| Year |
Citation |
Score |
| 2023 |
Grabe T, Jeyakumar K, Niggenaber J, Schulz T, Koska S, Kleinbölting S, Beck ME, Müller MP, Rauh D. Addressing the Osimertinib Resistance Mutation EGFR-L858R/C797S with Reversible Aminopyrimidines. Acs Medicinal Chemistry Letters. 14: 591-598. PMID 37197473 DOI: 10.1021/acsmedchemlett.2c00514 |
0.313 |
|
| 2023 |
Goebel L, Kirschner T, Koska S, Rai A, Janning P, Maffini S, Vatheuer H, Czodrowski P, Goody RS, Müller MP, Rauh D. Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors. Elife. 12. PMID 36972177 DOI: 10.7554/eLife.82184 |
0.373 |
|
| 2023 |
Stehle J, Weisner J, Eichhorn L, Rauh D, Drescher M. Insights into the Conformational Plasticity of the Protein Kinase Akt1 by Multi-Lateral Dipolar Spectroscopy. Chemistry (Weinheim An Der Bergstrasse, Germany). e202203959. PMID 36795969 DOI: 10.1002/chem.202203959 |
0.37 |
|
| 2022 |
Gehrtz P, Marom S, Bührmann M, Hardick J, Kleinbölting S, Shraga A, Dubiella C, Gabizon R, Wiese JN, Müller MP, Cohen G, Babaev I, Shurrush K, Avram L, Resnick E, ... ... Rauh D, et al. Optimization of Covalent MKK7 Inhibitors Crude Nanomole-Scale Libraries. Journal of Medicinal Chemistry. PMID 35912476 DOI: 10.1021/acs.jmedchem.1c02206 |
0.306 |
|
| 2022 |
Lategahn J, Tumbrink HL, Schultz-Fademrecht C, Heimsoeth A, Werr L, Niggenaber J, Keul M, Parmaksiz F, Baumann M, Menninger S, Zent E, Landel I, Weisner J, Jeyakumar K, Heyden L, ... ... Rauh D, et al. Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors. Journal of Medicinal Chemistry. PMID 35486541 DOI: 10.1021/acs.jmedchem.1c02080 |
0.685 |
|
| 2022 |
van der Westhuizen L, Weisner J, Taher A, Landel I, Quambusch L, Lindemann M, Uhlenbrock N, Müller MP, Green IR, Pelly SC, Rauh D, van Otterlo WAL. Covalent allosteric inhibitors of Akt generated using a click fragment approach. Chemmedchem. PMID 35170857 DOI: 10.1002/cmdc.202100776 |
0.829 |
|
| 2021 |
Quambusch L, Depta L, Landel I, Lubeck M, Kirschner T, Nabert J, Uhlenbrock N, Weisner J, Kostka M, Levy LM, Schultz-Fademrecht C, Glanemann F, Althoff K, Müller MP, Siveke JT, ... Rauh D, et al. Cellular model system to dissect the isoform-selectivity of Akt inhibitors. Nature Communications. 12: 5297. PMID 34489430 DOI: 10.1038/s41467-021-25512-8 |
0.816 |
|
| 2020 |
Niggenaber J, Heyden L, Grabe T, Müller MP, Lategahn J, Rauh D. Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands. Acs Medicinal Chemistry Letters. 11: 2484-2490. PMID 33335671 DOI: 10.1021/acsmedchemlett.0c00472 |
0.401 |
|
| 2020 |
Lategahn J, Hardick J, Grabe T, Niggenaber J, Jeyakumar K, Keul M, Tumbrink HL, Becker C, Hodson L, Kirschner T, Klövekorn P, Ketzer J, Baumann M, Terheyden S, Unger A, ... ... Rauh D, et al. Targeting Her2-insYVMA with Covalent Inhibitors - A Focused Compound Screening and Structure-Based Design Approach. Journal of Medicinal Chemistry. PMID 32931277 DOI: 10.1021/Acs.Jmedchem.0C00870 |
0.503 |
|
| 2020 |
Roser P, Weisner J, Stehle J, Rauh D, Drescher M. Conformational selection vs. induced fit: insights into the binding mechanisms of p38α MAP Kinase inhibitors. Chemical Communications (Cambridge, England). 56: 8818-8821. PMID 32749403 DOI: 10.1039/D0Cc02539A |
0.424 |
|
| 2020 |
Volz C, Breid S, Selenz C, Zaplatina A, Golfmann K, Meder L, Dietlein F, Borchmann S, Chatterjee S, Siobal M, Schöttle J, Florin A, Koker M, Nill M, Ozretić L, ... ... Rauh D, et al. Inhibition of Tumor VEGFR2 Induces Serine 897 EphA2-Dependent Tumor Cell Invasion and Metastasis in NSCLC. Cell Reports. 31: 107568. PMID 32348765 DOI: 10.1016/J.Celrep.2020.107568 |
0.396 |
|
| 2020 |
Landel I, Quambusch L, Depta L, Rauh D. Spotlight on AKT: Current Therapeutic Challenges. Acs Medicinal Chemistry Letters. 11: 225-227. PMID 32184947 DOI: 10.1021/Acsmedchemlett.9B00548 |
0.798 |
|
| 2020 |
Khosroyani H, Klug LR, Town A, Lategahn J, Falkenhorst J, Grunewald S, Mühlenberg T, Ehrt C, Wardelmann E, Hartmann W, Schildhaus H, Jung S, Czodrowski P, Agaimy A, Rutkowski P, ... Rauh D, et al. Abstract 3005: Comprehensive profile of platelet derived growth factor receptor alpha (PDGFRA) mutations in gastrointestinal stromal tumors Cancer Research. 80: 3005-3005. DOI: 10.1158/1538-7445.Am2020-3005 |
0.466 |
|
| 2019 |
Fassunke J, Heydt C, Michels S, Van Veggel B, Müller F, Keul M, Dammert MA, Schmitt A, Smit EF, Kast S, Wolf J, Buettner R, Sos ML, Rauh D, Merkelbach-Bruse S. New insights into acquired resistance mechanisms to third-generation EGFR tyrosine kinase inhibitor therapy in lung cancer. Annals of Oncology : Official Journal of the European Society For Medical Oncology. 30: ii51. PMID 32131274 DOI: 10.1093/Annonc/Mdz063.030 |
0.708 |
|
| 2019 |
Lategahn J, Keul M, Klövekorn P, Tumbrink HL, Niggenaber J, Müller MP, Hodson L, Flaßhoff M, Hardick J, Grabe T, Engel J, Schultz-Fademrecht C, Baumann M, Ketzer J, Mühlenberg T, ... ... Rauh D, et al. Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S. Chemical Science. 10: 10789-10801. PMID 31857889 DOI: 10.1039/C9Sc03445E |
0.459 |
|
| 2019 |
Quambusch L, Landel I, Depta L, Weisner J, Uhlenbrock N, Müller MP, Glanemann F, Althoff K, Siveke JT, Rauh D. Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity. Angewandte Chemie (International Ed. in English). PMID 31584233 DOI: 10.1002/Anie.201909857 |
