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Tytuł :
Resistance to Avapritinib in PDGFRA-Driven GIST Is Caused by Secondary Mutations in the PDGFRA Kinase Domain.
Autorzy :
Grunewald S; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany.; DKTK partner site Essen, German Cancer Consortium (DKTK), Heidelberg, Germany.
Klug LR; Portland VA Health Care System, Portland, Oregon; Knight Cancer Institute, Oregon Health and Science University, Portland, Oregon; and Division of Hematology and Medical Oncology, Oregon Health and Science University, Portland, Oregon.
Mühlenberg T; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany.; DKTK partner site Essen, German Cancer Consortium (DKTK), Heidelberg, Germany.
Lategahn J; Faculty of Chemistry and Chemical Biology, TU Dortmund University, Dortmund, Germany.; Drug Discovery Hub Dortmund (DDHD) am Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Falkenhorst J; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany.; DKTK partner site Essen, German Cancer Consortium (DKTK), Heidelberg, Germany.
Town A; Portland VA Health Care System, Portland, Oregon; Knight Cancer Institute, Oregon Health and Science University, Portland, Oregon; and Division of Hematology and Medical Oncology, Oregon Health and Science University, Portland, Oregon.
Ehrt C; Faculty of Chemistry and Chemical Biology, TU Dortmund University, Dortmund, Germany.; Drug Discovery Hub Dortmund (DDHD) am Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Wardelmann E; Gerhard-Domagk-Institute of Pathology, University of Münster Medical Center, Münster, Germany.
Hartmann W; Gerhard-Domagk-Institute of Pathology, University of Münster Medical Center, Münster, Germany.
Schildhaus HU; Institute of Pathology, University Medical Center Essen, Essen, Germany.
Treckmann J; Department of Visceral Surgery, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany.
Fletcher JA; Department of Pathology, Brigham and Women's Hospital, Boston, Massachusetts.
Jung S; Faculty of Chemistry and Chemical Biology, TU Dortmund University, Dortmund, Germany.
Czodrowski P; Faculty of Chemistry and Chemical Biology, TU Dortmund University, Dortmund, Germany.
Miller S; Blueprint Medicines, Cambridge, Massachusetts.
Schmidt-Kittler O; Blueprint Medicines, Cambridge, Massachusetts.
Rauh D; Faculty of Chemistry and Chemical Biology, TU Dortmund University, Dortmund, Germany.; Drug Discovery Hub Dortmund (DDHD) am Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Heinrich MC; Portland VA Health Care System, Portland, Oregon; Knight Cancer Institute, Oregon Health and Science University, Portland, Oregon; and Division of Hematology and Medical Oncology, Oregon Health and Science University, Portland, Oregon.
Bauer S; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany. .; DKTK partner site Essen, German Cancer Consortium (DKTK), Heidelberg, Germany.
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Źródło :
Cancer discovery [Cancer Discov] 2020 Sep 24. Date of Electronic Publication: 2020 Sep 24.
Typ publikacji :
Journal Article
Czasopismo naukowe
Tytuł :
KIT-Dependent and KIT-Independent Genomic Heterogeneity of Resistance in Gastrointestinal Stromal Tumors - TORC1/2 Inhibition as Salvage Strategy.
Autorzy :
Mühlenberg T; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany. thomas.muehlenberg@uk-essen.de .; German Cancer Consortium (DKTK), Heidelberg, Germany.
Ketzer J; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany.; German Cancer Consortium (DKTK), Heidelberg, Germany.
Heinrich MC; Portland VA Health Care System, Knight Cancer Institute, Oregon Health and Science University, Portland, Oregon.
Grunewald S; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany.; German Cancer Consortium (DKTK), Heidelberg, Germany.
Marino-Enriquez A; Department of Pathology, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts.
Trautmann M; Gerhard Domagk Institute of Pathology, University Hospital Münster, Münster, Germany.
Hartmann W; Gerhard Domagk Institute of Pathology, University Hospital Münster, Münster, Germany.
Wardelmann E; Gerhard Domagk Institute of Pathology, University Hospital Münster, Münster, Germany.
Treckmann J; Department of Visceral and Transplant Surgery, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany.
