dorval T, Lesur B, Olayo F R, 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. 2021 Dec 14;10.1038/d41573-021-00196-3.

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.

Sequence-Selective Covalent CaaX-Box Receptors Prevent Farnesylation of Oncogenic Ras Proteins and Impact MAPK/PI3 K Signaling

Franz M, Möhrchen B, Degenhart C, Gülden D, Shkura O, Wolters D, Koch, Klebl B, Stoll R, Helfrich I, Scherkenbeck J. ChemMedChem. 2021 Aug 19;16(16):2504-2514. doi: 10.1002/cmdc.202100167. Epub 2021 May 19.

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. Combinatorial Drug Treatments Reveal Promising Anticytomegaloviral Profiles for Clinically Relevant Pharmaceutical Kinase Inhibitors (PKIs). Int J Mol Sci. 2021 Jan 8;22(2):E575.

2019
Chronic high dose P2X7 receptor inhibition exacerbates cancer-induced bone pain

Falk S, Appel CK, Bennedbæk HB, Al-Dihaissy T, Unger A, Dinkel K, Heegaard AM. Eur J Pharmacol. 2019 Feb 15;845:48-55

Chemical Validation of DegS As a Target for the Development of Antibiotics with a Novel Mode of Action

Bongard J, Schmitz AL, Wolf A, Zischinsky G, Pieren M, Schellhorn B, Bravo-Rodriguez K, Schillinger J, Koch U, Nussbaumer P, Klebl B, Steinmann J, Buer J, Sanchez-Garcia E, Ehrmann M, Kaiser M. ChemMedChem. 2019 Jun 5;14(11):1074-1078.

Kinase Chemodiversity from the Arctic: The Breitfussins

Hansen KØ, Andersen JH, Bayer A, Pandey SK, Lorentzen M, Jørgensen KB, Sydnes MO, Guttormsen Y, Baumann M, Koch U, Klebl B, Eickhoff J, Haug BE, Isaksson J, Hansen EH. J Med Chem. 2019 Nov 27;62(22):10167-10181.

Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß

Kremer L, Hennes E, Brause A, Ursu A, Robke L, Matsubayashi HT, Nihongaki Y, Flegel J, Mejdrová I, Eickhoff J, Baumann M, Nencka R, Janning , Kordes S, Schöler HR, Sterneckert J, Inoue T, Ziegler S, Waldmann H. Angew Chem Int Ed Engl. 2019 Nov 11;58(46):16617-16628.

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. 2019 Jan;161:63-69.

Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S

Lategahn J, Keul M, Klövekorn P, Tumbrink HL, Niggenaber J, Müller MP, Hodson L, Flaßhoff M, Hardick J, Grabe T, Engel J, Schultz-Fademrecht C, Baumann M, Ketzer J, Mühlenberg T, Hiller W, Günther G, Unger A, Müller H, Heimsoeth A, Golz C, Blank-Landeshammer B, Kollipara L, Zahedi RP, Strohmann C, Hengstler JG, van Otterlo WAL, Bauer S, Rauh D. Chem Sci. 2019 Oct 4;10(46):10789-10801.

Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in KRAS-Mutant Pancreatic and Colorectal Cancer

Weisner J, Landel I, Reintjes C, Uhlenbrock N, Trajkovic-Arsic M, Dienstbier N, Hardick J, Ladigan S, Lindemann M, Smith S, Quambusch L, Scheinpflug R, Depta L, Gontla R, Unger A, Müller H, Baumann M, Schultz-Fademrecht C, Günther G, Maghnouj A, Müller MP, Pohl M, Teschendorf C, Wolters H, Viebahn R, Tannapfel A, Uhl W, Hengstler J, Hahn SA, Siveke JT, Rauh D. Cancer Res. 2019 May 1;79(9):2367-2378.

Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors

Wolle P, Hardick J, Cronin SJF, Engel J, Baumann M, Lategahn J, Penninger JM, Rauh D. J Med Chem. 2019 Mar 14;62(5):2843-2848.

Small-Molecule Inhibition of the UNC-Src Interaction Impairs Dynamic Src Localization in Cells

Garivet G, Hofer W, Konitsiotis A, Klein C, Kaiser N, Mejuch T, Fansa E, Alsaabi R, Wittinghofer A, Bastiaens PIH, Waldmann H. Cell Chem Biol. 2019 Jun 20;26(6):842-851.

Analysis and Modelling of False Positives in GPCR Assays

Ghosh D, Tetko I, Klebl B, Nussbaumer P, Koch U. International Conference on Artificial Neural Networks 2019, 764-770.