SMOOSE
Publications
2018
Ackermann, S., Cartolano, M., Hero, B., Welte, A., Kahlert, Y., Roderwieser, A., Bartenhagen, C., Walter, E., Gecht, J., Kerschke, L., Volland, R., Menon, R., Heuckmann, J. M., Gartlgruber, M., Hartlieb, S., Henrich, K.-O., Okonechnikov, K., Altmüller, J., Nürnberg, P., Lefever, S., Wilde, B. d., Sand, F., Ikram, F., Rosswog, C., Fischer, J., Theissen, J., Hertwig, F., Singhi, A. D., Simon, T., Vogel, W., Perner, S., Krug, B., Schmidt, M., Rahmann, S., Achter, V., Lang, U., Vokuhl, C., Ortmann, M., Büttner, R., Eggert, A., Speleman, F., O’Sullivan, R. J., Thomas, R. K., Berthold, F., Vandesompele, J., Schramm, A., Westermann, F., Schulte, J. H., Peifer, M.Fischer, M., 2018. A mechanistic classification of clinical phenotypes in neuroblastoma. Science, 362(6419), 1165-1170. doi.org/10.1126/science.aat6768
Castiglione, R., Alidousty, C., Holz, B., Wagener, S., Baar, T., Heydt, C., Binot, E., Zupp, S., Kron, A., Wolf, J., Merkelbach-Bruse, S., Reinhardt, H. C., Buettner, R.Schultheis, A. M., 2018. Comparison of the genomic background of MET-altered carcinomas of the lung: biological differences and analogies. Mod. Pathol. doi.org/10.1038/s41379-018-0182-8
Cun, Y., Yang, T.-P., Achter, V., Lang, U.Peifer, M., 2018. Copy-number analysis and inference of subclonal populations in cancer genomes using Sclust. Nat Protoc, 13(6), 1488-1501. doi.org/10.1038/nprot.2018.033
Depuydt, P., Boeva, V., Hocking, T. D., Cannoodt, R., Ambros, I. M., Ambros, P. F., Asgharzadeh, S., Attiyeh, E. F., Combaret, V., Defferrari, R., Fischer, M., Hero, B., Hogarty, M. D., Irwin, M. S., Koster, J., Kreissman, S., Ladenstein, R., Lapouble, E., Laureys, G., London, W. B., Mazzocco, K., Nakagawara, A., Noguera, R., Ohira, M., Park, J. R., Potschger, U., Theissen, J., Tonini, G. P., Valteau-Couanet, D., Varesio, L., Versteeg, R., Speleman, F., Maris, J. M., Schleiermacher, G.De Preter, K., 2018. Genomic Amplifications and Distal 6q Loss: Novel Markers for Poor Survival in High-risk Neuroblastoma Patients. J Natl Cancer Inst, 110(10), 1084-1093. doi.org/10.1093/jnci/djy022
Fassunke, J., Müller, F., Keul, M., Michels, S., Dammert, M. A., Schmitt, A., Plenker, D., Lategahn, J., Heydt, C., Brägelmann, J., Tumbrink, H. L., Alber, Y., Klein, S., Heimsoeth, A., Dahmen, I., Fischer, R. N., Scheffler, M., Ihle, M. A., Priesner, V., Scheel, A. H., Wagener, S., Kron, A., Frank, K., Garbert, K., Persigehl, T., Püsken, M., Haneder, S., Schaaf, B., Rodermann, E., Engel-Riedel, W., Felip, E., Smit, E. F., Merkelbach-Bruse, S., Reinhardt, H. C., Kast, S. M., Wolf, J., Rauh, D., Büttner, R.Sos, M. L., 2018. Overcoming EGFRG724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors. Nat Commun, 9(1), 4655. doi.org/10.1038/s41467-018-07078-0
George, J., Walter, V., Peifer, M., Alexandrov, L. B., Seidel, D., Leenders, F., Maas, L., Müller, C., Dahmen, I., Delhomme, T. M., Ardin, M., Leblay, N., Byrnes, G., Sun, R., De Reynies, A., McLeer-Florin, A., Bosco, G., Malchers, F., Menon, R., Altmüller, J., Becker, C., Nürnberg, P., Achter, V., Lang, U., Schneider, P. M., Bogus, M., Soloway, M. G., Wilkerson, M. D., Cun, Y., McKay, J. D., Moro-Sibilot, D., Brambilla, C. G., Lantuejoul, S., Lemaitre, N., Soltermann, A., Weder, W., Tischler, V., Brustugun, O. T., Lund-Iversen, M., Helland, Å., Solberg, S., Ansén, S., Wright, G., Solomon, B., Roz, L., Pastorino, U., Petersen, I., Clement, J. H., Sänger, J., Wolf, J., Vingron, M., Zander, T., Perner, S., Travis, W. D., Haas, S. A., Olivier, M., Foll, M., Büttner, R., Hayes, D. N., Brambilla, E., Fernandez-Cuesta, L.Thomas, R. K., 2018. Integrative genomic profiling of large-cell neuroendocrine carcinomas reveals distinct subtypes of high-grade neuroendocrine lung tumors. Nat Commun, 9(1), 1048. doi.org/10.1038/s41467-018-03099-x
