Daniel Rauh

Daniel Rauh

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Daniel Rauh

Daniel Rauh

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Mutant-Specific Targeting of Ras G12C Activity by Covalently Reacting Small Molecules.

Cell Chem Biol 2019 Oct 1;26(10):1338-1348. Epub 2019 Aug 1.

Faculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227 Dortmund, Germany; Drug Discovery Hub Dortmund (DDHD) am Zentrum für integrierte Wirkstoffforschung (ZIW), Otto-Hahn-Strasse 4a, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1016/j.chembiol.2019.07.005DOI Listing
October 2019

Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity.

Angew Chem Int Ed Engl 2019 Oct 4. Epub 2019 Oct 4.

Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

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http://dx.doi.org/10.1002/anie.201909857DOI Listing
October 2019

Structure Defines Function: Clinically Relevant Mutations in ErbB Kinases.

J Med Chem 2019 Aug 28. Epub 2019 Aug 28.

Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , ( Germany ).

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http://dx.doi.org/10.1021/acs.jmedchem.9b00964DOI Listing
August 2019

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).

J Med Chem 2019 Jun 31;62(11):5541-5546. Epub 2019 May 31.

Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00472DOI Listing
June 2019

Co-crystal structure determination and cellular evaluation of 1,4-dihydropyrazolo[4,3-c] [1,2] benzothiazine 5,5-dioxide p38α MAPK inhibitors.

Biochem Biophys Res Commun 2019 Apr 27;511(3):579-586. Epub 2019 Feb 27.

University of Perugia, Department of Pharmaceutical Sciences, Italy.

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http://dx.doi.org/10.1016/j.bbrc.2019.02.063DOI Listing
April 2019

Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors.

J Med Chem 2019 Mar 21;62(5):2843-2848. Epub 2019 Feb 21.

Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00102DOI Listing
March 2019

Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.

Chem Sci 2019 Mar 13;10(12):3573-3585. Epub 2019 Feb 13.

Faculty of Chemistry and Chemical Biology , TU Dortmund University , Drug Discovery Hub Dortmund (DDHD) am Zentrum für integrierte Wirkstoffforschung (ZIW) , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; http://www.ddhdortmund.de ; www.twitter.com/DDHDortmund.

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http://dx.doi.org/10.1039/c8sc05212cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6430017PMC
March 2019

A novel scaffold for EGFR inhibition: Introducing N-(3-(3-phenylureido)quinoxalin-6-yl) acrylamide derivatives.

Sci Rep 2019 01 9;9(1):14. Epub 2019 Jan 9.

Instituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos (INCT-INOFAR; http://www.inct-inofar.ccs.ufrj.br/), Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio®, http://www.lassbio.icb.ufrj.br) Universidade Federal do Rio de Janeiro, CCS, Cidade Universitária, Rio de Janeiro, RJ, Brazil.

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http://www.nature.com/articles/s41598-018-36846-7
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http://dx.doi.org/10.1038/s41598-018-36846-7DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6327040PMC
January 2019

RASPELD to Perform High-End Screening in an Academic Environment toward the Development of Cancer Therapeutics.

ChemMedChem 2018 10 23;13(19):2065-2072. Epub 2018 Aug 23.

Faculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

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http://dx.doi.org/10.1002/cmdc.201800477DOI Listing
October 2018

Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α.

Chem Commun (Camb) 2018 Oct;54(85):12057-12060

Department of Chemistry and Konstanz Research School Chemical Biology, (KoRS-CB), University of Konstanz, Universitätsstraße 10, 78457 Konstanz, Germany.

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http://xlink.rsc.org/?DOI=C8CC06128A
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http://dx.doi.org/10.1039/c8cc06128aDOI Listing
October 2018

Insights into the Kinetics of the Resistance Formation of Bacteria against Ciprofloxacin Poly(2-methyl-2-oxazoline) Conjugates.

Bioconjug Chem 2018 08 11;29(8):2671-2678. Epub 2018 Jul 11.

Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany.

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http://dx.doi.org/10.1021/acs.bioconjchem.8b00361DOI Listing
August 2018

C797S Resistance: The Undruggable EGFR Mutation in Non-Small Cell Lung Cancer?

ACS Med Chem Lett 2018 Aug 23;9(8):779-782. Epub 2018 Jul 23.

Faculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227 Dortmund, Germany.

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http://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00314
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http://dx.doi.org/10.1021/acsmedchemlett.8b00314DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6088362PMC
August 2018

Chemical modulation of transcription factors.

Medchemcomm 2018 Aug 11;9(8):1249-1272. Epub 2018 Jul 11.

Technische Universität Dortmund , Fakultät für Chemie und Chemische Biologie , Otto-Hahn-Strasse 4a , D-44227 Dortmund , Germany . Email: ; ; Tel: +49 (0)231 755 7080.

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http://dx.doi.org/10.1039/c8md00273hDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6097187PMC
August 2018

Augmented Reality in Scientific Publications-Taking the Visualization of 3D Structures to the Next Level.

ACS Chem Biol 2018 03;13(3):496-499

Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , D-44227 Dortmund , Germany.

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http://dx.doi.org/10.1021/acschembio.8b00153DOI Listing
March 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 2018 02 12;57(9):2307-2313. Epub 2018 Jan 12.

Faculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

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http://dx.doi.org/10.1002/anie.201710398DOI Listing
February 2018

Try Me: Promiscuous Inhibitors Still Allow for Selective Targeted Protein Degradation.

Cell Chem Biol 2018 01;25(1):4-6

Technical University Dortmund, Faculty of Chemistry and Chemical Biology, Otto-Hahn-Straße 4a, 44227 Dortmund, Germany. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2018.01.004DOI Listing
January 2018

Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.

J Med Chem 2017 11 24;60(21):8801-8815. Epub 2017 Oct 24.

Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.7b00841DOI Listing
November 2017

Covalent Lipid Pocket Ligands Targeting p38α MAPK Mutants.

Angew Chem Int Ed Engl 2017 10 22;56(43):13232-13236. Epub 2017 Sep 22.

Faculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

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http://doi.wiley.com/10.1002/anie.201706345
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http://dx.doi.org/10.1002/anie.201706345DOI Listing
October 2017

Design, Synthesis, and Biological Evaluation of Novel Type I/ p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine.

J Med Chem 2017 10 7;60(19):8027-8054. Epub 2017 Sep 7.

Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmaceutical Sciences, Eberhard-Karls-Universitaet Tuebingen , Auf der Morgenstelle 8, 72076 Tuebingen, Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.7b00745DOI Listing
October 2017

Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34.

Angew Chem Int Ed Engl 2017 07 12;56(28):8153-8157. Epub 2017 Jun 12.

Faculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

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http://dx.doi.org/10.1002/anie.201703738DOI Listing
July 2017

Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.

J Med Chem 2017 07 21;60(13):5613-5637. Epub 2017 Jun 21.

Institute of Pharmaceutical Sciences, Pharmaceutical and Medicinal Chemistry, Eberhard Karls University Tübingen , Auf der Morgenstelle 8, 72076 Tübingen, Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.7b00316DOI Listing
July 2017

Optimized Target Residence Time: Type I1/2 Inhibitors for p38α MAP Kinase with Improved Binding Kinetics through Direct Interaction with the R-Spine.

Angew Chem Int Ed Engl 2017 05 11;56(19):5363-5367. Epub 2017 Apr 11.

Institute of Pharmaceutical Sciences, Pharmaceutical and Medicinal Chemistry, Eberhard Karls Universität Tübingen, Auf der Morgenstelle 8, 72076, Tübingen, Germany.

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http://dx.doi.org/10.1002/anie.201701185DOI Listing
May 2017

Characterization of Covalent-Reversible EGFR Inhibitors.

ACS Omega 2017 Apr 20;2(4):1563-1575. Epub 2017 Apr 20.

Faculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/acsomega.7b00157DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6018958PMC
April 2017

Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.

J Med Chem 2017 03 10;60(6):2361-2372. Epub 2017 Mar 10.

Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, Dortmund D-44227, Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.6b01626DOI Listing
March 2017

A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant.

Bioorg Med Chem Lett 2016 08 18;26(15):3436-40. Epub 2016 Jun 18.

Dipartimento di Farmacia, Università degli Studi di Genova, Viale Benedetto XV, 3, 16132 Genova, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2016.06.051DOI Listing
August 2016

Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR.

Angew Chem Int Ed Engl 2016 08 5;55(36):10909-12. Epub 2016 Aug 5.

Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

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http://dx.doi.org/10.1002/anie.201605011DOI Listing
August 2016

Monitoring Conformational Changes in the Receptor Tyrosine Kinase EGFR.

Chembiochem 2016 06 21;17(11):990-4. Epub 2016 Apr 21.

Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

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http://dx.doi.org/10.1002/cbic.201600115DOI Listing
June 2016

11th German Conference on Chemoinformatics (GCC 2015) : Fulda, Germany. 8-10 November 2015.

Authors:
Uli Fechner Chris de Graaf Andrew E Torda Stefan Güssregen Andreas Evers Hans Matter Gerhard Hessler Nicola J Richmond Peter Schmidtke Marwin H S Segler Mark P Waller Stefanie Pleik Joan-Emma Shea Zachary Levine Ryan Mullen Karina van den Broek Matthias Epple Hubert Kuhn Andreas Truszkowski Achim Zielesny Johannes Hans Fraaije Ruben Serral Gracia Stefan M Kast Krishna C Bulusu Andreas Bender Abraham Yosipof Oren Nahum Hanoch Senderowitz Timo Krotzky Robert Schulz Gerhard Wolber Stefan Bietz Matthias Rarey Markus O Zimmermann Andreas Lange Manuel Ruff Johannes Heidrich Ionut Onlia Thomas E Exner Frank M Boeckler Marcel Bermudez Dzmitry S Firaha Oldamur Hollóczki Barbara Kirchner Christofer S Tautermann Andrea Volkamer Sameh Eid Samo Turk Friedrich Rippmann Simone Fulle Noureldin Saleh Giorgio Saladino Francesco L Gervasio Elke Haensele Lee Banting David C Whitley Jana Sopkova-de Oliveira Santos Ronan Bureau Timothy Clark Achim Sandmann Harald Lanig Patrick Kibies Jochen Heil Franziska Hoffgaard Roland Frach Julian Engel Steven Smith Debjit Basu Daniel Rauh Oliver Kohlbacher Frank M Boeckler Jonathan W Essex Michael S Bodnarchuk Gregory A Ross Arndt R Finkelmann Andreas H Göller Gisbert Schneider Tamara Husch Christoph Schütter Andrea Balducci Martin Korth Fidele Ntie-Kang Stefan Günther Wolfgang Sippl Luc Meva'a Mbaze Fidele Ntie-Kang Conrad V Simoben Lydia L Lifongo Fidele Ntie-Kang Philip Judson Jiří Barilla Miloš V Lokajíček Hana Pisaková Pavel Simr Natalia Kireeva Alexandre Petrov Denis Ostroumov Vitaly P Solovev Vladislav S Pervov Nils-Ole Friedrich Kai Sommer Matthias Rarey Johannes Kirchmair Eugen Proschak Julia Weber Daniel Moser Lena Kalinowski Janosch Achenbach Mark Mackey Tim Cheeseright Gerrit Renner Gerrit Renner Torsten C Schmidt Jürgen Schram Marion Egelkraut-Holtus Albert van Oeyen Tuomo Kalliokoski Denis Fourches Akachukwu Ibezim Chika J Mbah Umale M Adikwu Ngozi J Nwodo Alexander Steudle Brian B Masek Stephan Nagy David Baker Fred Soltanshahi Roman Dorfman Karen Dubrucq Hitesh Patel Oliver Koch Florian Mrugalla Stefan M Kast Qurrat U Ain Julian E Fuchs Robert M Owen Kiyoyuki Omoto Rubben Torella David C Pryde Robert Glen Andreas Bender Petr Hošek Vojtěch Spiwok Lewis H Mervin Ian Barrett Mike Firth David C Murray Lisa McWilliams Qing Cao Ola Engkvist Dawid Warszycki Marek Śmieja Andrzej J Bojarski Natalia Aniceto Alex Freitas Taravat Ghafourian Guido Herrmann Valentina Eigner-Pitto Alexandra Naß Rafał Kurczab Andrzej J Bojarski Andreas Lange Marcel B Günther Susanne Hennig Felix M Büttner Christoph Schall Adrian Sievers-Engler Francesco Ansideri Pierre Koch Thilo Stehle Stefan Laufer Frank M Böckler Barbara Zdrazil Floriane Montanari Gerhard F Ecker Christoph Grebner Anders Hogner Johan Ulander Karl Edman Victor Guallar Christian Tyrchan Johan Ulander Christian Tyrchan Wolfgang Klute Fredrik Bergström Christian Kramer Quoc Dat Nguyen Roland Frach Patrick Kibies Steven Strohfeldt Saraphina Böttcher Tim Pongratz Dominik Horinek Stefan M Kast Bernd Rupp Raed Al-Yamori Michael Lisurek Ronald Kühne Filipe Furtado Karina van den Broek Ludger Wessjohann Miriam Mathea Knut Baumann Siti Zuraidah Mohamad-Zobir Xianjun Fu Tai-Ping Fan Andreas Bender Maximilian A Kuhn Christoph A Sotriffer Azedine Zoufir Xitong Li Lewis Mervin Ellen Berg Mark Polokoff Wolf D Ihlenfeldt Wolf D Ihlenfeldt Jette Pretzel Zayan Alhalabi Robert Fraczkiewicz Marvin Waldman Robert D Clark Neem Shaikh Prabha Garg Alexander Kos Hans-Jürgen Himmler Achim Sandmann Christophe Jardin Heinrich Sticht Thomas B Steinbrecher Markus Dahlgren Daniel Cappel Teng Lin Lingle Wang Goran Krilov Robert Abel Richard Friesner Woody Sherman Ina A Pöhner Joanna Panecka Rebecca C Wade Stefan Bietz Karen T Schomburg Matthias Hilbig Matthias Rarey Christian Jäger Vivien Wieczorek Lance M Westerhoff Oleg Y Borbulevych Hans-Ulrich Demuth Mirko Buchholz Denis Schmidt Thomas Rickmeyer Timo Krotzky Peter Kolb Sumit Mittal Elsa Sánchez-García Mauro S Nogueira Tiago B Oliveira Fernando B da Costa Thomas J Schmidt