0.821 |
|
| 2019 |
Niggenaber J, Hardick J, Lategahn J, Rauh D. Structure Defines Function - Clinically Relevant Mutations in ErbB Kinases. Journal of Medicinal Chemistry. PMID 31414802 DOI: 10.1021/Acs.Jmedchem.9B00964 |
0.498 |
|
| 2019 |
Goody RS, Müller MP, Rauh D. Mutant-Specific Targeting of Ras G12C Activity by Covalently Reacting Small Molecules. Cell Chemical Biology. PMID 31378709 DOI: 10.1016/J.Chembiol.2019.07.005 |
0.359 |
|
| 2019 |
Wolle P, Engel J, Smith S, Goebel L, Hennes E, Lategahn J, Rauh D. Characterization of Covalent Pyrazolopyrimidine-MKK7 Complexes and Report on a Unique DFG-in/Leu-in Conformation of the Mitogen Activated Protein Kinase Kinase 7 (MKK7). Journal of Medicinal Chemistry. PMID 31083997 DOI: 10.1021/acs.jmedchem.9b00472 |
0.413 |
|
| 2019 |
Uhlenbrock N, Smith S, Weisner J, Landel I, Lindemann M, Le TA, Hardick J, Gontla R, Scheinpflug R, Czodrowski P, Janning P, Depta L, Quambusch L, Müller MP, Engels B, ... Rauh D, et al. Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt. Chemical Science. 10: 3573-3585. PMID 30996949 DOI: 10.1039/C8Sc05212C |
0.822 |
|
| 2019 |
Schehr M, Ianes C, Weisner J, Heintze L, Müller MP, Pichlo C, Charl J, Brunstein E, Ewert J, Lehr M, Baumann U, Rauh D, Knippschild U, Peifer C, Herges R. 2-Azo-, 2-diazocine-thiazols and 2-azo-imidazoles as photoswitchable kinase inhibitors: limitations and pitfalls of the photoswitchable inhibitor approach. Photochemical & Photobiological Sciences : Official Journal of the European Photochemistry Association and the European Society For Photobiology. PMID 30924488 DOI: 10.2210/Pdb6Hwt/Pdb |
0.494 |
|
| 2019 |
Weisner J, Landel I, Reintjes C, Uhlenbrock N, Trajkovic-Arsic M, Dienstbier N, Hardick J, Ladigan S, Lindemann M, Smith S, Quambusch L, Scheinpflug R, Depta L, Gontla R, Unger A, ... ... Rauh D, et al. Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in KRAS-mutant Pancreatic and Colorectal Cancer. Cancer Research. PMID 30858154 DOI: 10.1158/0008-5472.Can-18-2861 |
0.808 |
|
| 2019 |
Bartolini D, Bührmann M, Barreca ML, Manfroni G, Cecchetti V, Rauh D, Galli F. Co-crystal structure determination and cellular evaluation of 1,4-dihydropyrazolo[4,3-c] [1,2] benzothiazine 5,5-dioxide p38α MAPK inhibitors. Biochemical and Biophysical Research Communications. PMID 30824186 DOI: 10.1016/J.Bbrc.2019.02.063 |
0.493 |
|
| 2019 |
Wolle P, Hardick J, Cronin SJF, Engel J, Baumann M, Lategahn J, Penninger JM, Rauh D. Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. Journal of Medicinal Chemistry. PMID 30768270 DOI: 10.2210/Pdb6Ib2/Pdb |
0.482 |
|
| 2019 |
do Amaral DN, Lategahn J, Fokoue HH, da Silva EMB, Sant'Anna CMR, Rauh D, Barreiro EJ, Laufer S, Lima LM. A novel scaffold for EGFR inhibition: Introducing N-(3-(3-phenylureido)quinoxalin-6-yl) acrylamide derivatives. Scientific Reports. 9: 14. PMID 30626888 DOI: 10.1038/S41598-018-36846-7 |
0.446 |
|
| 2019 |
Wolle P, Engel J, Smith S, Goebel L, Hennes E, Lategahn J, Rauh D. Characterization of Covalent Pyrazolopyrimidine–MKK7 Complexes and a Report on a Unique DFG-in/Leu-in Conformation of Mitogen-Activated Protein Kinase Kinase 7 (MKK7) Journal of Medicinal Chemistry. 62: 5541-5546. DOI: 10.2210/Pdb6Qfl/Pdb |
0.499 |
|
| 2019 |
Sos ML, Tumbrink HL, Schultz-Fademrecht C, Lategahn J, Keul M, Niggenaber J, Heimsoeth A, Baumann M, Werr LH, Degenhart C, Menninger S, Heuckmann JM, Thomas RK, Rauh D, Klebl B. Targeting EGFR Ex20 mutant lung cancer with the wild type sparing kinase inhibitor PRB001. Journal of Clinical Oncology. 37: e14718-e14718. DOI: 10.1200/Jco.2019.37.15_Suppl.E14718 |
0.732 |
|
| 2018 |
Fassunke J, Müller F, Keul M, Michels S, Dammert MA, Schmitt A, Plenker D, Lategahn J, Heydt C, Brägelmann J, Tumbrink HL, Alber Y, Klein S, Heimsoeth A, Dahmen I, ... ... Rauh D, et al. Overcoming EGFR-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors. Nature Communications. 9: 4655. PMID 30405134 DOI: 10.1038/S41467-018-07078-0 |
0.713 |
|
| 2018 |
Roser P, Weisner J, Simard JR, Rauh D, Drescher M. Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α. Chemical Communications (Cambridge, England). PMID 30295691 DOI: 10.1039/C8Cc06128A |
0.443 |
|
| 2018 |
Wiedemann B, Weisner J, Rauh D. Chemical modulation of transcription factors. Medchemcomm. 9: 1249-1272. PMID 30151079 DOI: 10.1039/C8Md00273H |
0.345 |
|
| 2018 |
Grabe T, Lategahn J, Rauh D. C797S Resistance: The Undruggable EGFR Mutation in Non-Small Cell Lung Cancer? Acs Medicinal Chemistry Letters. 9: 779-782. PMID 30128066 DOI: 10.1021/Acsmedchemlett.8B00314 |
0.419 |
|
| 2018 |
Wolle P, Weisner J, Keul M, Landel I, Lategahn J, Rauh D. RASPELD to Perform High-End Screening in an Academic Environment Toward the Development of Cancer Therapeutics. Chemmedchem. PMID 30079978 DOI: 10.1002/Cmdc.201800477 |
0.336 |
|
| 2018 |
Tesch R, Becker C, Müller MP, Beck ME, Quambusch L, Getlik M, Lategahn J, Uhlenbrock N, Costa FN, Polêto MD, de Sena Murteira Pinheiro P, Rodrigues DA, Sant'Anna CM, Ferreira FF, Verli H, ... ... Rauh D, et al. An Unusual Intramolecular Halogen Bond guides Conformational Selection. Angewandte Chemie (International Ed. in English). PMID 29873877 DOI: 10.1002/Anie.201804917 |
