Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity

The promiscuity of most kinase inhibitors can cause drug toxicity and complicate the interpretation of experiments. Rather than assessing kinase-compound binding, Anastassiadis et al . use functional assays to profile the activities of 178 commercially available kinase inhibitors against 300 recombi...

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Veröffentlicht in:	Nature biotechnology 2011-11, Vol.29 (11), p.1039-1045
Hauptverfasser:	Anastassiadis, Theonie, Deacon, Sean W, Devarajan, Karthik, Ma, Haiching, Peterson, Jeffrey R
Format:	Artikel
Sprache:	eng
Schlagworte:	631/61/32 631/92/613 692/308/153 Agriculture Analysis ATP Bioassays Bioinformatics Biological and medical sciences Biomedical and Life Sciences Biomedical Engineering/Biotechnology Biomedicine Biotechnology Cancer Care and treatment Catalysis Cellular biology Drug Design Enzyme Stability Fundamental and applied biological sciences. Psychology Health aspects Health. Pharmaceutical industry High-Throughput Screening Assays Humans Industrial applications and implications. Economical aspects Inhibitors Kinases Life Sciences Miscellaneous Molecular and cellular biology Molecular biology Phosphotransferases Physiological aspects Protection and preservation Protein Binding Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - classification Protein Kinases - chemistry Protein Kinases - classification Proteins Recombinant proteins resource Signal Transduction Substrate Specificity
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