Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach

Journal of Medicinal Chemistry

Volumn 58, Issue 17, 2015, Pages 6844-6863

  Engel, Julian ^a   Richters, André ^a   Getlik, Matthäus ^b   Tomassi, Stefano ^a   Keul, Marina ^a   Termathe, Martin ^b   Lategahn, Jonas ^a   Becker, Christian ^a   Mayer Wrangowski, Svenja ^a   Grütter, Christian ^a   Uhlenbrock, Niklas ^a   Krüll, Jasmin ^a   Schaumann, Niklas ^a   Eppmann, Simone ^a   Kibies, Patrick ^a   Hoffgaard, Franziska ^a   Heil, Jochen ^a   Menninger, Sascha ^c   Ortiz Cuaran, Sandra ^d   Heuckmann, Johannes M ^d   Tinnefeld, Verena ^e   Zahedi, René P ^e   Sos, Martin L ^d,f   Schultz Fademrecht, Carsten ^c   Thomas, Roman K ^d   Kast, Stefan M ^a   Rauh, Daniel ^a,b   more..

^a TU DORTMUND UNIVERSITY   (Germany)

^b CHEMICAL GENOMICS CENTRE OF THE MAX PLANCK SOCIETY   (Germany)

^c Lead Discovery Center GmbH   (Germany)

^d UNIVERSITY OF COLOGNE   (Germany)

^e LEIBNIZ INSTITUT FÜR ANALYTISCHE WISSENSCHAFTEN ISAS E V   (Germany)

^f UNIVERSITY HOSPITAL OF COLOGNE   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; N [3 [[5 CHLORO 2 [[2 METHOXY 4 (4 METHYL 1 PIPERAZINYL)PHENYL]AMINO] 4 PYRIMIDINYL]OXY]PHENYL]ACRYLAMIDE; EGFR PROTEIN, HUMAN; MOLECULAR LIBRARY; PROTEIN TYROSINE KINASE; PYRAZOLE DERIVATIVE; PYRIMIDINE DERIVATIVE; QUINAZOLINE DERIVATIVE;

ANTINEOPLASTIC ACTIVITY; ARTICLE; COVALENT BOND; CRYSTAL STRUCTURE; HUMAN; HUMAN CELL; LIQUID CHROMATOGRAPHY; MOLECULAR LIBRARY; MOLECULARLY TARGETED THERAPY; NON SMALL CELL LUNG CANCER; PHENOTYPE; PROTEIN DEGRADATION; SYNTHESIS; TANDEM MASS SPECTROMETRY; X RAY CRYSTALLOGRAPHY; ANTAGONISTS AND INHIBITORS; CELL MEMBRANE PERMEABILITY; CHEMICAL DATABASE; CHEMICAL STRUCTURE; CHEMISTRY; CONFORMATION; DRUG DESIGN; DRUG RESISTANCE; GENETICS; KINETICS; LUNG TUMOR; MUTATION; SOLUBILITY; STRUCTURE ACTIVITY RELATION; TUMOR CELL LINE;

ANTINEOPLASTIC AGENTS; CARCINOMA, NON-SMALL-CELL LUNG; CELL LINE, TUMOR; CELL MEMBRANE PERMEABILITY; CRYSTALLOGRAPHY, X-RAY; DATABASES, CHEMICAL; DRUG DESIGN; DRUG RESISTANCE, NEOPLASM; HUMANS; KINETICS; LUNG NEOPLASMS; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MUTATION; PYRAZOLES; PYRIMIDINES; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; SMALL MOLECULE LIBRARIES; SOLUBILITY; SRC-FAMILY KINASES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84941585574     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01082     Document Type: Article

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