100 Antonchick A.P, S. López-Tosco, J. Parga, S. Sievers, M. Schürmann, H. Preut, S. Höing, H.R. Schöler, J. Sterneckert, D. Rauh, H. Waldmann.  Highly Enantioselective Catalytic Synthesis of Neurite Growth-Promoting Secoyohimbanes Chemistry & Biology, 2013, 20(4):500-9.

99 Becker Kerstin, Claudia Vollbrecht, Ulrike Koitzsch, Katharina Koenig,Jana Fassunke, Sebastian Huss, Peter Nuernberg, Lukas C Heukamp,Reinhard Buettner, Margarete Odenthal, Janine Altmueller, Sabine Merkelbach-Bruse. Deep ion sequencing of amplicon adapter ligated libraries: a novel tool in molecular diagnostics of formalin fixed and paraffin embedded tissues. Journal of Clinical Pathology, jclinpath-2013-201549, in press.

98 Bos M, Gardizi M, Schildhaus HU, Heukamp LC, Geist T, Kaminsky B, Zander T, Nogova L, Scheffler M, Dietlein M, Kobe C, Holstein A, Maintz D, Büttner R, Wolf J. Complete metabolic response in a patient with repeatedly relapsed non-small cell lung cancer harboring ros1 gene rearrangement after treatment with crizotinib. Lung Cancer 2013.

97 Büttner R, Wolf J, Thomas RK. Lessons learned from lung cancer genomics: The emerging concept of individualized diagnostics and treatment. J Clin Oncol 2013.

96 Chatterjee S, Heukamp LC, Siobal M, Schöttle J, Wieczorek C, Peifer M, Frasca D, Koker M, König K, Meder L, Rauh D, Buettner R, Wolf J, Brekken RA, Neumaier B, Christofori G, Thomas RK, Ullrich RT.  Tumor VEGF:VEGFR2 autocrine feed-forward loop triggers angiogenesis in lung cancer. J Clin Invest. 2013 Apr 1;123(4):1732-40.

95 Fang Z., C. Grütter, D. Rauh. Strategies for the Selective Regulation of Kinases with Allosteric Modulators - Exploiting Exclusive Structural Features. ACS Chem Biol, 2013, 8(1):58-70.

94 Jaiswal M, Dvorsky R, Ahmadian MR. Deciphering the Molecular and Functional Basis of Dbl Family Proteins: A NOVEL SYSTEMATIC APPROACH TOWARD CLASSIFICATION OF SELECTIVE ACTIVATION OF THE Rho FAMILY PROTEINS.  J Biol Chem 288, 4486-4500. PMID: 23255595.

93 Over, B., S. Wetzel, C. Grütter, Y. Nakai, S. Renner, D. Rauh, H. Waldmann. Natural product derived fragments for fragment-based ligand discovery. Nat Chemistry, 2013, 5(1):21-8.
92 Rauh, D. Chemical Biology ? current and next challenges. ACS Chem Biol, 2013, 8(1):1-2.

91 Scheffler M, Zander T, Nogova L, Kobe C, Kahraman D, Dietlein M, Papachristou I, Heukamp L, Büttner R, Boellaard R, Lammertsma AA, Querings S, Stoelben E, Engel-Riedel W, Neumaier B, Wolf J:  Prognostic impact of [18f]fluorothymidine and [18f]fluoro-d-glucose baseline uptakes in patients with lung cancer treated first-line with erlotinib.  PLoS One 2013;8:e53081.

90 Schelhorn, S.E. et al. Sensitive Detection of Viral Transcripts in Human Tumor Transcriptomes, erscheint in PLOS Comput Biol 2013.

89 Schneider R., A. Gohla, J.R. Simard, D.B. Yadav, Z. Fang, W.A.L. van Otterlo, D. Rauh. Overcoming compound fluorescence in the FLiK screening assay with red-shifted fluorophores. J Am Chem Soc, 2013, in press.

88 Schneider R., C. Beumer, J.R. Simard, C. Grütter, D. Rauh. Selective Detection of Allosteric Phosphatase Inhibitors. J Am Chem Soc, 2013, 135(18):6838-41.

87 Schultheis A, Wolf J, Büttner R. Lung cancer. Molecular pathology and personalized therapy. Internist (Berl) 2013;54:179-180, 182-177..

86 Tolosi, L., et al. A method for finding consensus breakpoints in the cancer genome from copy number data. Bioinformatics. 2013 Jun 19. [Epub ahead of print].

85 Urich R., G. Wishart, M. Kiczun, A. Richters, N. Tidten-Luksch, D. Rauh, B. Sherborne, P.G. Wyatt and R. Brenk. De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments. ACS Chem Biol, 2013, in press.


