Oncogene Links

Publications:

Peifer, M., Weiss, J., Sos, M.L., Koker, M., Heynck, S., Netzer, C., Fischer, S., Rode, H., Rauh, D., Rahnenführer, J., Thomas, R.K.
Analysis of Compound Synergy in high-throughput Cellular Screens by Population-Based Lifetime Modelling.
PLoS ONE, 2010, 5(1): e8919
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Sos, M.L., Fischer, S., Ullrich, R., Peifer, M., Heuckmann, J.M., Koker, M., Heynck, S., Stückrath, I., Weiss, J., Fischer, F., Michel, K., Goel, A., Regales, L., Politi, K.A., Perera, S., Getlik, M., Heukamp, L.C., Ansén, S., Zander, T., Beroukhim, R., Kashkarh, H., Shokat, K.M., Sellers, W.R., Rauh, D., Orr, C., Hoeflich, K.P., Friedman, L., Wong, K., Paon, W. and Thomas, R.K
Identifying genotype-dependent eficacy of single and combined PI3K- and MAPK- pathway inhibition in cancer.
PNAS, 2009, 106:18351-18356;
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Sos, M.L., 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, B., Lin, W., Winckler, W., Shah, K., LaFramboise, T., Moriarty, W.F., Hanna, M., Tolosi, L., Rahnenführer, J., Verhaak, R., Chiang, D., Getz, G., Hellmich, M., Wolf, J., Girard, L., Peyton, M., Weir, B.A., Chen, T., Greulich, H., Barretina, J., Shapiro, G.I., Garraway, L.A., Gazdar, A.F, Minna, J. D., Meyerson, M., Wong, K. and Thomas, R.K.
Predicting drug susceptibilityof non-small cell lung cancers based on genetic legions.
J Clin Invest, 2009; 119(6):1727-1740.
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Sos, M.L., Koker, M., Weir, B.A., Heynck, S., Rabinovsky, R., Zander, T., Seeger, J.M., Weiss, J., Fischer, F., Frommolt, P., Michel, K., Peifer, M., Mermel, C., Girard, L., Peyton, M., Gazdar, A.F., Minna, J.D., Garraway, L.A., Kashkar, H., Pao, W., Meyerson, M. and Roman K. Thomas
PTEN Loss Contributes to Erlotinib Resistance in EGFR-Mutant Lung Cancer by Activation of Akt and EGFR.
Cancer Res, 2009 69:3256-3261
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Barbie, D.A., Tamayo, P., Boehm, J.S., Kim, S.Y., Moody, S.E., Dunn, I.F., Schinzel, A.C., Sandy, P., Meylan, E., Scholl, C., Fröhling, S., Chan, E.M., Sos, M.L., Michel, K., Mermel, C., Silver, S.j., Weir, B.A., Reiling, J.H., Sheng, Q., Gupta, P.B., Wadlow, R.C., Le, H., Hoersch, S., Wittner, B.S., Ramaswamy, S., Livingston, D.M., Sabatini, D.M., Meyerson, M, Thomas, R.K., Lander, E.S., Mesirov, J.P., Root, D.E., Gilliland, D.G., Jacks T, and Hahn, W.C.
Systematic RNA interference reveals that oncogenic KRAS-driven cancers require TBK1.
Nature, 2009; 462, 108-112
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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
Bioactivity-Guided Mapping of and Navigation in Chemical Space.
Nat Chem Biol, 2009, 5(8):585-92
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Simard, J.R., S. Klüter, C. Grütter, M. Rabiller, H.B. Rode, D. Rauh
A new screening assay for allosteric inhibitors of cSrc.
Nat Chem Biol, 2009, 5(6):394-6
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Wetzel S., K. Klein, S. Renner, D. Rauh, T. Oprea, P. Mutzel, H. Waldmann
Interactive Exploration of Chemical Space with Scaffold Hunter.
Nat Chem Biol, 2009, 5(8):581-3
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Getlik, M., C. Grütter, J. Simard, S. Klüter, M. Rabiller, H.B. Rode, A. Robubi, D. Rauh
Hybrid Compound Design To Overcome the Gatekeeper T338M Mutation in cSrc.
J Med Chem, 2009, 52(13):3915-26
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Simard, J.R., M. Getlik, C. Grütter, V. Pawar, S. Wulfert, M. Rabiller, D. Rauh
Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors.
J Am Chem Soc, 2009, 131(37):13286-96
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Vintonyak, V.V., A.P. Antonchick, D. Rauh, H. Waldmann
The Therapeutic Potential of Phosphatase Inhibitors.
Curr Opin Chem Biol, 2009, 13(3):272-83
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Simard, J.R., D. Rauh
Chemical and Structural Biology to Direct the Repurposing of Sulindac.
ChemMedChem, 2009, 4(11):1793-5
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Simard, J.R., C. Grütter, V. Pawar, B. Aust, A. Wolf, M. Rabiller, S. Wulfert, S. Klüter, C. Ottmann, D. Rauh
High-throughput screening to identify inhibitors which stabilize inactive kinase conformations in p38α.
J Am Chem Soc, 2009, 131(51):18478-88
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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
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Sos, M., H. Rode, S. Heynck, M. Peifer, F. Fischer, S. Klüter, V. Pawar, C. Reuter, J. Heuckmann, J. Weiss, L. Ruddigkeit, M. Rabiller, M. Koker, J. Simard, M. Getlik, R. Thomas and D. Rauh
Chemogenomic Profiling Provides Insights into the Limited Activity of Irreversible EGFR Inhibitors in Tumor Cells Expressing the T790M EGFR Resistance Mutation.
Cancer Research, 2010, February 1, 70(3)
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Simard, J.R., M. Getlik, C. Grütter, D. Rauh
Fluorophore-Labeled Glycine-Rich Loop Detects Ligands Which Stabilize Inactive Kinase Conformations.
J Am Chem Soc, in press