0.799 |
|
| 2018 |
Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, ... ... Rauh D, et al. Donated chemical probes for open science. Elife. 7. PMID 29676732 DOI: 10.7554/Elife.34311 |
0.302 |
|
| 2018 |
Lategahn J, Keul M, Rauh D. Lektion gelernt? Die molekularen Grundlagen von Kinase-gerichteten Therapien und Wirkstoffresistenz im nicht-kleinzelligen Lungenkrebs Angewandte Chemie. 130: 2329-2335. DOI: 10.1002/Ange.201710398 |
0.406 |
|
| 2017 |
Smith S, Keul M, Engel J, Basu D, Eppmann S, Rauh D. Characterization of Covalent-Reversible EGFR Inhibitors. Acs Omega. 2: 1563-1575. PMID 29963651 DOI: 10.1021/acsomega.7b00157 |
0.385 |
|
| 2017 |
Lategahn J, Keul M, Rauh D. Lessons to be Learned: The Molecular Basis of Kinase-Targeted Therapies and Drug Resistance in Non-Small Cell Lung Cancer. Angewandte Chemie (International Ed. in English). PMID 29178586 DOI: 10.1002/Anie.201710398 |
0.417 |
|
| 2017 |
Kaitsiotou H, Keul M, Hardick J, Mühlenberg T, Ketzer J, Ehrt C, Krüll J, Medda F, Koch O, Giordanetto F, Bauer S, Rauh D. Inhibitors to overcome secondary mutations in the stem cell factor receptor KIT. Journal of Medicinal Chemistry. PMID 28991465 DOI: 10.1021/Acs.Jmedchem.7B00841 |
0.461 |
|
| 2017 |
Brägelmann J, Dammert MA, Dietlein F, Heuckmann JM, Choidas A, Böhm S, Richters A, Basu D, Tischler V, Lorenz C, Habenberger P, Fang Z, Ortiz-Cuaran S, Leenders F, Eickhoff J, ... ... Rauh D, et al. Systematic Kinase Inhibitor Profiling Identifies CDK9 as a Synthetic Lethal Target in NUT Midline Carcinoma. Cell Reports. 20: 2833-2845. PMID 28930680 DOI: 10.1016/J.Celrep.2017.08.082 |
0.717 |
|
| 2017 |
Bührmann M, Wiedemann BM, Müller MP, Hardick J, Ecke M, Rauh D. Structure-based design, synthesis and crystallization of 2-arylquinazolines as lipid pocket ligands of p38α MAPK. Plos One. 12: e0184627. PMID 28892510 DOI: 10.1371/Journal.Pone.0184627 |
0.473 |
|
| 2017 |
Engel J, Smith S, Lategahn J, Tumbrink HL, Goebel L, Becker C, Hennes E, Keul M, Unger A, Müller H, Baumann M, Schultz-Fademrecht C, Günther G, Hengstler JG, Rauh D. Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. Journal of Medicinal Chemistry. PMID 28853575 DOI: 10.1021/Acs.Jmedchem.7B00515 |
0.481 |
|
| 2017 |
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 I½ p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency and Prolonged Target Residence Time by Interfering with the R Spine. Journal of Medicinal Chemistry. PMID 28834431 DOI: 10.1021/Acs.Jmedchem.7B00745 |
0.458 |
|
| 2017 |
Rauh D, Bührmann M, Hardick J, Weisner J, Quambusch L. Covalent Lipid Pocket Ligands Targeting p38α MAPK Mutants. Angewandte Chemie (International Ed. in English). PMID 28834017 DOI: 10.1002/Anie.201706345 |
0.78 |
|
| 2017 |
Günther M, Lategahn J, Juchum M, Doering E, Keul M, Engel J, Tumbrink HL, Rauh D, Laufer SA. Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. Journal of Medicinal Chemistry. PMID 28603991 DOI: 10.1021/Acs.Jmedchem.7B00316 |
0.483 |
|
| 2017 |
Waldmann H, Robke L, Laraia L, Carnero Corrales MA, Konstantinidis G, Muroi M, Richters A, Winzker M, Engbring T, Tomassi S, Watanabe N, Osada H, Rauh D, Wu Y, Engel J. Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34. Angewandte Chemie (International Ed. in English). PMID 28544137 DOI: 10.1002/Anie.201703738 |
0.432 |
|
| 2017 |
Wentsch HK, Walter NM, Bührmann M, Mayer-Wrangowski S, Rauh D, Zaman GJ, 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. Angewandte Chemie (International Ed. in English). PMID 28397331 DOI: 10.1002/Anie.201701185 |
0.459 |
|
| 2017 |
Halekotte J, Witt L, Ianes C, Krüger M, Bührmann M, Rauh D, Pichlo C, Brunstein E, Luxenburger A, Baumann U, Knippschild U, Bischof J, Peifer C. Optimized 4,5-Diarylimidazoles as Potent/Selective Inhibitors of Protein Kinase CK1δ and Their Structural Relation to p38α MAPK. Molecules (Basel, Switzerland). 22. PMID 28338621 DOI: 10.3390/Molecules22040522 |
0.427 |
|
| 2017 |
Tomassi S, Lategahn J, Engel J, Keul M, Tumbrink HL, Ketzer J, Mühlenberg T, Baumann M, Schultz-Fademrecht C, Bauer S, Rauh D. Indazole-Based Covalent Inhibitors to Target Drug Resistant Epidermal Growth Factor Receptor. Journal of Medicinal Chemistry. PMID 28225269 DOI: 10.1021/Acs.Jmedchem.6B01626 |
0.45 |
|
| 2017 |
Bartolini D, Buhrmann M, Barreca ML, Manfroni G, Cecchetti V, Rauh D, Galli F. Functional and structural characterization of a novel class of MAP-kinase inhibitors Free Radical Biology and Medicine. 108: S65. DOI: 10.1016/J.Freeradbiomed.2017.04.224 |
0.48 |
|
| 2017 |
Bührmann M, Hardick J, Weisner J, Quambusch L, Rauh D. Kovalente Liganden zur Adressierung einer lipophilen Bindetasche in der MAPK p38α Angewandte Chemie. 129: 13415-13419. DOI: 10.1002/Ange.201706345 |
0.357 |
|
| 2017 |
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. Optimierte Bindungsdauer am Zielenzym: Typ-I1/2
-Inhibitoren der p38α-MAP-Kinase mit verbesserter Bindungskinetik durch direkte Interaktion mit der R-Spine Angewandte Chemie. 129: 5448-5453. DOI: 10.1002/Ange.201701185 |