84 Bock, C. and T. Lengauer Managing drug resistance in cancer: lessons from HIV therapy.  Nat Rev Cancer, 2012. 12(7): p. 494-501.
83 Brenk R., D. Rauh. Change or be changed: Reflections of the workshop 'Future in Medicinal Chemistry'. Bioorg Med Chem, 2012, 20(12):3695-7.

82 Cancer Genome Atlas Research Network.  Comprehensive genomic characterization of squamous cell lung cancers.  Nature. 2012 Sep 27;489(7417):519-25. doi: 10.1038/nature11404. Epub 2012 Sep 9. Erratum in: Nature. 2012 Nov 8;491(7423):288. Rogers, Kristen [corrected to Rodgers, Kristen].

81 Chmielecki J, Peifer M, Viale A, Hutchinson K, Giltnane J, Socci ND, Hollis CJ, Dean RS, Yenamandra A, Jagasia M, Kim AS, Davé UP, Thomas RK, Pao W.  Systematic screen for tyrosine kinase rearrangements identifies a novel C6orf204-PDGFRB fusion in a patient with recurrent T-ALL and an associated myeloproliferative neoplasm.  Genes Chromosomes Cancer. 2012 Jan;51(1):54-65. doi: 10.1002/gcc.20930. Epub 2011 Sep 21.

80 Cirstea IC, Gremer L, Dvorsky R, Zhang SC, Piekorz RP, Zenker M, Ahmadian MR. Diverging gain-of-function mechanisms of two novel KRAS mutations associated with Noonan and cardio-facio-cutaneous syndromes.  Hum Mol Genet 22, 262-270. PMID: 23059812

79 Frasa MA, Koessmeier KT, Ahmadian MR, Braga VM.  Illuminating the functional and structural repertoire of human TBC/RABGAPs.  Nat Rev Mol Cell Biol 13:67-73. PMID: 22251903

78 Gärtner J, Wolf J, Voltz R. Early palliative care for patients with metastatic cancer. Curr Opin Oncol 2012;24:357-362
77 Getlik, M., C. Grütter, J.R. Simard, H.D. Nguyen, A. Robubi, B. Aust, W.A. van Otterlo* and D. Rauh. Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38? Eur J Med Chem, 2012, 48:1-15.

76 Getlik, M., J.R. Simard, M. Termathe, C. Grütter, M. Rabiller, W.A.L. van Otterlo, D. Rauh. Fluorophore labeled kinase detects ligands that bind within the MAPK insert of p38?Kinase PLoS ONE, 2012, 7(7):e39713.

75 Grütter, C., J.R. Simard, S.C. Mayer-Wrangowski, P.H. Schreier, J. Pérez-Martín, A. Richters, M. Getlik, O. Gutbrod, C.A. Braun, M.E. Beck, D. Rauh. Targeting GSK3 from Ustilago maydis: Type-II kinase Inhibitors as Potential Antifungals ACS. Chem Biol, 2012, 7(7):1257-67

74 Heuckmann JM, Balke-Want H, Malchers F, Peifer M, Sos ML, Koker M, Meder L, Lovly CM, Heukamp LC, Pao W, Küppers R, Thomas RK.  Differential protein stability and ALK inhibitor sensitivity of EML4-ALK fusion variants.  Clin Cancer Res. 2012 Sep 1;18(17):4682-90. doi: 10.1158/1078-0432.CCR-11-3260. Epub 2012 Aug 21.

73 Kahraman D, Holstein A, Scheffler M, Zander T, Nogova L, Lammertsma AA, Boellaard R, Neumaier B, Dietlein M, Wolf J, Kobe C. Tumor lesion glycolysis and tumor lesion proliferation for response prediction and prognostic differentiation in patients with advanced non-small cell lung cancer treated with erlotinib.  Clin Nucl Med 2012;37:1058-1064

72 Kobe C, Scheffler M, Holstein A, Zander T, Nogova L, Lammertsma AA, Boellaard R, Neumaier B, Ullrich RT, Dietlein M, Wolf J, Kahraman D. Predictive value of early and late residual 18f-fluorodeoxyglucose and 18f-fluorothymidine uptake using different suv measurements in patients with non-small-cell lung cancer treated with erlotinib.  Eur J Nucl Med Mol Imaging 2012;39:1117-1127

71 Koch, A., H.B. Rode, A. Richters, D. Rauh, S. Hauf. A chemical genetic approach for covalent inhibition of analogue-sensitive aurora kinase ACS Chem Biol, 2012, 7(4):723-31.

