Home » Core Members » University of Tübingen » Pharmaceutical Chemistry, Faculty for Chemistry and Pharmacy » Publications

Selected Publications

 

Walter NM, Wentsch HK, Bührmann M, Bauer SM, Döring E, Mayer-Wrangowski S, Sievers-Engler A, Willemsen-Seegers N, Zaman G, Buijsman R, Lämmerhofer M, Rauh D, Laufer SA. Design, Synthesis, and Biological Evaluation of Novel Type I(1)/(2)p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine. J Med Chem. 2017 Oct 12;60(19):8027-8054. doi: 10.1021/acs.jmedchem.7b00745.

 

Albrecht W, Unger A, Bauer SM, Laufer SA. Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases. J Med Chem. 2017 Jul 13;60(13):5290-5305. doi:10.1021/acs.jmedchem.6b01647

 

Juchum M, Günther M, Döring E, Sievers-Engler A, Lämmerhofer M, Laufer S. Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. J Med Chem. 2017 Jun 8;60(11):4636-4656. doi: 10.1021/acs.jmedchem.7b00178

 

Wentsch HK, Walter NM, Bührmann M, Mayer-Wrangowski S, Rauh D, Zaman GJR, Willemsen-Seegers N, Buijsman RC, Henning M, Dauch D, Zender L, Laufer S. Optimized Target Residence Time: Type I1/2 Inhibitors for p38α MAP Kinase with Improved Binding Kinetics through Direct Interaction with the R-Spine. Angew Chem Int Ed Engl. 2017 May 2;56(19):5363-5367. doi: 10.1002/anie.201701185.

 

Muth F, El-Gokha A, Ansideri F, Eitel M, Döring E, Sievers-Engler A, Lange A, Boeckler FM, Lämmerhofer M, Koch P, Laufer SA. Tri- and Tetrasubstituted Pyridinylimidazoles as Covalent Inhibitors of c-Jun N-Terminal Kinase 3. J Med Chem. 2017 Jan 26;60(2):594-607. doi: 10.1021/acs.jmedchem.6b01180.

 

Neul C, Schaeffeler E, Sparreboom A, Laufer S, Schwab M, Nies AT. Impact of Membrane Drug Transporters on Resistance to Small-Molecule Tyrosine Kinase Inhibitors. Trends Pharmacol Sci. 2016 Nov;37(11):904-932. doi:10.1016/j.tips.2016.08.003.

 

Günther M, Juchum M, Kelter G, Fiebig H, Laufer S. Lung Cancer: EGFR Inhibitors with Low Nanomolar Activity against a Therapy-Resistant L858R/T790M/C797S Mutant. Angew Chem Int Ed Engl. 2016 Aug 26;55(36):10890-4. doi: 10.1002/anie.201603736.

 

Dauch D, Rudalska R, Cossa G, Nault JC, Kang TW, Wuestefeld T, Hohmeyer A, Imbeaud S, Yevsa T, Hoenicke L, Pantsar T, Bozko P, Malek NP, Longerich T, Laufer S, Poso A, Zucman-Rossi J, Eilers M, Zender L. A MYC-aurora kinase A protein complex represents an actionable drug target in p53-altered liver cancer. Nat Med. 2016 Jul;22(7):744-53. doi: 10.1038/nm.4107.

 

Lange A, Günther M, Büttner FM, Zimmermann MO, Heidrich J, Hennig S, Zahn S, Schall C, Sievers-Engler A, Ansideri F, Koch P, Laemmerhofer M, Stehle T, Laufer SA, Boeckler FM. Targeting the Gatekeeper MET146 of C-Jun N-Terminal Kinase 3 Induces a Bivalent Halogen/Chalcogen Bond. J Am Chem Soc. 2015 Nov 25;137(46):14640-52. doi: 10.1021/jacs.5b07090.