Grimm, C., Fischer, A., Farrelly, A. M., Kalachand, R., Castiglione, R., Wasserburger, E., Hussong, M., Schultheis, A. M., Altmüller, J., Thiele, H., Reinhardt, H. C., Hauschulz, K., Hennessy, B. T., Herwig, R., Lienhard, M., Buettner, R.Schweiger, M. R., 2018. Combined Targeted Re-Sequencing of Cytosine DNA Methylation and Mutations of DNA Repair Genes with Potential Use for PARP1 Inhibitor Sensitivity Testing. J Mol Diagn. doi.org/10.1016/j.jmoldx.2018.10.007
Herling, C. D., Abedpour, N., Weiss, J., Schmitt, A., Jachimowicz, R. D., Merkel, O., Cartolano, M., Oberbeck, S., Mayer, P., Berg, V., Thomalla, D., Kutsch, N., Stiefelhagen, M., Cramer, P., Wendtner, C.-M., Persigehl, T., Saleh, A., Altmüller, J., Nürnberg, P., Pallasch, C., Achter, V., Lang, U., Eichhorst, B., Castiglione, R., Schäfer, S. C., Büttner, R., Kreuzer, K.-A., Reinhardt, H. C., Hallek, M., Frenzel, L. P.Peifer, M., 2018. Clonal dynamics towards the development of venetoclax resistance in chronic lymphocytic leukemia. Nat Commun, 9(1), 727. doi.org/10.1038/s41467-018-03170-7
Knittel, G., Rehkämper, T., Nieper, P., Schmitt, A., Flümann, R.Reinhardt, H. C., 2018. DNA damage pathways and B-cell lymphomagenesis. Curr. Opin. Hematol., 25(4), 315-322. doi.org/10.1097/MOH.0000000000000433
Lategahn, J., Keul, M.Rauh, D., 2018. Lessons To Be Learned: The Molecular Basis of Kinase-Targeted Therapies and Drug Resistance in Non-Small Cell Lung Cancer. Angew Chem Int Ed Engl, 57(9), 2307-2313. doi.org/10.1002/anie.201710398
Macheleidt, I. F., Dalvi, P. S., Lim, S.-Y., Meemboor, S., Meder, L., Käsgen, O., Müller, M., Kleemann, K., Wang, L., Nürnberg, P., Rüsseler, V., Schäfer, S. C., Mahabir, E., Büttner, R.Odenthal, M., 2018. Preclinical studies reveal that LSD1 inhibition results in tumor growth arrest in lung adenocarcinoma independently of driver mutations. Mol Oncol, 12(11), 1965-1979. doi.org/10.1002/1878-0261.12382
Meder, L., König, K., Dietlein, F., Macheleidt, I., Florin, A., Ercanoglu, M. S., Rommerscheidt-Fuss, U., Koker, M., Schön, G., Odenthal, M., Klein, F., Büttner, R., Schulte, J. H., Heukamp, L. C.Ullrich, R. T., 2018. LIN28B enhanced tumorigenesis in an autochthonous KRASG12V-driven lung carcinoma mouse model. Oncogene, 37(20), 2746-2756. doi.org/10.1038/s41388-018-0158-7
Meder, L., Schuldt, P., Thelen, M., Schmitt, A., Dietlein, F., Klein, S., Borchmann, S., Wennhold, K., Vlasic, I., Oberbeck, S., Riedel, R., Florin, A., Golfmann, K., Schlößer, H. A., Odenthal, M., Buettner, R., Wolf, J., Hallek, M., Herling, M., von Bergwelt-Baildon, M., Reinhardt, H. C.Ullrich, R. T., 2018. Combined VEGF and PD-L1 Blockade Displays Synergistic Treatment Effects in an Autochthonous Mouse Model of Small Cell Lung Cancer. Cancer Res., 78(15), 4270-4281. doi.org/10.1158/0008-5472.CAN-17-2176