Worm K; Institute of Pathology, University Hospital of Essen, University of Duisburg-Essen, Germany.
Bertram S; Institute of Pathology, University Hospital of Essen, University of Duisburg-Essen, Germany.
Herold T; German Cancer Consortium (DKTK), Heidelberg, Germany.; Institute of Pathology, University Hospital of Essen, University of Duisburg-Essen, Germany.
Schildhaus HU; Institute of Pathology, Universitätsmedizin Göttingen, Göttingen, Germany.
Glimm H; German Cancer Consortium (DKTK), Heidelberg, Germany.; Department of Translational Oncology, National Center for Tumor Diseases (NCT) Dresden, Dresden University Hospital, Dresden, Germany.
Stenzinger A; German Cancer Consortium (DKTK), Heidelberg, Germany.; Institute of Pathology, Heidelberg University Hospital, Heidelberg, Germany.
Brors B; German Cancer Consortium (DKTK), Heidelberg, Germany.; Department of Applied Bioinformatics, German Cancer Research Center (DKFZ), Heidelberg University, Heidelberg, Germany.
Horak P; German Cancer Consortium (DKTK), Heidelberg, Germany.; Department of Translational Oncology, National Center for Tumor Diseases (NCT) Heidelberg, German Cancer Research Center (DKFZ), Heidelberg University Hospital, Heidelberg, Germany.
Hohenberger P; Mannheim, University Medical Center, Mannheim, Germany.
Fröhling S; German Cancer Consortium (DKTK), Heidelberg, Germany.; Department of Translational Oncology, National Center for Tumor Diseases (NCT) Heidelberg, German Cancer Research Center (DKFZ), Heidelberg University Hospital, Heidelberg, Germany.
Fletcher JA; Department of Pathology, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts.
Bauer S; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Essen, Germany. thomas.muehlenberg@uk-essen.de .; German Cancer Consortium (DKTK), Heidelberg, Germany.
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Źródło :
Molecular cancer therapeutics [Mol Cancer Ther] 2019 Nov; Vol. 18 (11), pp. 1985-1996. Date of Electronic Publication: 2019 Jul 15.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms :
Drug Resistance, Neoplasm*/drug effects
Mutation*
Gastrointestinal Stromal Tumors/*genetics
High-Throughput Nucleotide Sequencing/*methods
Protein Kinase Inhibitors/*pharmacology
Proto-Oncogene Proteins c-kit/*genetics
Pyrazoles/*pharmacology
Pyrimidines/*pharmacology
Cell Line, Tumor ; Female ; Gastrointestinal Stromal Tumors/drug therapy ; Gene Regulatory Networks/drug effects ; Genetic Heterogeneity ; Humans ; Salvage Therapy ; Sequence Analysis, DNA ; Signal Transduction
Czasopismo naukowe
Tytuł :
Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S.
Autorzy :
Lategahn J; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.; Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) , 44227 Dortmund , Germany.
Keul M; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.; Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) , 44227 Dortmund , Germany.
Klövekorn P; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.
Tumbrink HL; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.
Niggenaber J; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.; Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) , 44227 Dortmund , Germany.
Müller MP; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.; Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) , 44227 Dortmund , Germany.
Hodson L; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.; Department of Chemistry and Polymer Science , Stellenbosch University , Private Bag X1 , Matieland 7602 , South Africa.
Flaßhoff M; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.
Hardick J; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.; Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) , 44227 Dortmund , Germany.
Grabe T; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.; Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) , 44227 Dortmund , Germany.
Engel J; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.
Schultz-Fademrecht C; Lead Discovery Center GmbH , Otto-Hahn-Strasse 15 , 44227 Dortmund , Germany.
Baumann M; Lead Discovery Center GmbH , Otto-Hahn-Strasse 15 , 44227 Dortmund , Germany.
Ketzer J; Department of Medical Oncology , Sarcoma Center , West German Cancer Center , University Duisburg-Essen , Medical School , Hufelandstrasse 55 , 45122 Essen , Germany.; German Cancer Consortium (DKTK) , 69120, Heidelberg , Germany.
Mühlenberg T; Department of Medical Oncology , Sarcoma Center , West German Cancer Center , University Duisburg-Essen , Medical School , Hufelandstrasse 55 , 45122 Essen , Germany.; German Cancer Consortium (DKTK) , 69120, Heidelberg , Germany.