70 Koeberle, S.C., S. Fischer, D. Schollmeyer, V. Schattel, C. Grütter, D. Rauh, S. A. Laufer. Design, Synthesis, and Biological Evaluation of Novel Disubstituted Dibenzosuberones as Highly Potent and Selective Inhibitors of p38 Mitogen Activated Protein Kinase J Med Chem, 2012, 55(12):5868-77.

69 Martz K., A. Dorn, B. Baur, V. Schattel, M. Goettert, S. Mayer-Wrangowski, D. Rauh, S.A. Laufer.  Targeting the hinge glycine flip and the activation loop: novel approach to potent p38? inhibitors.  J Med Chem, 2012, 55(17):7862-74.

68 Mayer-Wrangowski, S., D. Rauh. Symbiose aus Chemie und Medizin - Zielgerichtet gegen Krebs. BIOspektrum, 2012, 18(4):376:79.

67 Netzer C, Rahnenführer J.   Sample size estimation for cancer progression models. International Journal of  Computational Bioscience. 2012, Vol.1, 1:10.

66 Perez-Moreno P, Brambilla E, Thomas R, Soria JC.  Squamous cell carcinoma of the lung: molecular subtypes and therapeutic opportunities. Clin Cancer Res. 2012 May 1;18(9):2443-51. doi: 10.1158/1078-0432.CCR-11-2370. Epub 2012 Mar 8. Review.

65 Schildhaus HU, Heukamp LC, Merkelbach-Bruse S, Riesner K, Schmitz K, Binot E, Paggen E, Albus K, Schulte W, Ko YD, Schlesinger A, Ansén S, Engel-Riedel W, Brockmann M, Serke M, Gerigk U, Huss S, Goke F, Perner S, Hekmat K, Frank KF, Reiser M, Schnell R, Bos M, Mattonet C, Sos M, Stoelben E, Wolf J, Zander T, Buettner R. Definition of a fluorescence in-situ hybridization score identifies high- and low-level fgfr1 amplification types in squamous cell lung cancer.  Mod Pathol 2012;25:1473-1480

64 Schneider, R., C. Becker, J.R. Simard, M. Getlik, N. Bohlke, P. Janning, D. Rauh. Direct Binding Assay for the Detection of Type IV Allosteric Inhibitors of Abl.  J Am Chem Soc, 2012, 134(22):9138-41.

63 Shymanets A, Ahmadian MR, Koessmeier KT, Wetzker R, Harteneck C, Nürnberg B. The p101 subunit of PI3K? restores activation by G? mutants deficient in stimulating p110?. Biochem J 441, 851-858. PMID: 22054284.                                                            
62 Simard, J.R, D. Rauh. Fluorescence labels in kinases: a high-throughput kinase binding assay for the identification of DFG-out binding ligands. Methods Mol Biol, 2012;800:95-117.

61 Thomas R, Wolf J: Personalized therapy of lung cancer. Onkologie 2012;35 Suppl 1:14-19.
60 Ullrich RT, Zander T, Wolf J, Hallek M. Personalised treatment of lung cancer. Dtsch Med Wochenschr 2012;137:2179-2180.
59 Zhang J, Zhang L, Su X, Li M, Xie L, Malchers F, Fan S, Yin X, Xu Y, Liu K, Dong Z, Zhu G, Qian Z, Tang L, Zhan P, Ji Q, Kilgour E, Smith PD, Brooks AN, Thomas RK, Gavine PR.  Translating the therapeutic potential of AZD4547 in FGFR1-amplified non-small cell lung cancer through the use of patient-derived tumor xenograft models.  Clin Cancer Res. 2012 Dec 15;18(24):6658-67. doi: 10.1158/1078-0432.CCR-12-2694. Epub 2012 Oct 18.


58 Chmielecki J, Foo J, Oxnard GR, Hutchinson K, Ohashi K, Somwar R, Wang L, Amato KR, Arcila M, Sos ML, Socci ND, Viale A, de Stanchina E, Ginsberg MS, Thomas RK, Kris MG, Inoue A, Ladanyi M, Miller VA, Michor F, Pao W. Optimization of dosing for EGFR-mutant non-small cell lung cancer with evolutionary cancer modeling. Sci Transl Med. 2011 Jul 6;3(90):90ra59.

57 Di Gion P, Kanefendt F, Lindauer A, Scheffler M, Doroshyenko O, Fuhr U, Wolf J, and Jaehde U. Clinical pharmacokinetics of tyrosine kinase inhibitors: focus on pyrimidines, pyridines and pyrroles. Clin Pharmacokinet. 2011 vol. 50 (9) pp. 551-603.