Plenker, D., Bertrand, M., de Langen, A. J., Riedel, R., Lorenz, C., Scheel, A. H., Müller, J., Brägelmann, J., Daßler-Plenker, J., Kobe, C., Persigehl, T., Kluge, A., Wurdinger, T., Schellen, P., Hartmann, G., Zacherle, T., Menon, R., Thunnissen, E., Büttner, R., Griesinger, F., Wolf, J., Heukamp, L., Sos, M. L.Heuckmann, J. M., 2018. Structural Alterations of MET Trigger Response to MET Kinase Inhibition in Lung Adenocarcinoma Patients. Clin. Cancer Res., 24(6), 1337-1343. doi.org/10.1158/1078-0432.CCR-17-3001
Schmitt, A., Feldmann, G., Zander, T.Reinhardt, H. C., 2018. Targeting Defects in the Cellular DNA Damage Response for the Treatment of Pancreatic Ductal Adenocarcinoma. Oncol Res Treat, 41(10), 619-625. doi.org/10.1159/000493401
Tesch, R., Becker, C., Müller, M. P., Beck, M. E., Quambusch, L., Getlik, M., Lategahn, J., Uhlenbrock, N., Costa, F. N., Polêto, M. D., de Sena Murteira Pinheiro, P., Rodrigues, D. A., Sant'Anna, C. M. R., Ferreira, F. F., Verli, H., Fraga, C. A. M.Rauh, D., 2018. An Unusual Intramolecular Halogen Bond Guides Conformational Selection. Angew. Chem. Int. Ed. Engl. doi.org/10.1002/anie.201804917
Welcker, D., Jain, M., Khurshid, S., Jokic, M., Hohne, M., Schmitt, A., Frommolt, P., Niessen, C. M., Spiro, J., Persigehl, T., Wittersheim, M., Buttner, R., Fanciulli, M., Schermer, B., Reinhardt, H. C., Benzing, T.Hopker, K., 2018. AATF suppresses apoptosis, promotes proliferation and is critical for Kras-driven lung cancer. Oncogene, 37(11), 1503-1518. doi.org/10.1038/s41388-017-0054-6
Wiedemann, B., Weisner, J.Rauh, D., 2018. Chemical modulation of transcription factors. Medchemcomm, 9(8), 1249-1272. doi.org/10.1039/c8md00273h
Wolle, P., Müller, M. P.Rauh, D., 2018. Augmented Reality in Scientific Publications-Taking the Visualization of 3D Structures to the Next Level. ACS Chem. Biol., 13(3), 496-499. doi.org/10.1021/acschembio.8b00153
Wolle, P., Weisner, J., Keul, M., Landel, I., Lategahn, J.Rauh, D., 2018. RASPELD to Perform High-End Screening in an Academic Environment Toward the Development of Cancer Therapeutics. ChemMedChem. doi.org/10.1002/cmdc.201800477
Yang, D., Denny, S. K., Greenside, P. G., Chaikovsky, A. C., Brady, J. J., Ouadah, Y., Granja, J. M., Jahchan, N. S., Lim, J. S., Kwok, S., Kong, C. S., Berghoff, A. S., Schmitt, A., Reinhardt, H. C., Park, K.-S., Preusser, M., Kundaje, A., Greenleaf, W. J., Sage, J.Winslow, M. M., 2018. Intertumoral Heterogeneity in SCLC Is Influenced by the Cell Type of Origin. Cancer Discov, 8(10), 1316-1331. doi.org/10.1158/2159-8290.CD-17-0987
2017
Amer, W., Toth, C., Vassella, E., Meinrath, J., Koitzsch, U., Arens, A., Huang, J., Eischeid, H., Adam, A., Buettner, R., Scheel, A., Schaefer, S.C., Odenthal, M., 2017. Evolution analysis of heterogeneous non-small cell lung carcinoma by ultra-deep sequencing of the mitochondrial genome. Sci Rep 7, 11069. doi.org/10.1038/s41598-017-11345-3
Brägelmann, J., Dammert, M.A., Dietlein, F., Heuckmann, J.M., 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, C.A., Peifer, M., Reinhardt, H.C., Örfi, L., Kéri, G., Ansén, S., Heukamp, L.C., Büttner, R., Rauh, D., Klebl, B.M., Thomas, R.K., Sos, M.L., 2017. Systematic Kinase Inhibitor Profiling Identifies CDK9 as a Synthetic Lethal Target in NUT Midline Carcinoma. Cell Reports 20, 2833–2845. doi.org/10.1016/j.celrep.2017.08.082
Bührmann, M., Wiedemann, B.M., Müller, M.P., Hardick, J., Ecke, M., Rauh, D., 2017. Structure-based design, synthesis and crystallization of 2-arylquinazolines as lipid pocket ligands of p38α MAPK. PLoS ONE 12, e0184627. doi.org/10.1371/journal.pone.0184627
