Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors

Journal of the American Chemical Society

Volumn 131, Issue 37, 2009, Pages 13286-13296

  Simard, Jeffrey R ^a   Getlik, Matthäus ^a   Grütter, Christian ^a   Pawar, Vijaykumar ^a   Wulfert, Sabine ^a   Rabiller, Matthias ^a   Rauh, Daniel ^a  

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

Author keywords

[No Author keywords available]

Indexed keywords

, INHIBITOR; ACTIVATION LOOPS; ALLOSTERIC SITE; BINDING ASSAYS; BINDING MODES; BINDING POCKETS; CHEMICAL ENTITY; CONFORMATIONAL CHANGE; DISSOCIATION KINETICS; DRUG RESISTANCE; HIGH AFFINITY; HIGH-THROUGHPUT METHOD; INTRACELLULAR SIGNALING PATHWAYS; KINASE ASSAYS; KINASE INHIBITORS; NANOMOLAR INHIBITORS; NEW OPPORTUNITIES; PROTEIN X-RAY CRYSTALLOGRAPHY; QUINAZOLINES; SORAFENIB; TYPE II;

BINDING ENERGY; BINDING SITES; CONFORMATIONS; DISSOCIATION; FLUORESCENCE; IMAGE SENSORS; LIGANDS; MINERALOGY; SCAFFOLDS; SELF ASSEMBLY;

X RAY CRYSTALLOGRAPHY;

MITOGEN ACTIVATED PROTEIN KINASE 14; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; QUINAZOLINE DERIVATIVE; QUINOLINE DERIVATIVE; SERINE; SORAFENIB; THREONINE; UREA DERIVATIVE;

ALLOSTERISM; ARTICLE; CHEMICAL STRUCTURE; CONFORMATIONAL TRANSITION; DISSOCIATION; FLUORESCENCE; HUMAN; HUMAN CELL; LIGAND BINDING; SYNTHESIS; VALIDATION PROCESS; X RAY CRYSTALLOGRAPHY;

ADENOSINE TRIPHOSPHATE; ALLOSTERIC REGULATION; AMINO ACID SEQUENCE; BENZENESULFONATES; BINDING, COMPETITIVE; CATALYTIC DOMAIN; CRYSTALLOGRAPHY, X-RAY; DRUG EVALUATION, PRECLINICAL; ENZYME ACTIVATION; ENZYME STABILITY; FLUORESCENT DYES; HUMANS; KINETICS; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; P38 MITOGEN-ACTIVATED PROTEIN KINASES; PROTEIN KINASE INHIBITORS; PYRAZOLES; PYRIDINES; REPRODUCIBILITY OF RESULTS; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 67649995940     PISSN: 00027863     EISSN: None     Source Type: Journal    
DOI: 10.1021/ja902010p     Document Type: Article

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