56 Gaertner J, Wolf J, Frechen S, Klein U, Scheicht D, Hellmich M, Toepelt K, Glossmann JP,  Ostgathe C, Hallek M, Voltz R. Recommending early integration of palliative care - does it work? Support Care Cancer. 2012 Mar;20(3):507-13. Epub 2011 Feb 19.

55 Gaertner J, Wuerstlein R, Klein U, Scheicht D, Frechen S, Wolf J, Hellmich M, Mallmann P, Harbeck N, Voltz R. Integrating Palliative Medicine into Comprehensive Breast Cancer Therapy - a Pilot Project. Breast Care (Basel). 2011;6(3):215-220. Epub 2011 Jun 14.

54 Gremer L, Merbitz-Zahradnik T, Dvorsky R, Cirstea IC, Kratz CP, Zenker M, Wittinghofer A, Ahmadian MR. Impacts of germline mutations in KRAS on the GTPase cycle and effector interaction. Hum Mutat 32, 33-43. PMID: 20949621

53 Herrmann A, Haake A, Ammerpohl O, Martin-Guerrero I, Szafranski K, Stemshorn K, Nothnagel M, Kotsopoulos SK, Richter J, Warner J, Olson J, Link DR, Schreiber S, Krawczak M, Platzer M, Nürnberg P, Siebert R, Hampe J. Pipeline for large-scale microdroplet bisulfite PCR-based sequencing allows the tracking of hepitype evolution in tumors. PLoS One. 2011;6(7):e21332. Epub 2011 Jul 5. PMID: 21750708 [PubMed - indexed for MEDLINE]

52 Heuckmann, J.M., M. Hölzel, M.L. Sos, S. Heynck, H. Balke-Want, M. Koker, M. Peifer, J. Weiss, C.M. Lovly, C. Grütter, D. Rauh, W. Pao, R.K. Thoma. ALK mutations conferring differential resistance to structurally diverse ALK inhibitors. Clin Cancer Res, 2011, 17(23):7394-401.

51 Kahraman D, Scheffler M, Zander T, Nogova L, Lammertsma A, Boellaard R, Neumaier B, Ullrich R, Holstein A, Dietlein M, Wolf J, Kobe C. Quantitative Analysis of Response to Treatment with Erlotinib in Advanced Non?Small Cell Lung Cancer Using 18F-FDG and 39-Deoxy-39-18F-Fluorothymidine PET. Journal of Nuclear Medicine, published on November 7, 2011 as  doi:10.2967/jnumed.111.094458

50 Köberle, S.C., J. Romir, S. Fischer, A. Köberle, V. Schattel, W. Albrecht, C. Grütter, O. Werz, D. Rauh, T. Stehle, S.A. Laufer. Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. Nat Chem Biol, 2011, 8(2):141-43.

49 Kraft M, Cirstea IC, Voss AK, Thomas T, Goehring I, Sheikh BN, Gordon L, Scott H, Smyth GK, Ahmadian MR, Trautmann U, Zenker M, Tartaglia M, Ekici A, Reis A, Dörr HG, Rauch A, Thiel CT. Disruption of the histone acetyltransferase MYST4 leads to a Noonan syndrome-like phenotype and hyperactivated MAPK signaling in humans and mice. J Clin Invest 121:3479-3491. PMID:21804188

48 Park KS, Martelotto LG, Peifer M, Sos ML, Karnezis AN, Mahjoub MR, Bernard K, Conklin JF, Szczepny A, Yuan J, Guo R, Ospina B, Falzon J, Bennett S, Brown TJ, Markovic A, Devereux WL, Ocasio CA, Chen JK, Stearns T, Thomas RK, Dorsch M, Buonamici S, Watkins DN, Peacock CD, Sage J. A crucial requirement for Hedgehog signaling in small cell lung cancer. Nat Med. 2011 Oct 9;17(11):1504-8. doi: 10.1038/nm.2473

47 Querings S, Altmüller J, Ansén S, Zander T, Seidel D, Gabler F, Peifer M, Markert E, Stemshorn K, Timmermann B, Saal B, Klose S, Ernestus K, Scheffler M, Engel-Riedel W, Stoelben E, Brambilla E, Wolf J, Nürnberg P, Thomas RK. Benchmarking of mutation diagnostics in clinical lung cancer specimens. PLoS One. 2011 May 5;6(5):e19601.

46 Rode, H., M.L. Sos, C. Grütter, S. Heynck, J.R. Simard, D. Rauh. Synthesis and biological evaluation of 7-substituted-1-(3-bromophenylamino) isoquinoline-4-carbonitriles as inhibitors of Myosine Light Chain Kinase and Epidermal Growth Factor Receptor. Bioorg Med Chem, 2011, 19(1):429-39.