Büttner, R., Wolf, J., Thomas, R.K., Sos, M.L., 2017. Resistance Mechanisms to AZD9291 and Rociletinib-Response. Clin. Cancer Res. 23, 3967–3968. doi.org/10.1158/1078-0432.CCR-17-0948
Doerr, F., George, J., Schmitt, A., Beleggia, F., Rehkämper, T., Hermann, S., Walter, V., Weber, J.-P., Thomas, R.K., Wittersheim, M., Büttner, R., Persigehl, T., Reinhardt, H.C., 2017. Targeting a non-oncogene addiction to the ATR/CHK1 axis for the treatment of small cell lung cancer. Sci Rep 7, 15511. doi.org/10.1038/s41598-017-15840-5
Engel, J., Smith, S., Lategahn, J., Tumbrink, H.L., Goebel, L., Becker, C., Hennes, E., Keul, M., Unger, A., Müller, H., Baumann, M., Schultz-Fademrecht, C., Günther, G., Hengstler, J.G., Rauh, D., 2017. Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. J. Med. Chem. 60, 7725–7744. doi.org/10.1021/acs.jmedchem.7b00515
George, J., Saito, M., Tsuta, K., Iwakawa, R., Shiraishi, K., Scheel, A.H., Uchida, S., Watanabe, S.-I., Nishikawa, R., Noguchi, M., Peifer, M., Jang, S.J., Petersen, I., Büttner, R., Harris, C.C., Yokota, J., Thomas, R.K., Kohno, T., 2017. Genomic Amplification of CD274 (PD-L1) in Small-Cell Lung Cancer. Clin. Cancer Res. 23, 1220–1226. doi.org/10.1158/1078-0432.CCR-16-1069
Henssen, A.G., Odersky, A., Szymansky, A., Seiler, M., Althoff, K., Beckers, A., Speleman, F., Schäfers, S., De Preter, K., Astrahanseff, K., Struck, J., Schramm, A., Eggert, A., Bergmann, A., Schulte, J.H., 2017. Targeting tachykinin receptors in neuroblastoma. Oncotarget 8, 430–443. doi.org/10.18632/oncotarget.13440
Kaitsiotou, H., Keul, M., Hardick, J., Mühlenberg, T., Ketzer, J., Ehrt, C., Krüll, J., Medda, F., Koch, O., Giordanetto, F., Bauer, S., Rauh, D., 2017. Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. J. Med. Chem. 60, 8801–8815. doi.org/10.1021/acs.jmedchem.7b00841
Knittel, G., Rehkämper, T., Korovkina, D., Liedgens, P., Fritz, C., Torgovnick, A., Al-Baldawi, Y., Al-Maarri, M., Cun, Y., Fedorchenko, O., Riabinska, A., Beleggia, F., Nguyen, P.-H., Wunderlich, F.T., Ortmann, M., Montesinos-Rongen, M., Tausch, E., Stilgenbauer, S., P Frenzel, L., Herling, M., Herling, C., Bahlo, J., Hallek, M., Peifer, M., Buettner, R., Persigehl, T., Reinhardt, H.C., 2017. Two mouse models reveal an actionable PARP1 dependence in aggressive chronic lymphocytic leukemia. Nat Commun 8, 153. doi.org/10.1038/s41467-017-00210-6
Lim, S.-Y., Macheleidt, I., Dalvi, P., Schäfer, S.C., Kerick, M., Ozretić, L., Ortiz-Cuaran, S., George, J., Merkelbach-Bruse, S., Wolf, J., Timmermann, B., Thomas, R.K., Schweiger, M.R., Buettner, R., Odenthal, M., 2017. LSD1 modulates the non-canonical integrin β3 signaling pathway in non-small cell lung carcinoma cells. Sci Rep 7, 10292. doi.org/10.1038/s41598-017-09554-x
Malchers, F., Ercanoglu, M., Schütte, D., Castiglione, R., Tischler, V., Michels, S., Dahmen, I., Brägelmann, J., Menon, R., Heuckmann, J.M., George, J., Ansén, S., Sos, M.L., Soltermann, A., Peifer, M., Wolf, J., Büttner, R., Thomas, R.K., 2017. Mechanisms of Primary Drug Resistance inFGFR1-Amplified Lung Cancer. Clin. Cancer Res. 23, 5527–5536. doi.org/10.1158/1078-0432.CCR-17-0478
Mollaoglu, G., Guthrie, M.R., Böhm, S., Brägelmann, J., Can, I., Ballieu, P.M., Marx, A., George, J., Heinen, C., Chalishazar, M.D., Cheng, H., Ireland, A.S., Denning, K.E., Mukhopadhyay, A., Vahrenkamp, J.M., Berrett, K.C., Mosbruger, T.L., Wang, J., Kohan, J.L., Salama, M.E., Witt, B.L., Peifer, M., Thomas, R.K., Gertz, J., Johnson, J.E., Gazdar, A.F., Wechsler-Reya, R.J., Sos, M.L., Oliver, T.G., 2017. MYC Drives Progression of Small Cell Lung Cancer to a Variant Neuroendocrine Subtype with Vulnerability to Aurora Kinase Inhibition. Cancer Cell. doi.org/10.1016/j.ccell.2016.12.005