Hiller W; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.
Günther G; Leibniz Research Centre for Working Environment and Human Factors (IfADo) , TU Dortmund University , Ardeystrasse 67 , 44139 Dortmund , Germany.
Unger A; Lead Discovery Center GmbH , Otto-Hahn-Strasse 15 , 44227 Dortmund , Germany.
Müller H; Lead Discovery Center GmbH , Otto-Hahn-Strasse 15 , 44227 Dortmund , Germany.
Heimsoeth A; Molecular Pathology , Institute of Pathology , University Hospital of Cologne , Kerpener Strasse 62 , 50937 Cologne , Germany.; Department of Translational Genomics , Center of Integrated Oncology Cologne-Bonn , Medical Faculty , University of Cologne , Weyertal 115b , 50931 Cologne , Germany.
Golz C; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.
Blank-Landeshammer B; Leibniz-Institut für Analytische Wissenschaften - ISAS - e.V. , Otto-Hahn-Strasse 6b , 44227 Dortmund , Germany.
Kollipara L; Leibniz-Institut für Analytische Wissenschaften - ISAS - e.V. , Otto-Hahn-Strasse 6b , 44227 Dortmund , Germany.
Zahedi RP; Leibniz-Institut für Analytische Wissenschaften - ISAS - e.V. , Otto-Hahn-Strasse 6b , 44227 Dortmund , Germany.; Segal Cancer Proteomics Centre , Lady Davis Institute , Jewish General Hospital , McGill University , 3755 Côte Ste-Catherine Road , Montreal , Quebec H3T 1E2 , Canada.
Strohmann C; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.
Hengstler JG; Leibniz Research Centre for Working Environment and Human Factors (IfADo) , TU Dortmund University , Ardeystrasse 67 , 44139 Dortmund , Germany.
van Otterlo WAL; Department of Chemistry and Polymer Science , Stellenbosch University , Private Bag X1 , Matieland 7602 , South Africa.
Bauer S; Department of Medical Oncology , Sarcoma Center , West German Cancer Center , University Duisburg-Essen , Medical School , Hufelandstrasse 55 , 45122 Essen , Germany.; German Cancer Consortium (DKTK) , 69120, Heidelberg , Germany.
Rauh D; Faculty of Chemistry and Chemical Biology , TU Dortmund University , Otto-Hahn-Strasse 4a , 44227 Dortmund , Germany . Email: ; www.twitter.com/DDHDortmund ; Tel: +49-231-755-7080.; Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) , 44227 Dortmund , Germany.
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Źródło :
Chemical science [Chem Sci] 2019 Oct 04; Vol. 10 (46), pp. 10789-10801. Date of Electronic Publication: 2019 Oct 04 (Print Publication: 2019).
Typ publikacji :
Journal Article
Czasopismo naukowe
Tytuł :
Genomic aberrations in cell cycle genes predict progression of KIT -mutant gastrointestinal stromal tumors (GISTs).
Autorzy :
Heinrich MC; 1Hematology/Medical Oncology, Portland VA Health Care System and OHSU Knight Cancer Institute, 3710 SW U.S. Veterans Hospital Road, R&D 19, Portland, OR 97239 USA.
Patterson J; 1Hematology/Medical Oncology, Portland VA Health Care System and OHSU Knight Cancer Institute, 3710 SW U.S. Veterans Hospital Road, R&D 19, Portland, OR 97239 USA.
Beadling C; 1Hematology/Medical Oncology, Portland VA Health Care System and OHSU Knight Cancer Institute, 3710 SW U.S. Veterans Hospital Road, R&D 19, Portland, OR 97239 USA.
Wang Y; 2Department of Pathology, Brigham and Women's Hospital, 75 Francis Street, Boston, MA 02115 USA.
Debiec-Rychter M; 3Department of Human Genetics, Katholieke Universiteit Leuven and University Hospitals Leuven, Herestraat 49, 3000 Leuven, Belgium.
Dewaele B; 3Department of Human Genetics, Katholieke Universiteit Leuven and University Hospitals Leuven, Herestraat 49, 3000 Leuven, Belgium.