45 Tolosi L, Lengauer T. Classification with correlated features: unreliability of feature ranking and solutions. Bioinformatics. 2011 Jul 15;27(14):1986-94. Epub 2011 May 16.

44 Tückmantel, S., J.N. Greul, P. Janning, A. Brockmeyer, C. Grütter, J.R. Simard, O. Gutbrod, M.E. Beck, K. Tietjen, D. Rauh, P.H. Schreier. Identification of Ustilago maydis Aurora Kinase As a Novel Antifungal Target. ACS Chem Biol, 2011, 6(9):926-33.

43 Vansteenkiste J, Solomon B, Boyer M, Wolf J, Miller N, Di Scala L, Pylvaenaeinen I, Petrovic K, Dimitrijevic S, Anrys B, Laack E. Everolimus in Combination with Pemetrexed in Patients with Advanced Non-small Cell Lung Cancer Previously Treated with Chemotherapy: A Phase I Study Using a Novel, Adaptive Bayesian Dose-Escalation Model. J Thorac Oncol. 2011 Dec;6(12):2120-9.

42 Vintonyak, V.V., H. Waldmann, D. Rauh. Using small molecules to target protein phosphatases. Bioorg Med Chem, 2011, 19(7):2145-55.

41 Vintonyak, V.V., K. Warburg, B. Over, K. Hübel, D. Rauh, H. Waldmann. Identification and further development of thiazolidinones spiro-fused to indolin-2-ones as potent and selective inhibitors of Mycobacterium tuberculosis Protein Tyrosine Phosphatase B. Tetrahedron, 2011, 67(35):6713-29.

40 Zander T, Hofmann A, Staratschek-Jox A, Classen S, Debey-Pascher S, Maisel D, Ansén S, Hahn M, Beyer M, Thomas RK, Gathof B, Mauch C, Delank KS, Engel-Riedel W, Wichmann HE, Stoelben E, Schultze JL, Wolf J. Blood-based gene expression signatures in non-small cell lung cancer. Clin Cancer Res. 2011 May 15;17(10):3360-7. Epub 2011 May 10

39 Zander T, Scheffler M, Nogova L, Kobe C, Engel-Riedel W, Hellmich M, Papachristou I, Toepelt K, Draube A, Heukamp L, Buettner R, Ko YD, Ullrich RT, Smit E, Boellaard R, Lammertsma AA, Hallek M, Jacobs AH, Schlesinger A, Schulte K, Querings S, Stoelben E, Neumaier B, Thomas RK, Dietlein M, Wolf J Early Prediction of Nonprogression in Advanced Non-Small-Cell Lung Cancer Treated With Erlotinib By Using [18F]Fluorodeoxyglucose and [18F]Fluorothymidine Positron Emission Tomography. J Clin Oncol. 2011 Mar 21. [Epub ahead of print]


38 Altmann A, Tolosi L, Sander O, Lengauer T. Permutation importance:a corrected feature importance measure. Bioinformatics. 2010 Apr.

37 Ansén S, Bangard C, Querings S, Gabler F, Scheffler M, Seidel D, Saal B, Zander T, Nogová L, Töpelt K, Markert E, Stoelben E, Ernestus K, Thomas RK, Wolf J. Osteoblastic response in patients with non-small cell lung cancer with activating EGFR Mutations and bone metastases during treatment with EGFR kinase inhibitors.  J Thorac Oncol. 2010 Mar;5(3):407-9.

36 Antonchick, A. C. Gerding-Reimers, M. Catarinella, S. Ziegler, D. Rauh and H. Waldmann. Highly Enantioselective Synthesis and Cellular Evaluation of Natural Product-Inspired Spirooxindoles, Nature Chemistry, 2010, 2(9):735-40

35 Chmielecki J, Peifer M, Jia P, Socci ND, Hutchinson K, Viale A, Zhao Z, Thomas RK, Pao W.  Targeted next-generation sequencing of DNA regions proximal to a conserved GXGXXG signaling motif enables systematic discovery of tyrosine kinase fusions in cancer. Nucleic Acids Res. 2010 Nov 1;38(20):6985-96. Epub 2010 Jun 29

34 Cirstea IC, Kutsche K, Dvorsky R, Gremer L, Carta C, Horn D, Roberts AE, Lepri F, Merbitz-Zahradnik T, Konig, R, Kratz CP, Pantaleoni F, Dentici ML, Joshi VA, Kucherlapati RS, Mazzanti L, Mundlos S, Patton MA, Silengo MC, Rossi C, Zampino G, Digilio C, Stuppia L, Seemanova E, Pennacchio LA, Gelb BD, Dallapiccola B, Wittinghofer A, Ahmadian MR, Tartaglia M, Zenker M. A restricted spectrum of NRAS mutations causes Noonan syndrome. Nat Genet 42, 27-29. PMID: 19966803