Plenker, D., Riedel, M., Brägelmann, J., Dammert, M.A., Chauhan, R., Knowles, P.P., Lorenz, C., Keul, M., Bührmann, M., Pagel, O., Tischler, V., Scheel, A.H., Schütte, D., Song, Y., Stark, J., Mrugalla, F., Alber, Y., Richters, A., Engel, J., Leenders, F., Heuckmann, J.M., Wolf, J., Diebold, J., Pall, G., Peifer, M., Aerts, M., Gevaert, K., Zahedi, R.P., Buettner, R., Shokat, K.M., McDonald, N.Q., Kast, S.M., Gautschi, O., Thomas, R.K., Sos, M.L., 2017. Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors. Sci Transl Med 9. doi.org/10.1126/scitranslmed.aah6144
Rosswog, C., Schmidt, R., Oberthuer, A., Juraeva, D., Brors, B., Engesser, A., Kahlert, Y., Volland, R., Bartenhagen, C., Simon, T., Berthold, F., Hero, B., Faldum, A., Fischer, M., 2017. Molecular Classification Substitutes for the Prognostic Variables Stage, Age, and MYCN Status in Neuroblastoma Risk Assessment. Neoplasia 19, 982–990. doi.org/10.1016/j.neo.2017.09.006
Schmitt, A., Knittel, G., Welcker, D., Yang, T.-P., George, J., Nowak, M., Leeser, U., Büttner, R., Perner, S., Peifer, M., Reinhardt, H.C., 2017. ATM Deficiency Is Associated with Sensitivity to PARP1- and ATR Inhibitors in Lung Adenocarcinoma. Cancer Res. 77, 3040–3056. doi.org/10.1158/0008-5472.CAN-16-3398
Weischenfeldt, J., Dubash, T., Drainas, A.P., Mardin, B.R., Chen, Y., Stütz, A.M., Waszak, S.M., Bosco, G., Halvorsen, A.R., Raeder, B., Efthymiopoulos, T., Erkek, S., Siegl, C., Brenner, H., Brustugun, O.T., Dieter, S.M., Northcott, P.A., Petersen, I., Pfister, S.M., Schneider, M., Solberg, S.K., Thunissen, E., Weichert, W., Zichner, T., Thomas, R., Peifer, M., Helland, A., Ball, C.R., Jechlinger, M., Sotillo, R., Glimm, H., Korbel, J.O., 2017. Pan-cancer analysis of somatic copy-number alterations implicates IRS4 and IGF2 in enhancer hijacking. Nat. Genet. 49, 65–74. doi.org/10.1038/ng.3722
2016
Becker, C., Öcal, S., Nguyen, H.D., Phan, T., Keul, M., Simard, J.R., Rauh, D., 2016. Monitoring Conformational Changes in the Receptor Tyrosine Kinase EGFR. ChemBioChem 17, 990–994. doi.org/10.1002/cbic.201600115
Bunn, P.A., Minna, J.D., Augustyn, A., Gazdar, A.F., Ouadah, Y., Krasnow, M.A., Berns, A., Brambilla, E., Rekhtman, N., Massion, P.P., Niederst, M., Peifer, M., Yokota, J., Govindan, R., Poirier, J.T., Byers, L.A., Wynes, M.W., McFadden, D.G., MacPherson, D., Hann, C.L., Farago, A.F., Dive, C., Teicher, B.A., Peacock, C.D., Johnson, J.E., Cobb, M.H., Wendel, H.-G., Spigel, D., Sage, J., Yang, P., Pietanza, M.C., Krug, L.M., Heymach, J., Ujhazy, P., Zhou, C., Goto, K., Dowlati, A., Christensen, C.L., Park, K., Einhorn, L.H., Edelman, M.J., Giaccone, G., Gerber, D.E., Salgia, R., Owonikoko, T., Malik, S., Karachaliou, N., Gandara, D.R., Slotman, B.J., Blackhall, F., Goss, G., Thomas, R., Rudin, C.M., Hirsch, F.R., 2016. Small Cell Lung Cancer: Can Recent Advances in Biology and Molecular Biology Be Translated into Improved Outcomes? J Thorac Oncol 11, 453–474. doi.org/10.1016/j.jtho.2016.01.012
Engel, J., Becker, C., Lategahn, J., Keul, M., Ketzer, J., Mühlenberg, T., Kollipara, L., Schultz-Fademrecht, C., Zahedi, R.P., Bauer, S., Rauh, D., 2016a. Inhibition wirkstoffresistenter Mutationsvarianten der Rezeptortyrosinkinase EGFR. Angew. Chem. n/a-n/a. doi.org/10.1002/ange.201605011
