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.

2017
Na+ entry through heteromeric TRPC4/C1 channels mediates (-)Englerin A-induced cytotoxicity in synovial sarcoma cells

Muraki K, Ohnishi K, Takezawa A, Suzuki H, Hatano N, Muraki Y, Hamzah N, Foster R, Waldmann H, Nussbaumer P, Christmann M, Bon RS, Beech DJ.
Sci Rep. 2017, 7, 16988.

Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer

Lücking U., Scholz A., Lienau P., Siemeister G., Kosemund D., Bohlmann R., Briem H., Terebesi I., Meyer K., Prelle K., Denner K., Bömer U., Schäfer M., Eis K., Valencia R., Ince S., von Nussbaum F., Mumberg D., Ziegelbauer K., Klebl B., Choidas A., Nussbaumer P., Baumann M., Schultz-Fademrecht C., Rühter G., Eickhoff J., Brands M. (2017). ChemMedChem. 12, 1776-1793.

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. 2017, Oct 19. doi: 10.1021/acs.jmedchem.7b00574. [Epub ahead of print]

Discovery of a Novel Hedgehog Signaling Pathway Inhibitor by Cell-based Compound Discovery and Target Prediction

Waldmann H, Kremer L, Schultz-Fademrecht C, Baumann M, Habenberger P, Choidas A, Klebl B, Kordes S, Schöler HJ, Sterneckert J, Ziegler S, Schneider G.

Angew. Chem. Int. Ed. Engl. 2017, 56, 13021-13025.

Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor

Engel J, Smith S, Lategahn J, Tumbrink HL, Goebel L, Becker C, Hennes E, Keul M, Unger A, Müller H, Baumann M, Schultz-Fademrecht C, Günther G, Hengstler JG, Rauh D.

J. Med. Chem. 2017, 60, 7725-7744.

Systematic kinase inhibitor profiling identifies CDK9 as a synthetic lethal target in NUT midline carcinoma

Brägelmann J, Dammert MA, Dietlein F, Heuckmann JM, Choidas A, Böhm S, Richters A, Basu D, Tischler V, Lorenz C,  Habenberger P, Fang Z, Ortiz-Cuaran S, Leenders F, Eickhoff J, Koch U, Getlik M, Termathe M, Sallouh M, Greff Z, Varga Z, Balke-Want H, French CA, Peifer M, Reinhardt HC, Örfi L, Kéri G, Ansén S, Heukamp LC, Büttner R, Rauh D, Klebl BM, Thomas RK, Sos ML.

Cell Rep. 2017, 20, 2833-2845.

Stabilization of protein-protein interactions in drug discovery

Andrei SA, Sijbesma E, Hann M, Davis J, O’Mahony G, Perry MWD, Karawajczyk A, Eickhoff J, Brunsveld L, Doveston RG, Milroy LG, Ottmann C.
Expert Opin. Drug Discov. 2017, 12, 925-940.

Identification of Two Secondary Ligand Binding Sites in 14-3-3 Proteins Using Fragment Screening

Sijbesma E, Skora L, Leysen S, Brunsveld L, Koch U, Nussbaumer P, Jahnke W, Ottmann C.
Biochemistry 2017, 56, 3972-3982.

Small-Molecule Inhibition of the UNC119-Cargo Interaction

Mejuch T, Garivet G, Hofer W, Kaiser N, Fansa EK, Ehrt C, Koch O, Baumann M, Ziegler S, Wittinghofer A, Waldmann H.
Angew. Chem. Int. Ed. Engl. 2017, 56, 6181-6186.

Covalent Protein Labeling at Glutamic Acids

Martín-Gago P, Fansa EK, Winzker M, Murarka S, Janning P, Schultz-Fademrecht C, Baumann M, Wittinghofer A, Waldmann H.
Cell. Chem. Biol. 2017, 24, 589-597.