33 Dekker, F.J., O. Rocks, N. Vartak, S. Menninger, C. Hedberg, R. Balamurugan, S. Wetzel, S. Renner, M. Gerauer, B. Schölermann, M. Rusch, J.W. Kramer, D. Rauh, G.W. Coates, L. Brunsveld, P.I. Bastiaens*, H. Waldmann. Small-molecule inhibition of APT1 affects Ras localization and signaling, Nat Chem Biol, 2010, 6(6):449-56

32 Gremer L, De Luca A, Merbitz-Zahradnik T, Dallapiccola B, Morlot S, Tartaglia M, Kutsche K, Ahmadian MR, Rosenberger G. Duplication of Glu37 in the switch I region of HRAS impairs effector/GAP binding and underlies Costello syndrome by promoting enhanced growth factor-dependent MAPK and AKT activation. Hum Mol Genet 19, 790-802. PMID: 19995790

31 Gremer L, Merbitz-Zahradnik T, Dvorsky R, Cirstea IC, Kratz CP, Zenker M, Wittinghofer A,  Ahmadian M. Impacts of germline mutations in KRAS on the GTPase cycle and effector interaction. Hum Mutat 32, 33-43. PMID: 20949621

30 Klüter, S., C. Grütter, M. Rabiller, V. Pawar, M. Getlik, J.R. Simard, D. Rauh. Structure-based development of a displacement assay for the detection of stabilizers of inactive kinase conformations. J Med Chem, 2010, 53(1):357-67

29 Klüter, S., J.R. Simard, H. Rode, C. Grütter, V. Pawar, H.C.A. Raaijmakers, T.A. Barf, M. Rabiller, W.A.L. van Otterlo, D. Rauh. Characterization of irreversible kinase inhibitors by directly detecting covalent bond formation: a tool for dissecting kinase drug resistance, Chem BioChem, 2010, 11(18):2557-6

28 Pawar, V., M. Sos, H. Rode, M. Rabiller, S. Heynck, W. van Otterlo, R. Thomas, D. Rauh. Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of EGFR, J Med Chem, 2010, 53(7):2892-901

27 Peifer M, Weiss J, Sos ML, Koker M, Heynck S, Netzer C, Fischer S, Rode H, Rauh D, Rahnenführer J, Thomas RK. Analysis of compound synergy in high-throughput cellular screens by population-based lifetime modeling. PLoS One. 2010 Jan 27;5(1):e8919

26 Rabiller M., M. Getlik, S. Klüter, S. Tückmantel, A. Richters, J.R. Simard, D. Rauh. Proteus in the World of Proteins: Conformational Changes in Protein Kinases, Arch Pharm (Weinheim), 2010, 343(4):193-206

25 Rauh D. Inaktive Kinasekonformationen stabilisieren. Nachrichten aus der Chemie, Gesellschaft Deutscher Chemiker, 2010, 58(2)

24 Robubi, A., H. Waldmann, D. Rauh. RAF kinase inhibitors in cancer treatment: like a bull in a china shop?, ChemBioChem, 2010, 11(12):1645-8

23 Schmidt S, Schneider L, Essmann F, Cirstea IC, Kuck F, Kletke A, Jänicke RU, Wiek C, Hanenberg H, Ahmadian MR, Schulze-Osthoff K, Nürnberg B, Piekorz RP. The centrosomal protein TACC3 controls paclitaxel sensitivity by modulating a premature senescence program. Oncogene 29, 6184-92. PMID: 20729911

22 Simard, J.R., M. Getlik, C. Grütter, R. Schneider, S. Wulfert, D. Rauh. Fluorophore-labeling of the glycine-rich loop as a method of identifying inhibitors which bind to active and inactive kinase conformations. J Am Chem Soc, 2010, 132(12):4152-60

21 Sos ML, Rode HB, Heynck S, Peifer M, Fischer F, Klüter S, Pawar VG, Reuter C, Heuckmann JM, Weiss J, Ruddigkeit L, Rabiller M, Koker M, Simard JR, Getlik M, Yuza Y, Chen TH, Greulich H, Thomas RK, Rauh D. Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation. Cancer Res. 2010 Feb 1;70(3):868-74.