Engel, J., Lategahn, J., Rauh, D., 2016b. Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer. ACS Med Chem Lett 7, 2–5. doi.org/10.1021/acsmedchemlett.5b00475
Fernández-Majada, V., Welz, P.-S., Ermolaeva, M.A., Schell, M., Adam, A., Dietlein, F., Komander, D., Büttner, R., Thomas, R.K., Schumacher, B., Pasparakis, M., 2016. The tumour suppressor CYLD regulates the p53 DNA damage response. Nat Commun 7, 12508. doi.org/10.1038/ncomms12508
George, J., Saito, M., Tsuta, K., Iwakawa, R., Shiraishi, K., Scheel, A.H., Uchida, S., Watanabe, S.-I., Nishikawa, R., Noguchi, M., Peifer, M., Jang, S.J., Petersen, I., Büttner, R., Harris, C.C., Yokota, J., Thomas, R.K., Kohno, T., 2016. Genomic Amplification of CD274 (PD-L1) in Small-Cell Lung Cancer. Clin. Cancer Res. doi.org/10.1158/1078-0432.CCR-16-1069
Henssen, A., Althoff, K., Odersky, A., Beckers, A., Koche, R., Speleman, F., Schäfers, S., Bell, E., Nortmeyer, M., Westermann, F., De Preter, K., Florin, A., Heukamp, L., Spruessel, A., Astrahanseff, K., Lindner, S., Sadowski, N., Schramm, A., Astorgues-Xerri, L., Riveiro, M.E., Eggert, A., Cvitkovic, E., Schulte, J.H., 2016. Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition. Clin. Cancer Res. 22, 2470–2481. doi.org/10.1158/1078-0432.CCR-15-1449
Ikram, F., Ackermann, S., Kahlert, Y., Volland, R., Roels, F., Engesser, A., Hertwig, F., Kocak, H., Hero, B., Dreidax, D., Henrich, K.-O., Berthold, F., Nürnberg, P., Westermann, F., Fischer, M., 2016. Transcription factor activating protein 2 beta (TFAP2B) mediates noradrenergic neuronal differentiation in neuroblastoma. Mol Oncol 10, 344–359. doi.org/10.1016/j.molonc.2015.10.020
Meder, L., König, K., Ozretić, L., Schultheis, A.M., Ueckeroth, F., Ade, C.P., Albus, K., Boehm, D., Rommerscheidt-Fuss, U., Florin, A., Buhl, T., Hartmann, W., Wolf, J., Merkelbach-Bruse, S., Eilers, M., Perner, S., Heukamp, L.C., Buettner, R., 2016. NOTCH, ASCL1, p53 and RB alterations define an alternative pathway driving neuroendocrine and small cell lung carcinomas. Int. J. Cancer 138, 927–938. doi.org/10.1002/ijc.29835
Ortiz-Cuaran, S., Scheffler, M., Plenker, D., Dahmen, L., Scheel, A.H., Fernandez-Cuesta, L., Meder, L., Lovly, C.M., Persigehl, T., Merkelbach-Bruse, S., Bos, M., Michels, S., Fischer, R., Albus, K., König, K., Schildhaus, H.-U., Fassunke, J., Ihle, M.A., Pasternack, H., Heydt, C., Becker, C., Altmüller, J., Ji, H., Müller, C., Florin, A., Heuckmann, J.M., Nuernberg, P., Ansén, S., Heukamp, L.C., Berg, J., Pao, W., Peifer, M., Buettner, R., Wolf, J., Thomas, R.K., Sos, M.L., 2016. Heterogeneous Mechanisms of Primary and Acquired Resistance to Third-Generation EGFR Inhibitors. Clin. Cancer Res. 22, 4837–4847. doi.org/10.1158/1078-0432.CCR-15-1915
Radi, M., Schneider, R., Fallacara, A.L., Botta, L., Crespan, E., Tintori, C., Maga, G., Kissova, M., Calgani, A., Richters, A., Musumeci, F., Rauh, D., Schenone, S., 2016. A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant. Bioorg. Med. Chem. Lett. 26, 3436–3440. doi.org/10.1016/j.bmcl.2016.06.051
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2015
Basu, D., Richters, A., Rauh, D., 2015. Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR. Bioorg. Med. Chem. 23, 2767–2780. doi.org/10.1016/j.bmc.2015.04.038