0.374 |
|
| 2016 |
Engel J, Becker C, Lategahn J, Keul M, Ketzer J, Mühlenberg T, Kollipara L, Schultz-Fademrecht C, Zahedi RP, Bauer S, Rauh D. Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR. Angewandte Chemie (International Ed. in English). PMID 27496389 DOI: 10.1002/Anie.201605011 |
0.472 |
|
| 2016 |
Radi M, Schneider R, Fallacara AL, Botta L, Crespan E, Tintori C, Maga G, Kissova M, Calgani A, Richters A, Musumeci F, Rauh D, Schenone S. A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant. Bioorganic & Medicinal Chemistry Letters. PMID 27374241 DOI: 10.1016/J.Bmcl.2016.06.051 |
0.442 |
|
| 2016 |
Becker C, Öcal S, Nguyen HD, Phan T, Keul M, Simard JR, Rauh D. Monitoring conformational changes in the receptor tyrosine kinase EGFR. Chembiochem : a European Journal of Chemical Biology. PMID 26991964 DOI: 10.1002/Cbic.201600115 |
0.42 |
|
| 2016 |
Engel J, Lategahn J, Rauh D. Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer. Acs Medicinal Chemistry Letters. 7: 2-5. PMID 26819655 DOI: 10.1021/Acsmedchemlett.5B00475 |
0.399 |
|
| 2016 |
Braegelmann J, Habenberger P, Dietlein F, Heuckmann JM, Menninger S, Koch U, Choidas A, Rauh D, Klebl B, Sos ML, Thomas RK. Abstract 1349: Systematic deconvolution of kinase inhibitor profiles identifies synthetic lethal targets in ERBB2-mutant and BRD4-NUT rearranged cancer Cancer Research. 76: 1349-1349. DOI: 10.1158/1538-7445.Am2016-1349 |
0.486 |
|
| 2016 |
Engel J, Becker C, Lategahn J, Keul M, Ketzer J, Mühlenberg T, Kollipara L, Schultz-Fademrecht C, Zahedi RP, Bauer S, Rauh D. Inhibition wirkstoffresistenter Mutationsvarianten der Rezeptortyrosinkinase EGFR Angewandte Chemie. 128: 11069-11073. DOI: 10.1002/Ange.201605011 |
0.382 |
|
| 2015 |
Basu D, Richters A, Rauh D. Corrigendum to "Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR" [Bioorg. Med. Chem. 23, 2015, 2767-2780]. Bioorganic & Medicinal Chemistry. 23: 5075. PMID 32689707 DOI: 10.1016/J.Bmc.2015.06.001 |
0.399 |
|
| 2015 |
Schöttle J, Chatterjee S, Volz C, Siobal M, Florin A, Rokitta D, Hinze Y, Dietlein F, Plenker D, König K, Albus K, Heuckmann JM, Rauh D, Franz T, Neumaier B, et al. Intermittent high-dose treatment with erlotinib enhances therapeutic efficacy in EGFR-mutant lung cancer. Oncotarget. PMID 26540572 DOI: 10.18632/Oncotarget.6276 |
0.39 |
|
| 2015 |
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, ... ... Rauh D, et al. Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach. Journal of Medicinal Chemistry. 58: 6844-63. PMID 26275028 DOI: 10.1021/Acs.Jmedchem.5B01082 |
0.735 |
|
| 2015 |
Dietlein F, Kalb B, Jokic M, Noll EM, Strong A, Tharun L, Ozretić L, Künstlinger H, Kambartel K, Randerath WJ, Jüngst C, Schmitt A, Torgovnick A, Richters A, Rauh D, et al. A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer. Cell. 162: 146-59. PMID 26140595 DOI: 10.1016/J.Cell.2015.05.053 |
0.408 |
|
| 2015 |
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 SC, Bauer S, van Otterlo WA, Rauh D. Covalent-Allosteric Kinase Inhibitors. Angewandte Chemie (International Ed. in English). 54: 10313-6. PMID 26110718 DOI: 10.1002/Anie.201502142 |
0.508 |
|
| 2015 |
Basu D, Richters A, Rauh D. Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR. Bioorganic & Medicinal Chemistry. 23: 2767-80. PMID 25975640 DOI: 10.1016/J.Bmc.2015.04.038 |
0.478 |
|
| 2015 |
Schröder P, Förster T, Kleine S, Becker C, Richters A, Ziegler S, Rauh D, Kumar K, Waldmann H. Neuritogenic Militarinone-Inspired 4-Hydroxypyridones Target the Stress Pathway Kinase MAP4K4. Angewandte Chemie (International Ed. in English). PMID 25908259 DOI: 10.1002/Anie.201501515 |
0.48 |
|
| 2015 |
Richters A, Basu D, Engel J, Ercanoglu MS, Balke-Want H, Tesch R, Thomas RK, Rauh D. Identification and further development of potent TBK1 inhibitors. Acs Chemical Biology. 10: 289-98. PMID 25540906 DOI: 10.1021/Cb500908D |
0.443 |
|
| 2015 |
Tintori C, Fallacara AL, Radi M, Zamperini C, Dreassi E, Crespan E, Maga G, Schenone S, Musumeci F, Brullo C, Richters A, Gasparrini F, Angelucci A, Festuccia C, Delle Monache S, ... Rauh D, et al. Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma. Journal of Medicinal Chemistry. 58: 347-61. PMID 25469771 DOI: 10.1021/Jm5013159 |
0.449 |
|
| 2015 |
Fang Z, Simard JR, Plenker D, Nguyen HD, Phan T, Wolle P, Baumeister S, Rauh D. Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors. Acs Chemical Biology. 10: 279-88. PMID 24959717 DOI: 10.1021/Cb500355C |
0.494 |
|
| 2015 |
Rauh D. Special Issue Focused on Two Areas Pertinent to Chemical Biology: Post-Translational Modifications and New Frontiers on Kinases Acs Chemical Biology. 10: 1-2. DOI: 10.1021/Acschembio.5B00010 |
0.374 |
|
| 2015 |
Dietlein F, Kalb B, Jokic M, Noll EM, Strong A, Tharun L, Ozretić L, Künstlinger H, Kambartel K, Randerath WJ, Jüngst C, Schmitt A, Torgovnick A, Richters A, Rauh D, et al. Erratum: A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer (Cell (2015) 162 (146-159)) Cell. 162. DOI: 10.1016/J.Cell.2015.08.017 |
0.388 |
|
| 2015 |