Corless CL; 1Hematology/Medical Oncology, Portland VA Health Care System and OHSU Knight Cancer Institute, 3710 SW U.S. Veterans Hospital Road, R&D 19, Portland, OR 97239 USA.
Duensing A; 4Cancer Therapeutics Program, UPMC Hillman Cancer Center, 5117 Centre Avenue, Pittsburgh, PA 15213 USA.
Raut CP; 5Department of Surgery, Brigham and Women's Hospital, Dana-Farber Cancer Institute and Harvard Medical School, Boston, MA USA.
Rubin B; 6Department of Molecular Genetics, Cleveland Clinic and Lerner Research Institute, L25, 9500 Euclid Avenue, Cleveland, OH 44195 USA.
Ordog T; 7Department of Physiology and Biomedical Engineering, Division of Gastroenterology and Hepatology and Center for Individualized Medicine, Mayo Clinic, 200 1st Street SW, Rochester, MN USA.
van de Rijn M; 8Department of Pathology, Stanford University Medical Center, 300 Pasteur Dr., Stanford, CA 94305 USA.
Call J; 9The Life Raft Group, 155 Route 46 West, Suite 202, Wayne, NJ 07470 USA.
Mühlenberg T; Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University of Duisburg-Essen, Hufelandstrasse 55, 45147 Essen, Germany.
Fletcher JA; 2Department of Pathology, Brigham and Women's Hospital, 75 Francis Street, Boston, MA 02115 USA.
Bauer S; Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University of Duisburg-Essen, Hufelandstrasse 55, 45147 Essen, Germany.; 11Germany and German Cancer Consortium (DKTK), Partner Site University Hospital Essen, Essen, Germany.
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Źródło :
Clinical sarcoma research [Clin Sarcoma Res] 2019 Mar 05; Vol. 9, pp. 3. Date of Electronic Publication: 2019 Mar 05 (Print Publication: 2019).
Typ publikacji :
Journal Article
Czasopismo naukowe
Tytuł :
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.
Autorzy :
Kaitsiotou H; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.
Keul M; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.
Hardick J; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.
Mühlenberg T; Department of Medical Oncology, Sarcoma Centre West German Cancer Centre University Duisburg-Essen, Medical School , Hufelandstraße 55, D-45122 Essen, Germany.; Germany and German Cancer Consortium (DKTK), Partner Site University Hospital Essen , D-45147 Essen, Germany.
Ketzer J; Department of Medical Oncology, Sarcoma Centre West German Cancer Centre University Duisburg-Essen, Medical School , Hufelandstraße 55, D-45122 Essen, Germany.; Germany and German Cancer Consortium (DKTK), Partner Site University Hospital Essen , D-45147 Essen, Germany.
Ehrt C; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.
Krüll J; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.
Medda F; Taros Chemicals GmbH & Co. KG , Emil-Figge-Straße 76a, D-44227 Dortmund, Germany.
Koch O; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.
Giordanetto F; Taros Chemicals GmbH & Co. KG , Emil-Figge-Straße 76a, D-44227 Dortmund, Germany.
Bauer S; Department of Medical Oncology, Sarcoma Centre West German Cancer Centre University Duisburg-Essen, Medical School , Hufelandstraße 55, D-45122 Essen, Germany.; Germany and German Cancer Consortium (DKTK), Partner Site University Hospital Essen , D-45147 Essen, Germany.
Rauh D; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2017 Nov 09; Vol. 60 (21), pp. 8801-8815. Date of Electronic Publication: 2017 Oct 24.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Mutation*
Drug Resistance, Neoplasm/*drug effects
Protein Kinase Inhibitors/*chemical synthesis
Proto-Oncogene Proteins c-kit/*antagonists & inhibitors
Drug Resistance, Neoplasm/genetics ; Gastrointestinal Neoplasms/drug therapy ; Humans ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive/drug therapy ; Proto-Oncogene Proteins c-kit/genetics ; Receptor Protein-Tyrosine Kinases/antagonists & inhibitors ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.
Autorzy :
Tomassi S; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, Dortmund D-44227, Germany.
Lategahn J; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, Dortmund D-44227, Germany.
Engel J; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, Dortmund D-44227, Germany.