Carter, D.R., Murray, J., Cheung, B.B., Gamble, L., Koach, J., Tsang, J., Sutton, S., Kalla, H., Syed, S., Gifford, A.J., Issaeva, N., Biktasova, A., Atmadibrata, B., Sun, Y., Sokolowski, N., Ling, D., Kim, P.Y., Webber, H., Clark, A., Ruhle, M., Liu, B., Oberthuer, A., Fischer, M., Byrne, J., Saletta, F., Thwe, L.M., Purmal, A., Haderski, G., Burkhart, C., Speleman, F., De Preter, K., Beckers, A., Ziegler, D.S., Liu, T., Gurova, K.V., Gudkov, A.V., Norris, M.D., Haber, M., Marshall, G.M., 2015. Therapeutic targeting of the MYC signal by inhibition of histone chaperone FACT in neuroblastoma. Sci Transl Med 7, 312ra176. doi.org/10.1126/scitranslmed.aab1803
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Engel, J., Richters, A., Getlik, M., Tomassi, S., Keul, M., Termathe, M., Lategahn, J., Becker, C., Mayer-Wrangowski, S., Grütter, C., Uhlenbrock, N., Krüll, J., Schaumann, N., Eppmann, S., Kibies, P., Hoffgaard, F., Heil, J., Menninger, S., Ortiz-Cuaran, S., Heuckmann, J.M., Tinnefeld, V., Zahedi, R.P., Sos, M.L., Schultz-Fademrecht, C., Thomas, R.K., Kast, S.M., Rauh, D., 2015. Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach. J. Med. Chem. 58, 6844–6863. doi.org/10.1021/acs.jmedchem.5b01082
Fang, Z., Simard, J.R., Plenker, D., Nguyen, H.D., Phan, T., Wolle, P., Baumeister, S., Rauh, D., 2015. Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors. ACS Chem. Biol. 10, 279–288. doi.org/10.1021/cb500355c
Fernandez-Cuesta, L., Sun, R., Menon, R., George, J., Lorenz, S., Meza-Zepeda, L.A., Peifer, M., Plenker, D., Heuckmann, J.M., Leenders, F., Zander, T., Dahmen, I., Koker, M., Schöttle, J., Ullrich, R.T., Altmüller, J., Becker, C., Nürnberg, P., Seidel, H., Böhm, D., Göke, F., Ansén, S., Russell, P.A., Wright, G.M., Wainer, Z., Solomon, B., Petersen, I., Clement, J.H., Sänger, J., Brustugun, O.-T., Helland, Å., Solberg, S., Lund-Iversen, M., Buettner, R., Wolf, J., Brambilla, E., Vingron, M., Perner, S., Haas, S.A., Thomas, R.K., 2015. Identification of novel fusion genes in lung cancer using breakpoint assembly of transcriptome sequencing data. Genome Biol. 16, 7. doi.org/10.1186/s13059-014-0558-0
Fey, D., Halasz, M., Dreidax, D., Kennedy, S.P., Hastings, J.F., Rauch, N., Munoz, A.G., Pilkington, R., Fischer, M., Westermann, F., Kolch, W., Kholodenko, B.N., Croucher, D.R., 2015. Signaling pathway models as biomarkers: Patient-specific simulations of JNK activity predict the survival of neuroblastoma patients. Sci Signal 8, ra130. doi.org/10.1126/scisignal.aab0990
George, J., Lim, J.S., Jang, S.J., Cun, Y., Ozretić, L., Kong, G., Leenders, F., Lu, X., Fernández-Cuesta, L., Bosco, G., Müller, C., Dahmen, I., Jahchan, N.S., Park, K.-S., Yang, D., Karnezis, A.N., Vaka, D., Torres, A., Wang, M.S., Korbel, J.O., Menon, R., Chun, S.-M., Kim, D., Wilkerson, M., Hayes, N., Engelmann, D., Pützer, B., Bos, M., Michels, S., Vlasic, I., Seidel, D., Pinther, B., Schaub, P., Becker, C., Altmüller, J., Yokota, J., Kohno, T., Iwakawa, R., Tsuta, K., Noguchi, M., Muley, T., Hoffmann, H., Schnabel, P.A., Petersen, I., Chen, Y., Soltermann, A., Tischler, V., Choi, C., Kim, Y.-H., Massion, P.P., Zou, Y., Jovanovic, D., Kontic, M., Wright, G.M., Russell, P.A., Solomon, B., Koch, I., Lindner, M., Muscarella, L.A., la Torre, A., Field, J.K., Jakopovic, M., Knezevic, J., Castaños-Vélez, E., Roz, L., Pastorino, U., Brustugun, O.-T., Lund-Iversen, M., Thunnissen, E., Köhler, J., Schuler, M., Botling, J., Sandelin, M., Sanchez-Cespedes, M., Salvesen, H.B., Achter, V., Lang, U., Bogus, M., Schneider, P.M., Zander, T., Ansén, S., Hallek, M., Wolf, J., Vingron, M., Yatabe, Y., Travis, W.D., Nürnberg, P., Reinhardt, C., Perner, S., Heukamp, L., Büttner, R., Haas, S.A., Brambilla, E., Peifer, M., Sage, J., Thomas, R.K., 2015. Comprehensive genomic profiles of small cell lung cancer. Nature 524, 47–53. doi.org/10.1038/nature14664