J Cheminform 2016 Apr 26;8(Suppl 1):18. Epub 2016 Apr 26.

Central Institute for Scientific Computing (ZISC), FAU-Erlangen-Nürnberg, Martensstr. 5a, 91058, Erlangen, Germany.

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http://dx.doi.org/10.1186/s13321-016-0119-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4896257PMC
April 2016

Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer.

ACS Med Chem Lett 2016 Jan 18;7(1):2-5. Epub 2015 Dec 18.

Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/acsmedchemlett.5b00475DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4716607PMC
January 2016

Neuritogenic militarinone-inspired 4-hydroxypyridones target the stress pathway kinase MAP4K4.

Angew Chem Int Ed Engl 2015 Oct 23;54(42):12398-403. Epub 2015 Apr 23.

Max-Planck-Institut für Molekulare Physiologie, Abteilung Chemische Biologie, Otto-Hahn-Straße 11, 44227 Dortmund (Germany).

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http://dx.doi.org/10.1002/anie.201501515DOI Listing
October 2015

Covalent-Allosteric Kinase Inhibitors.

Angew Chem Int Ed Engl 2015 Aug 25;54(35):10313-6. Epub 2015 Jun 25.

Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund (Germany).

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http://dx.doi.org/10.1002/anie.201502142DOI Listing
August 2015

FLiK: a direct-binding assay for the identification and kinetic characterization of stabilizers of inactive kinase conformations.

Methods Enzymol 2014 ;548:147-71

Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany; Fakultät Chemie, Chemische Biologie, Technische Universität Dortmund, Dortmund, Germany. Electronic address:

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http://dx.doi.org/10.1016/B978-0-12-397918-6.00006-9DOI Listing
July 2015

Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.

Bioorg Med Chem 2015 Jun 23;23(12):2767-80. Epub 2015 Apr 23.

Department of Chemistry and Chemical Biology, Technische Universität Dortmund, Otto-Hahn-Straße 6, 44227 Dortmund, Germany. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2015.04.038DOI Listing
June 2015

Monitoring ligand-induced conformational changes for the identification of estrogen receptor agonists and antagonists.

Angew Chem Int Ed Engl 2015 Mar 9;54(14):4379-82. Epub 2015 Feb 9.

Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund (Germany).

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http://dx.doi.org/10.1002/anie.201410148DOI Listing
March 2015

Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors.

ACS Chem Biol 2015 Jan 3;10(1):279-88. Epub 2014 Jul 3.

