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.

2015
Expansion of Chemical Space for Collaborative Lead Generation and Drug Discovery: The European Lead Factory Perspective

Anna Karawajczyk, Fabrizio Giordanetto, Jorg Benningshof, Daniel Hamza, Tuomo Kalliokoski, Kees Pouwer, Remy Morgentin, Adam Nelson, Gerhard Müller, Alexander Piechot and Dimitrios Tzalis.

(Nov 2015): 1310-16.doi:10.1016/j.drudis.2015.09.009

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Medicinal Chemists of the 21st Century – Who Are We and Where to Go?

Dr. Peter Nussbaumer

ChemMedChem 2015, 10(7), 1133-1139

Professional translational research: a new hybrid paradigm in early drug discovery

Dr. Peter Nussbaumer, Dr. Bert Klebl

Vol. 7, No. 14, Pages 1879-1889, DOI 10.4155/fmc.15.124 (doi:10.4155/fmc.15.124)

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Price-Focused Analysis of Commercially Available Building Blocks for Combinatorial Library Synthesis

Tuomo Kalliokoski

ACS Comb. Sci, Article ASAP DOI: 10.1021/ arscombsci.5b00063

Protein-protein interactions as drug targets

Malgorzata Skwarczynska and Christian Ottmann

Future Med Chem. 2015;7(16):2195-219. doi: 10.4155/fmc.15.138.

Aminomethylhydroxylation of alkenes: Exploitation in the synthesis of scaffolds for small molecule libraries

Ignacio Colomer, Ololade Adeniji, George M. Burslem, Philip Craven, Martin Ohsten Rasmussen, Anthony Willaume, Tuomo Kalliokoski, Richard Foster, Stephen P. Marsden, Adam Nelson

Bioorganic & Medicinal Chemistry 23 (2015) 2629–2635, journal homepage: www.elsevier.com/locate/bmc

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A Novel CDK7 Inhibitor of the Pyrazolotriazine Class Exerts Broad-Spectrum Antiviral Activity at Nanomolar Concentrations

Hutterer C, Eickhoff J, Milbradt J, Korn K, Zeitträger I, Bahsi H, Wagner S, Zischinsky G, Wolf A, Degenhart C, Unger A, Baumann M, Klebl B, Marschall M.

Antimicrob. Agents Chemother. 2015 Apr;59(4):2062-71. doi: 10.1128/AAC.04534-14. Epub 2015 Jan 26.

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Selective inhibitors of the FK506-binding protein 51 by induced fit

Gaali S, Kirschner A, Cuboni S, Hartmann J, Kozany C, Balsevich G, Namendorf C, Fernandez-Vizarra P2, Sippel C1, Zannas AS, Draenert R4, Binder EB, Almeida OF, Rühter G6, Uhr M1, Schmidt MV, Touma C, Bracher A, Hausch F.
Nat Chem Biol. 2015 Jan;11(1):33-7. doi: 10.1038/nchembio.1699. Epub 2014 Dec 1.