Kinase inhibitors : methods and protocols / edited by Bernhard Kuster.

Contributor(s): Kuster, Bernhard
Material type: TextTextSeries: Methods in molecular biology (Clifton, N.J.): v. 795.Publisher: New York : Humana Press : Springer Science+Business Media [distributor], ©2012Description: 1 online resource (xi, 256 pages) : illustrationsContent type: text Media type: computer Carrier type: online resourceISBN: 9781617793370; 161779337X; 9781617793363; 1617793361Subject(s): Protein kinases -- Inhibitors | Enzyme Inhibitors | Investigative Techniques | Drug Therapy | Publication Formats | Molecular Mechanisms of Pharmacological Action | Analytical, Diagnostic and Therapeutic Techniques and Equipment | Publication Characteristics | Therapeutics | Pharmacologic Actions | Chemical Actions and Uses | Chemicals and Drugs | Protein Kinase Inhibitors | Methods | Laboratory Manuals | Molecular Targeted Therapy | Medicine | Cytology | Biomedicine | Molecular Medicine | Cell Biology | celbiologie | cellular biology | biomedische wetenschappen | geneeskunde | Medicine (General) | Geneeskunde (algemeen)Genre/Form: Electronic books. Additional physical formats: Print version:: Kinase inhibitors.DDC classification: 572/.792 LOC classification: QP606.P76 | K56 2012Online resources: Click here to access online
Contents:
Measuring the activity of leucine-rich repeat kinase 2: A kinase involved in Parkinson's disease -- Measuring PI3K lipid kinase activity -- A fluorescence polarization assay for the discovery of inhibitors of the polo-box domain of polo-like kinase 1 -- Assessment of hepatotoxicity potential of drug candidate molecules including kinase inhibitors by hepatocyte imaging assay technology and bile flux imaging assay technology -- Kinase inhibitor selectivity profiling using differential scanning fluorimetry -- Chemoproteomic characterization of protein kinase inhibitors using immobilized ATP -- Proteome-wide identification of staurosporine-binding kinases using capture compound mass spectrometry -- Affinity purification of proteins binding to kinase inhibitors immobilized on self-assembling monolayers -- Kinase inhibitor profiling using chemoproteomics -- Covalent cross-linking of kinases with their corresponding peptide substrates -- Receptor tyrosine kinase inhibitor profiling using bead-based multiplex sandwich immunoassays -- Monitoring phosphoproteomic response to targeted kinase inhibitors using reverse-phase protein microarrays -- Measuring phosphorylation-specific changes in response to kinase inhibitors in mammalian cells using quantitative proteomics -- Investigation of acquired resistance to EGFR-targeted therapies in lung cancer using cDNA microarrays.
Summary: Protein and lipid kinases are often the master regulators of cell signaling in eukaryotic systems. The human genome codes for more than 500 of these enzymes and their misregulation has been shown to be involved in the onset and progression of many diseases including cancer and inflammation. Therefore, small molecule kinase inhibitors have become important research tools for the elucidation of the many biological roles of kinases and their mechanisms of action. Kinase inhibitors thus also contribute significantly to the drug pipelines of the pharmaceutical and biotechnology industries and to the growing need to treat cancer and inflammation. In Kinase Inhibitors: Methods and Protocols, experts in kinase biology, drug discovery, and clinical research present a series of exemplary methods that can be used to address the many challenges facing scientists in the discovery and development of kinase inhibitors both for research and clinical use. Written in the highly successful Methods in Molecular Biology series format, chapters contain introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and notes on troubleshooting and avoiding known pitfalls. Authoritative and accessible, Kinase Inhibitors: Methods and Protocols aims to provide scientists with modern and relevant methods to accelerate or strengthen their research and drug discovery programs through the utilization of these vital regulators.
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Includes bibliographical references and index.

Measuring the activity of leucine-rich repeat kinase 2: A kinase involved in Parkinson's disease -- Measuring PI3K lipid kinase activity -- A fluorescence polarization assay for the discovery of inhibitors of the polo-box domain of polo-like kinase 1 -- Assessment of hepatotoxicity potential of drug candidate molecules including kinase inhibitors by hepatocyte imaging assay technology and bile flux imaging assay technology -- Kinase inhibitor selectivity profiling using differential scanning fluorimetry -- Chemoproteomic characterization of protein kinase inhibitors using immobilized ATP -- Proteome-wide identification of staurosporine-binding kinases using capture compound mass spectrometry -- Affinity purification of proteins binding to kinase inhibitors immobilized on self-assembling monolayers -- Kinase inhibitor profiling using chemoproteomics -- Covalent cross-linking of kinases with their corresponding peptide substrates -- Receptor tyrosine kinase inhibitor profiling using bead-based multiplex sandwich immunoassays -- Monitoring phosphoproteomic response to targeted kinase inhibitors using reverse-phase protein microarrays -- Measuring phosphorylation-specific changes in response to kinase inhibitors in mammalian cells using quantitative proteomics -- Investigation of acquired resistance to EGFR-targeted therapies in lung cancer using cDNA microarrays.

Protein and lipid kinases are often the master regulators of cell signaling in eukaryotic systems. The human genome codes for more than 500 of these enzymes and their misregulation has been shown to be involved in the onset and progression of many diseases including cancer and inflammation. Therefore, small molecule kinase inhibitors have become important research tools for the elucidation of the many biological roles of kinases and their mechanisms of action. Kinase inhibitors thus also contribute significantly to the drug pipelines of the pharmaceutical and biotechnology industries and to the growing need to treat cancer and inflammation. In Kinase Inhibitors: Methods and Protocols, experts in kinase biology, drug discovery, and clinical research present a series of exemplary methods that can be used to address the many challenges facing scientists in the discovery and development of kinase inhibitors both for research and clinical use. Written in the highly successful Methods in Molecular Biology series format, chapters contain introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and notes on troubleshooting and avoiding known pitfalls. Authoritative and accessible, Kinase Inhibitors: Methods and Protocols aims to provide scientists with modern and relevant methods to accelerate or strengthen their research and drug discovery programs through the utilization of these vital regulators.

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