Technische Universität Dortmund , Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/cb500355cDOI Listing
January 2015

Identification and further development of potent TBK1 inhibitors.

ACS Chem Biol 2015 Jan;10(1):289-98

Department of Chemistry and Chemical Biology, Technical University of Dortmund , Otto-Hahn-Straße 6, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/cb500908dDOI Listing
January 2015

Identification of type II and III DDR2 inhibitors.

J Med Chem 2014 May 5;57(10):4252-62. Epub 2014 May 5.

Department of Chemistry and Chemical Biology, Technical University of Dortmund , Otto-Hahn-Straße 6, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/jm500167qDOI Listing
May 2014

Cell-autonomous and non-cell-autonomous mechanisms of transformation by amplified FGFR1 in lung cancer.

Cancer Discov 2014 Feb 3;4(2):246-57. Epub 2013 Dec 3.

1Department of Translational Genomics, University of Cologne; 2Max-Planck-Institute for Neurological Research; Institutes of 3Pathology and 4Virology, University of Cologne;5Department I of Internal Medicine and Center for Integrated Oncology, University Hospital of Cologne; 6Blackfield AG, Cologne; 7Technical University Dortmund, Dortmund, Germany; 8Medical Oncology and 9Institute of Pathology, Cantonal Hospital, Luzern; 10Novartis Pharma AG, Basel, Switzerland; and 11Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, India.

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http://cancerdiscovery.aacrjournals.org/cgi/doi/10.1158/2159
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http://dx.doi.org/10.1158/2159-8290.CD-13-0323DOI Listing
February 2014

Structural characterization of the RLCK family member BSK8: a pseudokinase with an unprecedented architecture.

J Mol Biol 2013 Nov 2;425(22):4455-67. Epub 2013 Aug 2.

Technische Universität Dortmund Fakultät Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1016/j.jmb.2013.07.034DOI Listing
November 2013

Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood.

J Med Chem 2013 Nov 5;56(21):8561-78. Epub 2013 Nov 5.

Institute of Pharmacy , Department of Pharmaceutical and Medicinal Chemistry, Eberhard-Karls-University Tübingen , Auf der Morgenstelle 8, 72076 Tübingen, Germany.

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http://dx.doi.org/10.1021/jm401276hDOI Listing
November 2013

Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.

J Med Chem 2013 Jul 10;56(14):5757-72. Epub 2013 Jul 10.

Department of Chemistry and Chemical Biology, Technical University of Dortmund, Otto-Hahn-Strasse 6, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/jm4004076DOI Listing
July 2013

BSKs are partially redundant positive regulators of brassinosteroid signaling in Arabidopsis.

Plant J 2013 Jun 15;74(6):905-19. Epub 2013 Apr 15.

Department of Molecular Biology and Ecology of Plants, Tel-Aviv University, Tel-Aviv, 69978, Israel.

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http://dx.doi.org/10.1111/tpj.12175DOI Listing
June 2013

Overcoming compound fluorescence in the FLiK screening assay with red-shifted fluorophores.

J Am Chem Soc 2013 Jun 24;135(22):8400-8. Epub 2013 May 24.

Chemical Genomics Centre of the Max-Planck-Society , Otto-Hahn-Strasse 15, 44137 Dortmund, Germany.

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http://dx.doi.org/10.1021/ja403074jDOI Listing
June 2013

De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments.

ACS Chem Biol 2013 May 27;8(5):1044-52. Epub 2013 Mar 27.

Drug Discovery Unit (DDU), Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Sir James Black Centre, DD1 5EH, UK.

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http://pubs.acs.org/doi/10.1021/cb300729y
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http://dx.doi.org/10.1021/cb300729yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3833278PMC
May 2013

Selective detection of allosteric phosphatase inhibitors.

J Am Chem Soc 2013 May 26;135(18):6838-41. Epub 2013 Apr 26.

Chemical Genomics Centre der Max-Planck-Gesellschaft, Dortmund, Germany.

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http://dx.doi.org/10.1021/ja4030484DOI Listing
May 2013

Tumor VEGF:VEGFR2 autocrine feed-forward loop triggers angiogenesis in lung cancer.

