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.

2012
Development of Selective, Potent RabGGTase Inhibitors

Stigter EA, Guo Z, Bon RS, Wu YW, Choidas A, Wolf A, Menninger S, Waldmann H, Blankenfeldt W, Goody RS.

J Med Chem. 2012 Oct 11;55(19):8330-40. doi: 10.1021/jm300624s. Epub 2012 Oct 3. [Epub ahead of print] PMID: 22963166

Amorfrutins are potent antidiabetic dietary natural products

Weidner C, de Groot JC, Prasad A, Freiwald A, Quedenau C, Kliem M, Witzke A, Kodelja V, Han CT, Giegold S, Baumann M, Klebl B, Siems K, Müller-Kuhrt L, Schürmann A, Schüler R, Pfeiffer AF, Schroeder FC, Büssow K, Sauer S.

Proc Natl Acad Sci USA 2012, 109(19), 7257-62

Psoromic Acid is a Selective and Covalent Rab-Prenylation Inhibitor Targeting Autoinhibited RabGGTase

Deraeve C, Guo Z, Bon RS, Blankenfeldt W, DiLucrezia R, Wolf R, Choidas A, Wetzel S, Alexandrov K, Waldmann H, Goody RS, Wu Y.

J Am Chem Soc. 2012 May 2;134(17):7384-91.