Lindner, S., Bachmann, H.S., Odersky, A., Schaefers, S., Klein-Hitpass, L., Hero, B., Fischer, M., Eggert, A., Schramm, A., Schulte, J.H., 2015. Absence of telomerase reverse transcriptase promoter mutations in neuroblastoma. Biomed Rep 3, 443–446. doi.org/10.3892/br.2015.463
Mayer-Wrangowski, S.C., Rauh, D., 2015. Monitoring ligand-induced conformational changes for the identification of estrogen receptor agonists and antagonists. Angew. Chem. Int. Ed. Engl. 54, 4379–4382. doi.org/10.1002/anie.201410148
Peifer, M., Hertwig, F., Roels, F., Dreidax, D., Gartlgruber, M., Menon, R., Krämer, A., Roncaioli, J.L., Sand, F., Heuckmann, J.M., Ikram, F., Schmidt, R., Ackermann, S., Engesser, A., Kahlert, Y., Vogel, W., Altmüller, J., Nürnberg, P., Thierry-Mieg, J., Thierry-Mieg, D., Mariappan, A., Heynck, S., Mariotti, E., Henrich, K.-O., Gloeckner, C., Bosco, G., Leuschner, I., Schweiger, M.R., Savelyeva, L., Watkins, S.C., Shao, C., Bell, E., Höfer, T., Achter, V., Lang, U., Theissen, J., Volland, R., Saadati, M., Eggert, A., de Wilde, B., Berthold, F., Peng, Z., Zhao, C., Shi, L., Ortmann, M., Büttner, R., Perner, S., Hero, B., Schramm, A., Schulte, J.H., Herrmann, C., O’Sullivan, R.J., Westermann, F., Thomas, R.K., Fischer, M., 2015. Telomerase activation by genomic rearrangements in high-risk neuroblastoma. Nature 526, 700–704. doi.org/10.1038/nature14980
Richters, A., Basu, D., Engel, J., Ercanoglu, M.S., Balke-Want, H., Tesch, R., Thomas, R.K., Rauh, D., 2015. Identification and further development of potent TBK1 inhibitors. ACS Chem. Biol. 10, 289–298. doi.org/10.1021/cb500908d
Scheffler, M., Merkelbach-Bruse, S., Bos, M., Fassunke, J., Gardizi, M., Michels, S., Groneck, L., Schultheis, A.M., Malchers, F., Leenders, F., Kobe, C., König, K., Heukamp, L.C., Sos, M.L., Thomas, R.K., Büttner, R., Wolf, J., 2015. Spatial Tumor Heterogeneity in Lung Cancer with Acquired Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitor Resistance: Targeting High-Level MET-Amplification and EGFR T790M Mutation Occurring at Different Sites in the Same Patient. J Thorac Oncol 10, e40-43. doi.org/10.1097/JTO.0000000000000503
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Schultheis, A.M., Scheel, A.H., Ozretić, L., George, J., Thomas, R.K., Hagemann, T., Zander, T., Wolf, J., Buettner, R., 2015. PD-L1 expression in small cell neuroendocrine carcinomas. Eur. J. Cancer 51, 421–426. doi.org/10.1016/j.ejca.2014.12.006
Weisner, J., Gontla, R., van der Westhuizen, L., Oeck, S., Ketzer, J., Janning, P., Richters, A., Mühlenberg, T., Fang, Z., Taher, A., Jendrossek, V., Pelly, S.C., Bauer, S., van Otterlo, W.A.L., Rauh, D., 2015. Covalent-Allosteric Kinase Inhibitors. Angew. Chem. Int. Ed. Engl. 54, 10313–10316. doi.org/10.1002/anie.201502142
2014
Richters, A., Nguyen, H.D., Phan, T., Simard, J.R., Grütter, C., Engel, J., Rauh, D., 2014. Identification of type II and III DDR2 inhibitors. J. Med. Chem. 57, 4252–4262. doi.org/10.1021/jm500167q