J Clin Invest 2013 Apr;123(4):1732-40

Max Planck Institute for Neurological Research, with Klaus-Joachim-Zülch Laboratories of the Max Planck Society and the Medical Faculty of the University of Cologne, Cologne, Germany.

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http://dx.doi.org/10.1172/JCI65385DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3613914PMC
April 2013

Highly enantioselective catalytic synthesis of neurite growth-promoting secoyohimbanes.

Chem Biol 2013 Apr;20(4):500-9

Abteilung Chemische Biologie, Max-Planck-Institut für Molekulare Physiologie, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1016/j.chembiol.2013.03.011DOI Listing
April 2013

Natural-product-derived fragments for fragment-based ligand discovery.

Nat Chem 2013 Jan 2;5(1):21-8. Epub 2012 Dec 2.

Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, D-44227 Dortmund, Germany.

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http://www.nature.com/articles/nchem.1506
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January 2013

Strategies for the selective regulation of kinases with allosteric modulators: exploiting exclusive structural features.

ACS Chem Biol 2013 Jan 31;8(1):58-70. Epub 2012 Dec 31.

Technische Universität Dortmund, Fakultät Chemie - Chemische Biologie, Otto-Hahn-Strasse 6, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/cb300663jDOI Listing
January 2013

Chemical biology--current and next challenges.

Authors:
Daniel Rauh

ACS Chem Biol 2013 Jan;8(1):1-2

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http://dx.doi.org/10.1021/cb400013tDOI Listing
January 2013

Integrative genome analyses identify key somatic driver mutations of small-cell lung cancer.

Nat Genet 2012 Oct 2;44(10):1104-10. Epub 2012 Sep 2.

Department of Translational Genomics, University of Cologne, Cologne, Germany.

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http://dx.doi.org/10.1038/ng.2396DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4915822PMC
October 2012

Targeting the hinge glycine flip and the activation loop: novel approach to potent p38α inhibitors.

J Med Chem 2012 Sep 29;55(17):7862-74. Epub 2012 Aug 29.

Institute of Pharmacy, Department of Pharmaceutical and Medicinal Chemistry, Eberhard-Karls-University Tübingen , Auf der Morgenstelle 8, 72076 Tübingen, Germany.

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http://pubs.acs.org/doi/10.1021/jm300951u
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September 2012

Epidermal growth factor receptor (EGFR) signaling and covalent EGFR inhibition in lung cancer.

J Clin Oncol 2012 Sep 20;30(27):3417-20. Epub 2012 Aug 20.

Technical University Dortmund, Dortmund, Germany.

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http://ascopubs.org/doi/10.1200/JCO.2012.43.1825
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September 2012

Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals.

ACS Chem Biol 2012 Jul 15;7(7):1257-67. Epub 2012 May 15.

Fakultät Chemie - Chemische Biologie, Technische Universität Dortmund, Germany.

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http://dx.doi.org/10.1021/cb300128bDOI Listing
July 2012

Change or be changed: reflections of the workshop 'Future in Medicinal Chemistry'.

Bioorg Med Chem 2012 Jun 25;20(12):3695-7. Epub 2012 Apr 25.

Biological Chemistry and Drug Discovery, College of Life Sciences University of Dundee, Dow St., Dundee DD1 5EH, UK.

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http://dx.doi.org/10.1016/j.bmc.2012.04.038DOI Listing
June 2012

Direct binding assay for the detection of type IV allosteric inhibitors of Abl.

J Am Chem Soc 2012 Jun 25;134(22):9138-41. Epub 2012 May 25.

Chemical Genomics Centre of the Max-Planck-Society, Dortmund, Germany.

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http://pubs.acs.org/doi/10.1021/ja303858w
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June 2012

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 Jun 15;55(12):5868-77. Epub 2012 Jun 15.

Institute of Pharmacy, Department of Pharmaceutical and Medicinal Chemistry, Eberhard-Karls-University, Auf der Morgenstelle 8, 72076 Tübingen, Germany.

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http://dx.doi.org/10.1021/jm300327hDOI Listing
June 2012

A chemical genetic approach for covalent inhibition of analogue-sensitive aurora kinase.

ACS Chem Biol 2012 Apr 1;7(4):723-31. Epub 2012 Feb 1.

Friedrich Miescher Laboratory of the Max Planck Society, Tübingen, Germany.