Keul M; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, Dortmund D-44227, Germany.
Tumbrink HL; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, Dortmund D-44227, Germany.
Ketzer J; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen , Medical School, Hufelandstraße 55, Essen D-45122, Germany.; German Cancer Consortium (DKTK) , Heidelberg D-69120, Germany.
Mühlenberg T; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen , Medical School, Hufelandstraße 55, Essen D-45122, Germany.; German Cancer Consortium (DKTK) , Heidelberg D-69120, Germany.
Baumann M; Lead Discovery Center GmbH , Otto-Hahn-Straße 15, Dortmund D-44227, Germany.
Schultz-Fademrecht C; Lead Discovery Center GmbH , Otto-Hahn-Straße 15, Dortmund D-44227, Germany.
Bauer S; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen , Medical School, Hufelandstraße 55, Essen D-45122, Germany.; German Cancer Consortium (DKTK) , Heidelberg D-69120, Germany.
Rauh D; Faculty of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 4a, Dortmund D-44227, Germany.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2017 Mar 23; Vol. 60 (6), pp. 2361-2372. Date of Electronic Publication: 2017 Mar 10.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Antineoplastic Agents/*chemistry
Antineoplastic Agents/*pharmacology
Carcinoma, Non-Small-Cell Lung/*drug therapy
ErbB Receptors/*antagonists & inhibitors
Lung Neoplasms/*drug therapy
Animals ; Antineoplastic Agents/pharmacokinetics ; Carcinoma, Non-Small-Cell Lung/genetics ; Cell Line, Tumor ; Drug Resistance, Neoplasm/drug effects ; ErbB Receptors/genetics ; Humans ; Indazoles ; Lung/drug effects ; Lung/metabolism ; Lung Neoplasms/genetics ; Mice ; Molecular Docking Simulation ; Mutation/drug effects ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacokinetics ; Protein Kinase Inhibitors/pharmacology
Czasopismo naukowe
Tytuł :
Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR.
Autorzy :
Engel J; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.
Becker C; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.
Lategahn J; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.
Keul M; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.
Ketzer J; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Hufelandstrasse 55, 45122, Essen, Germany.; German Cancer Consortium (DKTK), 69120, Heidelberg, Germany.
Mühlenberg T; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Hufelandstrasse 55, 45122, Essen, Germany.; German Cancer Consortium (DKTK), 69120, Heidelberg, Germany.
Kollipara L; Leibnitz-Institut für Analytische Wissenschaften-ISAS-e.V., Otto-Hahn-Strasse 6b, 44227, Dortmund, Germany.
Schultz-Fademrecht C; Lead Discovery Center, Otto-Hahn-Strasse 15, 44227, Dortmund, Germany.
Zahedi RP; Leibnitz-Institut für Analytische Wissenschaften-ISAS-e.V., Otto-Hahn-Strasse 6b, 44227, Dortmund, Germany.
Bauer S; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School, Hufelandstrasse 55, 45122, Essen, Germany.; German Cancer Consortium (DKTK), 69120, Heidelberg, Germany.
Rauh D; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany. .
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Źródło :
Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2016 Aug 26; Vol. 55 (36), pp. 10909-12. Date of Electronic Publication: 2016 Aug 05.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
ErbB Receptors/*metabolism
Protein Kinase Inhibitors/*metabolism
Binding Sites ; Carcinoma, Non-Small-Cell Lung/metabolism ; Carcinoma, Non-Small-Cell Lung/pathology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Resistance, Neoplasm/drug effects ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/genetics ; Humans ; Kinetics ; Lung Neoplasms/metabolism ; Lung Neoplasms/pathology ; Molecular Docking Simulation ; Phosphorylation ; Point Mutation ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Pyrazoles/chemistry ; Pyrazoles/metabolism ; Pyrazoles/pharmacology ; Pyridines/chemistry ; Pyridines/metabolism ; Pyridines/pharmacology
Czasopismo naukowe
Tytuł :
Inhibitor of Apoptosis Proteins (IAPs) are commonly dysregulated in GIST and can be pharmacologically targeted to enhance the pro-apoptotic activity of imatinib.
Autorzy :
Falkenhorst J; Sarcoma Center, Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.
Grunewald S; Sarcoma Center, Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.