20 Truong T, Hung RJ, Amos CI, Wu X, Bickeböller H, Rosenberger A, Sauter W, Illig T, Wichmann HE, Risch A, Dienemann H, Kaaks R, Yang P, Jiang R, Wiencke JK, Wrensch M, Hansen H, Kelsey KT, Matsuo K, Tajima K, Schwartz AG, Wenzlaff A, Seow A, Ying C, Staratschek-Jox A, Nürnberg P, Stoelben E, Wolf J, Lazarus P, Muscat JE, Gallagher CJ, Zienolddiny S, Haugen A, van der Heijden HF, Kiemeney LA, Isla D, Mayordomo JI, Rafnar T, Stefansson K, Zhang ZF, Chang SC, Kim JH, Hong YC, Duell EJ, Andrew AS, Lejbkowicz F, Rennert G, Müller H, Brenner H, Le Marchand L, Benhamou S, Bouchardy C, Teare MD, Xue X, McLaughlin J, Liu G, McKay JD, Brennan P, Spitz MR. Replication of lung cancer susceptibility loci at chromosomes 15q25, 5p15, and 6p21: a pooled analysis from the International Lung Cancer Consortium.. J Natl Cancer Inst. 2010 Jul 7;102(13):959-71. Epub 2010 Jun 14.

19 Vintonyak, V.V., K. Warburg, H. Kruse, S. Grimme, K. Hübel, D. Rauh and H. Waldmann. Identification of Spiro-fused Indolin-2-one-thiazolidinones as Potent and Selective Inhibitors of Mycobacterium tuberculosis Protein Tyrosine Phosphatase B, Angew Chem Int Ed Engl, 2010, 49(34):5902-5

18 Weiss, J., M. Sos*, D. Seidel, M. Peifer, T. Zander, J. Heuckmann, R. Ullrich, R. Menon, S. Maier, A. Soltermann, H. Moch, P. Wagener, F. Fischer, S. Heynck, M. Koker, J. Schöttle, F. Leenders, F. Gabler, I. Dabow, S. Querings, L. Heukamp, H. Balke-Want, S. Ansén, D. Rauh, I. Baessmann, J. Altmüller, Z.Wainer, M. Conron, G. Wright, B. Solomon, E. Brambilla, C. Brambilla, P. Lorimier, S. Solberg, O. T. Brustgun, W. Engel-Riedel, C. Ludwig, I. Petersen, J. Sänger, J. Clement, H. Groen, W. Timens, H. Sietsma, E. Thunnissen, E. Smit, D. Heideman, F. Cappuzzo, C. Ligorio, S. Damiani, R. Beroukhim, W. Pao, B. Klebl, M. Baumann, R. Buettner, K. Ernestus, E. Stoelben, J. Wolf, P. Nürnberg, S. Perner, R. Thomas. Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous-cell lung cancer, Sci Transl Med, 2010, 2(62):62-9

17 Wetzel, S., W. Wilk, S. Chammaa, B. Sperl, A. Roth, A. Yektaoglu, S. Renner, T. Berg, C. Arenz, A. Giannis, T.I. Oprea, D. Rauh, M. Kaiser, H. Waldmann, A. Scaffold-Tree-Merging Strategy for Prospective Bioactivity Annotation of gamma-Pyrones, Angew Chem Int Ed Engl, 2010, 49(21):3666-70


16 Barbie DA, Tamayo P, Boehm JS, Kim SY, Moody SE, Dunn IF, Schinzel AC, Sandy P, Meylan E, Scholl C, Fröhling S, Chan EM, Sos ML, Michel K, Mermel C, Silver SJ, Weir BA, Reiling JH, Sheng Q, Gupta PB, Wadlow RC, Le H, Hoersch S, Wittner BS, Ramaswamy S, Livingston DM, Sabatini DM, Meyerson M, Thomas RK, Lander ES, Mesirov JP, Root DE, Gilliland DG, Jacks T, Hahn WC. Systematic RNA interference reveals that oncogenic KRAS-driven cancers require TBK1. Nature. 2009 Nov 5;462(7269):108-12

15 Getlik, M., Grutter, C., Simard, J.R., Kluter, S., Rabiller, M., Rode, H.B., Robubi, A., and Rauh, D. (2009). Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. J Med Chem, 2009, 52, 3915-3926.

14 Gong Y, Yao E, Shen R, Goel A, Arcila M, Teruya-Feldstein J, Zakowski MF, Frankel S, Peifer M, Thomas RK, Ladanyi M, Pao W. High expression levels of total IGF-1R and sensitivity of NSCLC cells in vitro to an anti-IGF-1R antibody (R1507). PLoS One. 2009 Oct 6;4(10):e7273.