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.
Archiv der Pharmazie, in press

Simard, J.R, D. Rauh
Screening for allosteric kinase inhibitors in high-throughput: A novel fluorescence approach for detecting DFG-out kinase inhibitors.
SCREENING -Trends in Drug Discovery, Wiley GIT, 2009. (Book chapter)

D. Rauh
Inaktive Kinasekonformationen stabilisieren.
Nachrichten aus der Chemie, Gesellschaft Deutscher Chemiker, 2010, in press

Gremer, L., De Luca, A., Merbitz-Zahradnik, T., Dallapiccola, B., Morlot, S., Tartaglia, M., Kutsche, K., Ahmadian, M.R., and Rosenberger, G.
Duplication of Glu37 in the switch I region of HRAS impairs effector/GAP binding and underlies Costello syndrome by promoting growth factor-dependent MAPK and AKT activation.
Hum Mol Genet, 2009,
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Cirstea, I.C., Kutsche, K., Dvorsky, R., Gremer, L., Carta, C., Horn, D., Roberts, A.E., Lepri, F., Merbitz-Zahradnik, T., König, R., Kratz, C.P., Pantaleoni, F., Dentici, M.L., Joshi, V.A., Kucherlapati, R.S., Mazzanti, L., Mundlos, S., Patton, M., Cirillo Silengo, M., Rossi, C., Zampino, G., Digilio, C., Stuppia, L., Pennacchio, L.A., Gelb, B.D., Dallapiccola, B., Wittinghofer, A., Ahmadian, M.R., Tartaglia, M. and Zenker, M.
A restricted spectrum of NRAS mutations causes Noonan syndrome.
Nature Genetics, 2010, Jan;42(1):27-9
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Patent applications:

Simard J.R., Getlik M., D. Rauh
Development of fluorescently P-loop labeled kinases for screening of inhibitors.
Submitted to EPO and USPTO, July 24th, 2008, PCT filed July 2009.

Simard J.R., D. Rauh
Fluorescently or spin-labeled kinases for rapid screening and identification of novel kinase inhibitor scaffolds.
Submitted to EPO and USPTO, April 17th, 2009.

Database entries:

Group D. Rauh:

3HV6: human p38α MAP Kinase (2009)
3HV7: human p38α MAP Kinase (2009)
3HUB: human p38α MAP Kinase (2009)
3HUC: human p38α MAP Kinase (2009)
3HV3: human p38α MAP Kinase (2009)
3HV4: human p38α MAP Kinase (2009)
3HV5: human p38α MAP Kinase (2009)
3GCP: human p38α MAP Kinase (2009)
3GCQ: human p38α MAP Kinase (2009)
3GCS: human p38α MAP Kinase (2009)
3GCU: human p38α MAP Kinase (2009)
3GCV: human p38α MAP Kinase (2009)
3F3T: cSrc Kinase (2009)
3F3U: cSrc Kinase (2009)
3F3V: cSrc Kinase (2009)
3F3W: cSrc Kinase (2009)
3G5D: cSrc Kinase (2009)
2QI8: cSrc Kinase (2008)
2QLQ: cSrc Kinase (2008)
2QQ7: cSrc Kinase (2008)