Mühlenberg T; Sarcoma Center, Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.
Marino-Enriquez A; Department of Pathology, Brigham and Women's Hospital, Boston, MA, USA.
Reis AC; Sarcoma Center, Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.; Department of Pathology and Neuropathology, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.
Corless C; Department of Pathology, Oregon Health and Science University Knight Cancer Institute, Portland, OR, USA.
Heinrich M; Department of Medical Oncology, Oregon Health and Science University Knight Cancer Institute, Portland, OR, USA.
Treckmann J; Sarcoma Center, Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.; Department of Surgery, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.
Podleska LE; Sarcoma Center, Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.; Department of Surgery, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.
Schuler M; Sarcoma Center, Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.; German Cancer Consortium (DKTK), Heidelberg, Germany.
Fletcher JA; Department of Pathology, Brigham and Women's Hospital, Boston, MA, USA.
Bauer S; Sarcoma Center, Department of Medical Oncology, West German Cancer Center, University Hospital Essen, University Duisburg-Essen, Essen, Germany.; German Cancer Consortium (DKTK), Heidelberg, Germany.
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Źródło :
Oncotarget [Oncotarget] 2016 Jul 05; Vol. 7 (27), pp. 41390-41403.
Typ publikacji :
Journal Article
MeSH Terms :
Gastrointestinal Neoplasms/*drug therapy
Gastrointestinal Neoplasms/*genetics
Gastrointestinal Stromal Tumors/*drug therapy
Gastrointestinal Stromal Tumors/*genetics
Imatinib Mesylate/*therapeutic use
Inhibitor of Apoptosis Proteins/*genetics
Protein Kinase Inhibitors/*therapeutic use
Apoptosis/drug effects ; Apoptosis/genetics ; Cell Line, Tumor ; Gastrointestinal Neoplasms/pathology ; Gastrointestinal Stromal Tumors/pathology ; Gene Expression Regulation, Neoplastic ; Humans ; Molecular Targeted Therapy ; Proto-Oncogene Proteins c-kit/antagonists & inhibitors ; Signal Transduction/drug effects ; Signal Transduction/genetics
Czasopismo naukowe
Tytuł :
Covalent-Allosteric Kinase Inhibitors.
Autorzy :
Weisner J; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund (Germany).
Gontla R; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund (Germany).
van der Westhuizen L; Department of Chemistry and Polymer Sciences, Stellenbosch University, Matieland (South Africa).
Oeck S; Institute of Cell Biology (Cancer Research), Department of Molecular Cell Biology, University of Duisburg-Essen, Medical School (Germany).
Ketzer J; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School (Germany).; German Cancer Consortium (DKTK), Heidelberg (Germany).
Janning P; Max-Planck-Institut für Molekulare Physiologie, Abteilung Chemische Biologie, Dortmund (Germany).
Richters A; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund (Germany).
Mühlenberg T; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School (Germany).; German Cancer Consortium (DKTK), Heidelberg (Germany).
Fang Z; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund (Germany).
Taher A; Department of Chemistry and Polymer Sciences, Stellenbosch University, Matieland (South Africa).
Jendrossek V; Institute of Cell Biology (Cancer Research), Department of Molecular Cell Biology, University of Duisburg-Essen, Medical School (Germany).
Pelly SC; Department of Chemistry and Polymer Sciences, Stellenbosch University, Matieland (South Africa).
Bauer S; Department of Medical Oncology, Sarcoma Center, West German Cancer Center, University Duisburg-Essen, Medical School (Germany).; German Cancer Consortium (DKTK), Heidelberg (Germany).
van Otterlo WA; Department of Chemistry and Polymer Sciences, Stellenbosch University, Matieland (South Africa).
Rauh D; Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund (Germany). .
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Źródło :
Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2015 Aug 24; Vol. 54 (35), pp. 10313-6. Date of Electronic Publication: 2015 Jun 25.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Protein Kinase Inhibitors/*pharmacology
Proto-Oncogene Proteins c-akt/*antagonists & inhibitors
Signal Transduction/*drug effects
Adenosine Triphosphate/metabolism ; Allosteric Regulation ; Binding, Competitive ; Humans ; Models, Molecular
Czasopismo naukowe

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