13 LaFramboise T, Winckler W, Thomas RK. A flexible rank-based framework for detecting copy number aberrations from array data. Bioinformatics.  2009 Mar 15;25(6):722-8

12 Renner S., W. van Otterlo, M. Dominguez Seoane, S. Möcklinghoff, B. Hofmann, S. Wetzel, A. Schuffenhauer, P. Ertl, T. Oprea, D. Steinhilber, L. Brunsveld, D. Rauh, H. Waldmann. (2009). Bioactivity-Guided Mapping of and Navigation in Chemical Space. Nat Chem Biol, 2009, 5(8):585-92

11 Simard, J.R., and Rauh, D. (2009). Chemical and structural biology to direct the repurposing of sulindac. ChemMedChem 4, 2009, 1793-1795.

10 Simard, J.R., Getlik, M., Grutter, C., Pawar, V., Wulfert, S., Rabiller, M., and Rauh, D. (2009). Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors. J Am Chem Soc 131, 2009, 13286-13296.

9 Simard, J.R., Grutter, C., Pawar, V., Aust, B., Wolf, A., Rabiller, M., Wulfert, S., Robubi, A., Kluter, S., Ottmann, C., et al. (2009). High-throughput screening to identify inhibitors which stabilize inactive kinase conformations in p38alpha. J Am Chem Soc 131, 2009, 18478-18488.

8 Simard, J.R., S. Klüter, C. Grütter, M. Rabiller, H.B. Rode, D. Rauh. (2009). A new screening assay for allosteric inhibitors of cSrc. Nat Chem Biol, 2009, 5(6):394-6

7 Soria JC, Shepherd FA, Douillard JY, Wolf J, Giaccone G, Crino L, Cappuzzo F, Sharma S, Gross SH, Dimitrijevic S, Di Scala L, Gardner H, Nogova L, Papadimitrakopoulou V. Efficacy of everolimus (RAD001) in patients with advanced NSCLC previously treated with chemotherapy alone or with chemotherapy and EGFR inhibitors. Ann Oncol. 2009 Oct;20(10):1674-81. Epub 2009 Jun 23.

6 Sos ML, Fischer S, Ullrich R, Peifer M, Heuckmann JM, Koker M, Heynck S, Stückrath I, Weiss J, Fischer F, Michel K, Goel A, Regales L, Politi KA, Perera S, Getlik M, Heukamp LC, Ansén S, Zander T, Beroukhim R, Kashkar H, Shokat KM, Sellers WR, Rauh D, Orr C, Hoeflich KP, Friedman L, Wong KK, Pao W, Thomas RK.Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer. Proc Natl Acad Sci U S A. 2009 Oct 27; 106(43):18351-6

5 Sos ML, Koker M, Weir BA, Heynck S, Rabinovsky R, Zander T, Seeger JM, Weiss J, Fischer F, Frommolt P, Michel K, Peifer M, Mermel C, Girard L, Peyton M, Gazdar AF, Minna JD, Garraway LA, Kashkar H, Pao W, Meyerson M, Thomas RK. PTEN loss contributes to erlotinib resistance in EGFR-mutant lung cancer by activation of Akt and EGFR. Cancer Res. 2009 Apr 15; 69(8):3256-61.

4 Sos ML, Michel K, Zander T, Weiss J, Frommolt P, Peifer M, Li D, Ullrich R, Koker M, Fischer F, Shimamura T, Rauh D, Mermel C, Fischer S, Stückrath I, Heynck S, Beroukhim R, Lin W, Winckler W, Shah K, LaFramboise T, Moriarty WF, Hanna M, Tolosi L, Rahnenführer J, Verhaak R, Chiang D, Getz G, Hellmich M, Wolf J, Girard L, Peyton M, Weir BA, Chen TH, Greulich H, Barretina J, Shapiro GI, Garraway LA, Gazdar AF, Minna JD, Meyerson M, Wong KK, Thomas RK. Predicting drug susceptibility of non-small cell lung cancers based on genetic lesions. J Clin Invest. 2009 Jun; 119(6): 1727-40. doi: 10.1172/JCI37127. Epub 2009 May 18.

3 Triola, G., Wetzel, S., Ellinger, B., Koch, M.A., Hubel, K., Rauh, D., and Waldmann, H. ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds. Bioorg Med Chem 2009, 17, 1079-1087.

2 Vintonyak, V.V., Antonchick, A.P., Rauh, D., and Waldmann, H. (2009). The therapeutic potential of phosphatase inhibitors. Curr Opin Chem Biol, 2009, 13, 272-283.

1 Wetzel S., K. Klein, S. Renner, D. Rauh, T. Oprea, P. Mutzel, H. Waldmann. (2009). Interactive Exploration of Chemical Space with Scaffold Hunter. Nat Chem Biol; 2009; 5(8):581-3