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 SC, Bauer S, van Otterlo WAL, Rauh D. Kovalent-allosterische Kinase-Inhibitoren Angewandte Chemie. 127: 10452-10456. DOI: 10.1002/Ange.201502142 |
0.318 |
|
| 2014 |
Simard JR, Rauh D. FLiK: a direct-binding assay for the identification and kinetic characterization of stabilizers of inactive kinase conformations. Methods in Enzymology. 548: 147-71. PMID 25399645 DOI: 10.1016/B978-0-12-397918-6.00006-9 |
0.501 |
|
| 2014 |
Tziridis A, Rauh D, Neumann P, Kolenko P, Menzel A, Bräuer U, Ursel C, Steinmetzer P, Stürzebecher J, Schweinitz A, Steinmetzer T, Stubbs MT. Correlating structure and ligand affinity in drug discovery: a cautionary tale involving second shell residues. Biological Chemistry. 395: 891-903. PMID 25003390 DOI: 10.1515/Hsz-2014-0158 |
0.385 |
|
| 2014 |
Richters A, Nguyen HD, Phan T, Simard JR, Grütter C, Engel J, Rauh D. Identification of type II and III DDR2 inhibitors. Journal of Medicinal Chemistry. 57: 4252-62. PMID 24754677 DOI: 10.1021/Jm500167Q |
0.394 |
|
| 2014 |
Rauh D. A special thematic compilation/special issue crossover with Biochemistry, Journal of Medicinal Chemistry, and ACS Medicinal Chemistry Letters focused on kinases. Acs Chemical Biology. 9: 579-80. PMID 24650390 DOI: 10.1021/Cb500150D |
0.354 |
|
| 2014 |
Malchers F, Dietlein F, Schöttle J, Lu X, Nogova L, Albus K, Fernandez-Cuesta L, Heuckmann JM, Gautschi O, Diebold J, Plenker D, Gardizi M, Scheffler M, Bos M, Seidel D, ... ... Rauh D, et al. Cell-autonomous and non-cell-autonomous mechanisms of transformation by amplified FGFR1 in lung cancer. Cancer Discovery. 4: 246-57. PMID 24302556 DOI: 10.1158/2159-8290.Cd-13-0323 |
0.399 |
|
| 2013 |
Baur B, Storch K, Martz KE, Goettert MI, Richters A, Rauh D, Laufer SA. Metabolically stable dibenzo[ b, e ]oxepin-11(6 H)-ones as highly selective p38 MAP kinase inhibitors: Optimizing anti-cytokine activity in human whole blood Journal of Medicinal Chemistry. 56: 8561-8578. PMID 24131218 DOI: 10.1021/Jm401276H |
0.362 |
|
| 2013 |
Grütter C, Sreeramulu S, Sessa G, Rauh D. Structural characterization of the RLCK family member BSK8: a pseudokinase with an unprecedented architecture. Journal of Molecular Biology. 425: 4455-67. PMID 23911552 DOI: 10.1016/J.Jmb.2013.07.034 |
0.431 |
|
| 2013 |
Richters A, Ketzer J, Getlik M, Grütter C, Schneider R, Heuckmann JM, Heynck S, Sos ML, Gupta A, Unger A, Schultz-Fademrecht C, Thomas RK, Bauer S, Rauh D. Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. Journal of Medicinal Chemistry. 56: 5757-72. PMID 23773153 DOI: 10.1021/Jm4004076 |
0.705 |
|
| 2013 |
Schneider R, Gohla A, Simard JR, Yadav DB, Fang Z, van Otterlo WA, Rauh D. Overcoming compound fluorescence in the FLiK screening assay with red-shifted fluorophores. Journal of the American Chemical Society. 135: 8400-8. PMID 23672540 DOI: 10.1021/Ja403074J |
0.35 |
|
| 2013 |
Schneider R, Beumer C, Simard JR, Grütter C, Rauh D. Selective detection of allosteric phosphatase inhibitors. Journal of the American Chemical Society. 135: 6838-41. PMID 23611635 DOI: 10.1021/Ja4030484 |
0.515 |
|
| 2013 |
Urich R, Wishart G, Kiczun M, Richters A, Tidten-Luksch N, Rauh D, Sherborne B, Wyatt PG, Brenk R. De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments. Acs Chemical Biology. 8: 1044-52. PMID 23534475 DOI: 10.1021/Cb300729Y |
0.514 |
|
| 2013 |
Sreeramulu S, Mostizky Y, Sunitha S, Shani E, Nahum H, Salomon D, Hayun LB, Gruetter C, Rauh D, Ori N, Sessa G. BSKs are partially redundant positive regulators of brassinosteroid signaling in Arabidopsis. The Plant Journal : For Cell and Molecular Biology. 74: 905-19. PMID 23496207 DOI: 10.1111/Tpj.12175 |
0.375 |
|
| 2013 |
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 Journal of Medicinal Chemistry. 56: 241-253. PMID 23270382 DOI: 10.1021/Jm301539X |
0.471 |
|
| 2013 |
Fang Z, Grütter C, Rauh D. Strategies for the selective regulation of kinases with allosteric modulators: exploiting exclusive structural features. Acs Chemical Biology. 8: 58-70. PMID 23249378 DOI: 10.1021/Cb300663J |
0.523 |
|
| 2013 |
Over B, Wetzel S, Grütter C, Nakai Y, Renner S, Rauh D, Waldmann H. Natural-product-derived fragments for fragment-based ligand discovery. Nature Chemistry. 5: 21-8. PMID 23247173 DOI: 10.1038/Nchem.1506 |
0.368 |
|
| 2012 |
Sos ML, Dietlein F, Peifer M, Schöttle J, Balke-Want H, Müller C, Koker M, Richters A, Heynck S, Malchers F, Heuckmann JM, Seidel D, Eyers PA, Ullrich RT, Antonchick AP, ... ... Rauh D, et al. A framework for identification of actionable cancer genome dependencies in small cell lung cancer. Proceedings of the National Academy of Sciences of the United States of America. 109: 17034-9. PMID 23035247 DOI: 10.1073/Pnas.1207310109 |
0.714 |
|
| 2012 |
Peifer M, Fernández-Cuesta L, Sos ML, George J, Seidel D, Kasper LH, Plenker D, Leenders F, Sun R, Zander T, Menon R, Koker M, Dahmen I, Müller C, Di Cerbo V, ... ... Rauh D, et al. Integrative genome analyses identify key somatic driver mutations of small-cell lung cancer. Nature Genetics. 44: 1104-10. PMID 22941188 DOI: 10.1038/Ng.2396 |
0.655 |
|
| 2012 |
