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.

2011
Natural product-inspired cascade synthesis yields modulators of centrosome integrity

Dückert H, Pries V, Khedkar V, Menninger S, Bruss H, Bird AW, Maliga Z, Brockmeyer A, Janning P, Hyman A, Grimme S, Schürmann M, Preut H, Hübel K, Ziegler S, Kumar K, Waldmann H.
Nat Chem Biol. 2011 Dec 25;8(2):179-84. doi: 10.1038/nchembio.758.

Recruitment of cyclin-dependent kinase 9 to nuclear compartments during cytomegalovirus late replication: importance of an interaction between viral pUL69 and cyclin T1

Feichtinger S, Stamminger T, Müller R, Graf L, Klebl B, Eickhoff J, Marschall M.
J Gen Virol. 2011 Jul;92(Pt 7):1519-31. Epub 2011 Mar 30.

Structure-guided development of selective RabGGTase inhibitors

Bon RS, Guo Z, Stigter EA, Wetzel S, Menninger S, Wolf A, Choidas A, Alexandrov K, Blankenfeldt W, Goody RS, Waldmann H.
Angew Chem Int Ed Engl. 2011 May 16;50(21):4957-61. doi: 10.1002/anie.201101210. Epub 2011 Apr 21. No abstract available.

Total synthesis and biological evaluation of (-)-englerin A and B: synthesis of analogues with improved activity profile

Radtke L, Willot M, Sun H, Ziegler S, Sauerland S, Strohmann C, Fröhlich R, Habenberger P, Waldmann H, Christmann M.
Angew Chem Int Ed Engl. 2011 Apr 18;50(17):3998-4002. doi: 10.1002/anie.201007790. Epub 2011 Mar 29. No abstract available.

Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6Hindolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase

Narjes F., Crescenzi B., Ferrara M., Habermann J,Colarusso S., Ferreira M. del R., Stansfield I., MackayA.C., Conte I., Ercolani C., Zaramella S., Koch U., Migliaccio G., Altamura S., Laufer R., De Francesco R., Rowley M.
Med Chem. 2011 Jan 13;54(1):289-301.

Protein Kinases as Drug Targets: 49 (Methods and Principles in Medicinal Chemistry)

von Bert Klebl, Gerhard Müller und Michael Hamacher
Wiley-VCH Verlag GmbH & Co. KGaA

(Gebundene Ausgabe – 9. Februar 2011)

Screening for Kinase Inhibitors: From Biochemical to Cellular Assays

Eickhoff J., Choidas A in

Medicinal Chemistry 2011, Vol. 49, 45-67