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http://dx.doi.org/10.1021/cb200465cDOI Listing
April 2012

Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38α.

Eur J Med Chem 2012 Feb 18;48:1-15. Epub 2011 Nov 18.

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1016/j.ejmech.2011.11.019DOI Listing
February 2012

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

Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany.

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http://dx.doi.org/10.1007/978-1-61779-349-3_8DOI Listing
January 2012

ALK mutations conferring differential resistance to structurally diverse ALK inhibitors.

Clin Cancer Res 2011 Dec 26;17(23):7394-401. Epub 2011 Sep 26.

Max Planck Institute for Neurological Research, Klaus-Joachim-Zülch Laboratories of the Max Planck Society, Köln, Germany.

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http://dx.doi.org/10.1158/1078-0432.CCR-11-1648DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3382103PMC
December 2011

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor.

Nat Chem Biol 2011 Dec 25;8(2):141-3. Epub 2011 Dec 25.

Institute of Pharmacy, University of Tübingen, Tübingen, Germany.

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http://dx.doi.org/10.1038/nchembio.761DOI Listing
December 2011

Identification of Ustilago maydis Aurora kinase as a novel antifungal target.

ACS Chem Biol 2011 Sep 20;6(9):926-33. Epub 2011 Jun 20.

Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany.

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http://dx.doi.org/10.1021/cb200112yDOI Listing
September 2011

Using small molecules to target protein phosphatases.

Bioorg Med Chem 2011 Apr 2;19(7):2145-55. Epub 2011 Mar 2.

Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1016/j.bmc.2011.02.047DOI Listing
April 2011

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.

Bioorg Med Chem 2011 Jan 10;19(1):429-39. Epub 2010 Nov 10.

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1016/j.bmc.2010.11.007DOI Listing
January 2011

Highly enantioselective synthesis and cellular evaluation of spirooxindoles inspired by natural products.

Nat Chem 2010 Sep 11;2(9):735-40. Epub 2010 Jul 11.

Max-Planck-Institut für Molekulare Physiologie, Abteilung Chemische Biologie, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1038/nchem.730DOI Listing
September 2010

Identification of thiazolidinones spiro-fused to indolin-2-ones as potent and selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase B.

Angew Chem Int Ed Engl 2010 Aug;49(34):5902-5

Abteilung Chemische Biologie, Max-Planck-Institut für molekulare Physiologie, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1002/anie.201002138DOI Listing
August 2010

RAF kinase inhibitors in cancer treatment: like a bull in a China shop?

Chembiochem 2010 Aug;11(12):1645-8

Chemical Genomics Centre der Max-Planck-Gesellschaft, Otto-Hahn-Strasse 15, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1002/cbic.201000348DOI Listing
August 2010

A scaffold-tree-merging strategy for prospective bioactivity annotation of gamma-pyrones.

Angew Chem Int Ed Engl 2010 May;49(21):3666-70

Department of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1002/anie.200906555DOI Listing
May 2010

Proteus in the world of proteins: conformational changes in protein kinases.

Arch Pharm (Weinheim) 2010 Apr;343(4):193-206

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://doi.wiley.com/10.1002/ardp.201000028
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April 2010

Fluorophore labeling of the glycine-rich loop as a method of identifying inhibitors that bind to active and inactive kinase conformations.

J Am Chem Soc 2010 Mar;132(12):4152-60

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/ja908083eDOI Listing
March 2010

Displacement assay for the detection of stabilizers of inactive kinase conformations.

J Med Chem 2010 Jan;53(1):357-67

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/jm901297eDOI Listing
January 2010

Analysis of compound synergy in high-throughput cellular screens by population-based lifetime modeling.

PLoS One 2010 Jan 27;5(1):e8919. Epub 2010 Jan 27.

Max Planck Institute for Neurological Research with Klaus-Joachim-Zülch Laboratories of the Max Planck Society and the Medical Faculty of the University of Köln, Max Planck Society, Köln, Germany.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0008919PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2811738PMC
January 2010

Fullerene dimers (C60/C70) for energy harvesting.

Chemistry 2009 Dec;15(48):13474-82

Departamento de Química Orgánica, Facultad de Ciencias Químicas, Universidad Complutense de Madrid, 28040 Madrid, Spain.

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http://dx.doi.org/10.1002/chem.200902039DOI Listing
December 2009