Heuckmann JM, Rauh D, Thomas RK. Epidermal growth factor receptor (EGFR) signaling and covalent EGFR inhibition in lung cancer. Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology. 30: 3417-20. PMID 22915655 DOI: 10.1200/Jco.2012.43.1825 |
0.398 |
|
| 2012 |
Martz KE, Dorn A, Baur B, Schattel V, Goettert MI, Mayer-Wrangowski SC, Rauh D, Laufer SA. Targeting the hinge glycine flip and the activation loop: novel approach to potent p38α inhibitors. Journal of Medicinal Chemistry. 55: 7862-74. PMID 22897496 DOI: 10.1021/Jm300951U |
0.468 |
|
| 2012 |
Getlik M, Simard JR, Termathe M, Grütter C, Rabiller M, van Otterlo WA, Rauh D. Fluorophore labeled kinase detects ligands that bind within the MAPK insert of p38α kinase. Plos One. 7: e39713. PMID 22768308 DOI: 10.1371/Journal.Pone.0039713 |
0.487 |
|
| 2012 |
Koeberle SC, Fischer S, Schollmeyer D, Schattel V, Grütter C, Rauh D, Laufer SA. Design, synthesis, and biological evaluation of novel disubstituted dibenzosuberones as highly potent and selective inhibitors of p38 mitogen activated protein kinase. Journal of Medicinal Chemistry. 55: 5868-77. PMID 22676210 DOI: 10.1021/Jm300327H |
0.472 |
|
| 2012 |
Schneider R, Becker C, Simard JR, Getlik M, Bohlke N, Janning P, Rauh D. Direct binding assay for the detection of type IV allosteric inhibitors of Abl. Journal of the American Chemical Society. 134: 9138-41. PMID 22612329 DOI: 10.1021/Ja303858W |
0.456 |
|
| 2012 |
Grütter C, Simard JR, Mayer-Wrangowski SC, Schreier PH, Pérez-MartÃn J, Richters A, Getlik M, Gutbrod O, Braun CA, Beck ME, Rauh D. Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals. Acs Chemical Biology. 7: 1257-67. PMID 22545924 DOI: 10.1021/Cb300128B |
0.504 |
|
| 2012 |
Koch A, Rode HB, Richters A, Rauh D, Hauf S. A chemical genetic approach for covalent inhibition of analogue-sensitive aurora kinase. Acs Chemical Biology. 7: 723-31. PMID 22264160 DOI: 10.1021/Cb200465C |
0.507 |
|
| 2012 |
Koeberle SC, Romir J, Fischer S, Koeberle A, Schattel V, Albrecht W, Grütter C, Werz O, Rauh D, Stehle T, Laufer SA. Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. Nature Chemical Biology. 8: 141-3. PMID 22198732 DOI: 10.1038/Nchembio.761 |
0.464 |
|
| 2012 |
Getlik M, Grütter C, Simard JR, Nguyen HD, Robubi A, Aust B, van Otterlo WA, Rauh D. Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38α. European Journal of Medicinal Chemistry. 48: 1-15. PMID 22154891 DOI: 10.1016/J.Ejmech.2011.11.019 |
0.453 |
|
| 2012 |
Simard JR, Rauh D. Fluorescence labels in kinases: a high-throughput kinase binding assay for the identification of DFG-out binding ligands. Methods in Molecular Biology (Clifton, N.J.). 800: 95-117. PMID 21964785 DOI: 10.1007/978-1-61779-349-3_8 |
0.495 |
|
| 2012 |
Weiss J, Sos ML, Seidel D, Peifer M, Zander T, Heuckmann JM, Ullrich RT, Menon R, Maier S, Soltermann A, Moch H, Wagener P, Fischer F, Heynck S, Koker M, ... ... Rauh D, et al. Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer (Science Translational Medicine (2012) 4, (130er2)) Science Translational Medicine. 4. DOI: 10.1126/Scitranslmed.3002121 |
0.321 |
|
| 2012 |
Mayer-Wrangowski S, Rauh D. Symbiose aus Chemie und Medizin — zielgerichtet gegen Krebs Biospektrum. 18: 376-379. DOI: 10.1007/S12268-012-0195-7 |
0.373 |
|
| 2011 |
Hammerman PS, Sos ML, Ramos AH, Xu C, Dutt A, Zhou W, Brace LE, Woods BA, Lin W, Zhang J, Deng X, Lim SM, Heynck S, Peifer M, Simard JR, ... ... Rauh D, et al. Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. Cancer Discovery. 1: 78-89. PMID 22328973 DOI: 10.1158/2159-8274.Cd-11-0005 |
0.699 |
|
| 2011 |
Heuckmann JM, Hölzel M, Sos ML, Heynck S, Balke-Want H, Koker M, Peifer M, Weiss J, Lovly CM, Grütter C, Rauh D, Pao W, Thomas RK. ALK mutations conferring differential resistance to structurally diverse ALK inhibitors. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 17: 7394-401. PMID 21948233 DOI: 10.1158/1078-0432.Ccr-11-1648 |
0.693 |
|
| 2011 |
Tückmantel S, Greul JN, Janning P, Brockmeyer A, Grütter C, Simard JR, Gutbrod O, Beck ME, Tietjen K, Rauh D, Schreier PH. Identification of Ustilago maydis Aurora kinase as a novel antifungal target. Acs Chemical Biology. 6: 926-33. PMID 21671622 DOI: 10.1021/Cb200112Y |
0.492 |
|
| 2011 |
Vintonyak VV, Waldmann H, Rauh D. Using small molecules to target protein phosphatases. Bioorganic & Medicinal Chemistry. 19: 2145-55. PMID 21420867 DOI: 10.1016/J.Bmc.2011.02.047 |
0.455 |
|
| 2011 |
Rode HB, Sos ML, Grütter C, Heynck S, Simard JR, Rauh D. Synthesis and biological evaluation of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase and epidermal growth factor receptor. Bioorganic & Medicinal Chemistry. 19: 429-39. PMID 21130659 DOI: 10.1016/J.Bmc.2010.11.007 |
0.7 |
|
| 2011 |
Weiss J, Sos ML, Seidel D, Peifer M, Zander T, Heuckmann JM, Ullrich RT, Menon R, Maier S, Soltermann A, Moch H, Wagener P, Fischer F, Heynck S, Koker M, ... ... Rauh D, et al. Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer (Science Translational Medicine (2011) 3) Science Translational Medicine. 3. DOI: 10.1126/scitranslmed.3002121 |
0.614 |
|
| 2011 |
Vintonyak VV, Warburg K, Over B, Hübel K, Rauh D, Waldmann H. 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. 67: 6713-6729. DOI: 10.1016/J.Tet.2011.04.026 |