 

Koeberle A, Pergola C, Shindou H, Koeberle SC, Shimizu T, Laufer SA, Werz O. Role of p38 mitogen-activated protein kinase in linking stearoyl-CoA desaturase-1 activity with endoplasmic reticulum homeostasis. FASEB J. 2015 Jun;29(6):2439-49. doi: 10.1096/fj.14-268474

 

Muth F, Günther M, Bauer SM, Döring E, Fischer S, Maier J, Drückes P, Köppler J, Trappe J, Rothbauer U, Koch P, Laufer SA. Tetra-substituted pyridinylimidazoles as dual inhibitors of p38α mitogen-activated protein kinase and c-Jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases. J Med Chem. 2015 Jan 8;58(1):443-56. doi: 10.1021/jm501557a.

 

Rudalska R, Dauch D, Longerich T, McJunkin K, Wuestefeld T, Kang TW, Hohmeyer A, Pesic M, Leibold J, von Thun A, Schirmacher P, Zuber J, Weiss KH, Powers S, Malek NP, Eilers M, Sipos B, Lowe SW, Geffers R, Laufer S, Zender L. In vivo RNAi screening identifies a mechanism of sorafenib resistance in liver cancer. Nat Med. 2014 Oct;20(10):1138-46. doi: 10.1038/nm.3679.

 

Gehringer M, Forster M, Pfaffenrot E, Bauer SM, Laufer SA. Novel hinge-binding motifs for Janus kinase 3 inhibitors: a comprehensive structure-activity relationship study on tofacitinib bioisosteres. ChemMedChem. 2014 Nov;9(11):2516-27. doi: 10.1002/cmdc.201402252.

 

Freitag A, Prajwal P, Shymanets A, Harteneck C, Nürnberg B, Schächtele C, Kubbutat M, Totzke F, Laufer SA. Development of first lead structures for phosphoinositide 3-kinase-C2γ inhibitors. J Med Chem. 2015 Jan 8;58(1):212-21. doi: 10.1021/jm5006034.

 

Anton R, Bauer SM, Keck PR, Laufer S, Rothbauer U. A p38 substrate-specific MK2-EGFP translocation assay for identification and validation of new p38 inhibitors in living cells: a comprising alternative for acquisition of cellular p38 inhibition data. PLoS One. 2014 Apr 17;9(4):e95641. doi:10.1371/journal.pone.0095641.

 

Barbosa ML, Lima LM, Tesch R, Sant'Anna CM, Totzke F, Kubbutat MH, Schächtele C, Laufer SA, Barreiro EJ. Novel 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors. Eur J Med Chem. 2014 Jan;71:1-14. doi: 10.1016/ j.ejmech.2013.10.058.

 

Baur B, Storch K, Martz KE, Goettert MI, Richters A, Rauh D, Laufer SA. Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood. J Med Chem. 2013 Nov 14;56(21):8561-78. doi: 10.1021/jm401276h.

 

Borst O, Walker B, Münzer P, Russo A, Schmid E, Faggio C, Bigalke B, Laufer S, Gawaz M, Lang F. Skepinone-L, a novel potent and highly selective inhibitor of p38 MAP kinase, effectively impairs platelet activation and thrombus formation. Cell Physiol Biochem. 2013;31(6):914-24. doi: 10.1159/000350110.

 

Koeberle A, Shindou H, Koeberle SC, Laufer SA, Shimizu T, Werz O. Arachidonoyl-phosphatidylcholine oscillates during the cell cycle and counteracts proliferation by suppressing Akt membrane binding. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2546-51. doi: 10.1073/pnas.1216182110.

 

Fischer S, Wentsch HK, Mayer-Wrangowski SC, Zimmermann M, Bauer SM, Storch K,  Niess R, Koeberle SC, Grütter C, Boeckler FM, Rauh D, Laufer SA. Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity. J Med Chem. 2013 Jan 10;56(1):241-53. doi:  10.1021/jm301539x.