0.402 |
|
| 2010 |
Weiss J, Sos ML, Seidel D, Peifer M, Zander T, Heuckmann JM, Ullrich RT, Menon R, Maier S, Soltermann A, Moch H, Wagener P, Fischer F, Heynck S, Koker M, ... ... Rauh D, et al. Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer. Science Translational Medicine. 2: 62ra93. PMID 21160078 DOI: 10.1126/Scitranslmed.3001451 |
0.681 |
|
| 2010 |
Klüter S, Simard JR, Rode HB, Grütter C, Pawar V, Raaijmakers HC, Barf TA, Rabiller M, van Otterlo WA, Rauh D. Characterization of irreversible kinase inhibitors by directly detecting covalent bond formation: a tool for dissecting kinase drug resistance. Chembiochem : a European Journal of Chemical Biology. 11: 2557-66. PMID 21080395 DOI: 10.1002/Cbic.201000352 |
0.497 |
|
| 2010 |
Antonchick AP, Gerding-Reimers C, Catarinella M, Schürmann M, Preut H, Ziegler S, Rauh D, Waldmann H. Highly enantioselective synthesis and cellular evaluation of spirooxindoles inspired by natural products. Nature Chemistry. 2: 735-40. PMID 20729892 DOI: 10.1038/Nchem.730 |
0.316 |
|
| 2010 |
Robubi A, Waldmann H, Rauh D. RAF kinase inhibitors in cancer treatment: like a bull in a China shop? Chembiochem : a European Journal of Chemical Biology. 11: 1645-8. PMID 20648512 DOI: 10.1002/Cbic.201000348 |
0.446 |
|
| 2010 |
Vintonyak VV, Warburg K, Kruse H, Grimme S, Hübel K, Rauh D, Waldmann H. Identification of thiazolidinones spiro-fused to indolin-2-ones as potent and selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase B. Angewandte Chemie (International Ed. in English). 49: 5902-5. PMID 20632348 DOI: 10.1002/Anie.201002138 |
0.384 |
|
| 2010 |
Dekker FJ, Rocks O, Vartak N, Menninger S, Hedberg C, Balamurugan R, Wetzel S, Renner S, Gerauer M, Schölermann B, Rusch M, Kramer JW, Rauh D, Coates GW, Brunsveld L, et al. Small-molecule inhibition of APT1 affects Ras localization and signaling. Nature Chemical Biology. 6: 449-56. PMID 20418879 DOI: 10.1038/Nchembio.362 |
0.351 |
|
| 2010 |
Rabiller M, Getlik M, Klüter S, Richters A, Tückmantel S, Simard JR, Rauh D. Proteus in the world of proteins: conformational changes in protein kinases. Archiv Der Pharmazie. 343: 193-206. PMID 20336692 DOI: 10.1002/Ardp.201000028 |
0.461 |
|
| 2010 |
Pawar VG, Sos ML, Rode HB, Rabiller M, Heynck S, van Otterlo WA, Thomas RK, Rauh D. Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. Journal of Medicinal Chemistry. 53: 2892-901. PMID 20222733 DOI: 10.1021/Jm901877J |
0.728 |
|
| 2010 |
Simard JR, Getlik M, Grütter C, Schneider R, Wulfert S, Rauh D. Fluorophore labeling of the glycine-rich loop as a method of identifying inhibitors that bind to active and inactive kinase conformations. Journal of the American Chemical Society. 132: 4152-60. PMID 20201574 DOI: 10.1021/Ja908083E |
0.503 |
|
| 2010 |
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. 5: e8919. PMID 20111714 DOI: 10.1371/Journal.Pone.0008919 |
0.672 |
|
| 2010 |
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, ... ... Rauh D, et al. Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation. Cancer Research. 70: 868-74. PMID 20103621 DOI: 10.1158/0008-5472.Can-09-3106 |
0.724 |
|
| 2010 |
Klüter S, Grütter C, Naqvi T, Rabiller M, Simard JR, Pawar V, Getlik M, Rauh D. Displacement assay for the detection of stabilizers of inactive kinase conformations. Journal of Medicinal Chemistry. 53: 357-67. PMID 19928858 DOI: 10.1021/Jm901297E |
0.509 |
|
| 2010 |
Klüter S, Simard JR, Rode HB, Grütter C, Pawar V, Raaijmakers HCA, Barf TA, Rabiller M, van Otterlo WAL, Rauh D. Inside Cover: Characterization of Irreversible Kinase Inhibitors by Directly Detecting Covalent Bond Formation: A Tool for Dissecting Kinase Drug Resistance (ChemBioChem 18/2010) Chembiochem. 11: 2474-2474. DOI: 10.1002/Cbic.201090088 |
0.429 |
|
| 2009 |
Simard JR, Grütter C, Pawar V, Aust B, Wolf A, Rabiller M, Wulfert S, Robubi A, Klüter S, Ottmann C, Rauh D. High-throughput screening to identify inhibitors which stabilize inactive kinase conformations in p38alpha. Journal of the American Chemical Society. 131: 18478-88. PMID 19950957 DOI: 10.1021/ja907795q |
0.407 |
|
| 2009 |
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, ... ... Rauh D, et al. Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer. Proceedings of the National Academy of Sciences of the United States of America. 106: 18351-6. PMID 19805051 DOI: 10.1073/Pnas.0907325106 |
0.735 |
|
| 2009 |
Simard JR, Getlik M, Grütter C, Pawar V, Wulfert S, Rabiller M, Rauh D. Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors. Journal of the American Chemical Society. 131: 13286-96. PMID 19572644 DOI: 10.1021/Ja902010P |
0.501 |
|
| 2009 |
Wetzel S, Klein K, Renner S, Rauh D, Oprea TI, Mutzel P, Waldmann H. Interactive exploration of chemical space with Scaffold Hunter. Nature Chemical Biology. 5: 581-3. PMID 19561620 DOI: 10.1038/Nchembio.187 |
0.347 |
|
| 2009 |
Renner S, Van Otterlo WAL, Dominguez Seoane M, Möcklinghoff S, Hofmann B, Wetzel S, Schuffenhauer A, Ertl P, Oprea TI, Steinhilber D, Brunsveld L, Rauh D, Waldmann H. Bioactivity-guided mapping and navigation of chemical space Nature Chemical Biology. 5: 585-592. PMID 19561619 DOI: 10.1038/Nchembio.188 |
0.328 |
|
| 2009 |
Getlik M, Grütter C, Simard JR, Klüter S, Rabiller M, Rode HB, Robubi A, Rauh D. Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. Journal of Medicinal Chemistry. 52: 3915-26. PMID 19462975 DOI: 10.1021/Jm9002928 |
0.511 |
|
| 2009 |
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, et al. Predicting drug susceptibility of non-small cell lung cancers based on genetic lesions. The Journal of Clinical Investigation. 119: 1727-40. PMID 19451690 DOI: 10.1172/Jci37127 |
0.697 |
|
| 2009 |
Vintonyak VV, Antonchick AP, Rauh D, Waldmann H. The therapeutic potential of phosphatase inhibitors Current Opinion in Chemical Biology. 13: 272-283. PMID 19410499 DOI: 10.1016/J.Cbpa.2009.03.021 |
0.417 |
|
| 2009 |
Simard JR, Klüter S, Grütter C, Getlik M, Rabiller M, Rode HB, Rauh D. A new screening assay for allosteric inhibitors of cSrc. Nature Chemical Biology. 5: 394-6. PMID 19396179 DOI: 10.1038/Nchembio.162 |
0.497 |
|
| 2009 |
Triola G, Wetzel S, Ellinger B, Koch MA, Hübel K, Rauh D, Waldmann H. ATP competitive inhibitors of d-alanine-d-alanine ligase based on protein kinase inhibitor scaffolds Bioorganic and Medicinal Chemistry. 17: 1079-1087. PMID 18321716 DOI: 10.1016/J.Bmc.2008.02.046 |
0.46 |
|
| 2009 |
Simard JR, Getlik M, Klüter S, Grütter C, Rabiller M, Wulfert S, Ruddigkeit L, Pawar V, Rode HB, Rauh D. Fluorescent-tagged Kinases: A New Assay System For Detecting And Screening For Allosteric Kinase Inhibitors Biophysical Journal. 96: 597a-598a. DOI: 10.1016/J.Bpj.2008.12.3127 |
0.512 |
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| 2008 |
Bateman RL, Rauh D, Tavshanjian B, Shokat KM. Human carbonyl reductase 1 is an S-nitrosoglutathione reductase. The Journal of Biological Chemistry. 283: 35756-62. PMID 18826943 DOI: 10.1074/Jbc.M807125200 |
0.738 |
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| 2008 |
Michalczyk A, Klüter S, Rode HB, Simard JR, Grütter C, Rabiller M, Rauh D. Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. Bioorganic & Medicinal Chemistry. 16: 3482-8. PMID 18316192 DOI: 10.1016/J.Bmc.2008.02.053 |
0.445 |
|
| 2007 |
Bateman R, Rauh D, Shokat KM. Glutathione traps formaldehyde by formation of a bicyclo[4.4.1]undecane adduct. Organic & Biomolecular Chemistry. 5: 3363-7. PMID 17912391 DOI: 10.1039/B707602A |
0.762 |
|
| 2007 |
Blair JA, Rauh D, Kung C, Yun CH, Fan QW, Rode H, Zhang C, Eck MJ, Weiss WA, Shokat KM. Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. Nature Chemical Biology. 3: 229-38. PMID 17334377 DOI: 10.1038/Nchembio866 |
0.832 |
|
| 2007 |
Rauh D, Blair J, Shokat K. Structure guided Development of Functional Probes for Protein Kinases using Chemical Genetics Gbm Fall Meeting Hamburg 2007. 2007. DOI: 10.1240/sav_gbm_2007_h_002053 |
0.494 |
|
| 2006 |
Simon MD, Feldman ME, Rauh D, Maris AE, Wemmer DE, Shokat KM. Structure and properties of a re-engineered homeodomain protein-DNA interface. Acs Chemical Biology. 1: 755-60. PMID 17240973 DOI: 10.1021/Cb6003756 |
0.757 |
|
| 2006 |
Wei W, Bateman R, Rauh D, Li B, Shokat KM, Liu L. P0119. Pharmacological inhibitors of S-nitroso-glutathione reductase Nitric Oxide. 14: 55-56. DOI: 10.1016/J.Niox.2006.04.185 |
0.77 |
|
| 2006 |
Bateman R, Rauh D, Shokat K. Progress Toward the Development of Inhibitors of 11beta-Hydroxysteroid dehydrogenase 2: Inhibition of Cortisol Catabolism in the Lung Journal of Allergy and Clinical Immunology. 117: S91. DOI: 10.1016/J.Jaci.2005.12.363 |
0.449 |
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| 2005 |
Tanaka M, Bateman R, Rauh D, Vaisberg E, Ramachandani S, Zhang C, Hansen KC, Burlingame AL, Trautman JK, Shokat KM, Adams CL. An unbiased cell morphology-based screen for new, biologically active small molecules. Plos Biology. 3: e128. PMID 15799708 DOI: 10.1371/Journal.Pbio.0030128 |
0.824 |
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| 2004 |
Rauh D, Klebe G, Stubbs MT. Understanding protein-ligand interactions: the price of protein flexibility. Journal of Molecular Biology. 335: 1325-41. PMID 14729347 DOI: 10.1016/J.Jmb.2003.11.041 |
0.394 |
|
| 2004 |
Di Fenza A, Heine A, Vogler M, Stubbs MT, Rauh D, Tziridis A, Koert U, Klebe G. Structural studies of FXa-trypsin mutants complexed by dianhydrosugar-based benzamidine inhibitors Acta Crystallographica Section a Foundations of Crystallography. 60: s163-s163. DOI: 10.1107/S0108767304096771 |
0.389 |
|
| 2003 |
Radau G, Gebel J, Rauh D. New cyanopeptide-derived low molecular weight thrombin inhibitors. Archiv Der Pharmazie. 336: 372-80. PMID 14502757 DOI: 10.1002/Ardp.200300726 |
0.391 |
|
| 2003 |
Rauh D, Klebe G, Stürzebecher J, Stubbs MT. ZZ made EZ: influence of inhibitor configuration on enzyme selectivity. Journal of Molecular Biology. 330: 761-70. PMID 12850145 DOI: 10.1016/S0022-2836(03)00617-X |
0.322 |
|
| 2002 |
Rauh D, Reyda S, Klebe G, Stubbs MT. Trypsin mutants for structure-based drug design: expression, refolding and crystallisation. Biological Chemistry. 383: 1309-14. PMID 12437122 DOI: 10.1515/Bc.2002.148 |
0.328 |
|
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