Kinase Screening and Profiling, 1st ed. 2016 Methods and Protocols Methods in Molecular Biology Series, Vol. 1360

This volume focuses on screening and profiling kinase inhibitors or activators. Chapters in this book cover several facets of the drug discovery processes starting with target identification, and assay development and screening chemical libraries for hit identification and lead optimization. The profiling portion of Kinase Screening and Profiling: Methods and Protocols discusses several strategies and techniques that are required to minimize off target hits and reduce cellular toxicities that are caused by liability kinases. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls.

Timely and authoritative, Kinase Screening and Profiling: Methods and Protocols, will benefit scientists and researchers who are interested in exploring the role of kinases in academic, as well as pharmaceutical research.

HTRF Kinase Assay Development and Methods in Inhibitor Characterization.- Application of Eukaryotic Elongation Factor-2 Kinase (eEF-2K) for Cancer Therapy: Expression, Purification, and High-Throughput Inhibitor Screening.- Recombinant Kinase Production and Fragment Screening by NMR Spectroscopy.- Bioluminescence Methods for Assaying Kinases in Quantitative High-Throughput Screening (qHTS) Format Applied to Yes1 Tyrosine Kinase, Glucokinase and PI5P4Kα Lipid Kinase.- Using Bioluminescent Kinase Profiling Strips to Identify Kinase Inhibitor Selectivity and Promiscuity.- Measuring Activity of Phosphoinositide Lipid Kinases Using a Bioluminescent ADP-Detecting Assay.- A High-Throughput Radiometric Kinase Assay.- A High Content Assay to Screen for Modulators of EGFR Function.- Monitoring Protein Kinase Expression and Phosphorylation in Cell Lysates with Antibody Microarrays.- From Enzyme to Whole Blood: Sequential Screening Procedure for Identification and Evaluation of p38 MAPK Inhibitors.- Genetically Encoded Fluorescent Indicators to Visualize Protein Phosphorylation in Living Cells.- Characterization of an Engineered Src Kinase to Study Src Signaling and Biology.- Screening One-Bead-One-Compound Peptide Libraries for Optimal Kinase Substrates.- Determination of the Substrate Specificity of Protein Kinases with Peptide Micro- and Macroarrays.- Rapid Identification of Protein Kinase Phosphorylation Site Motifs Using Combinatorial Peptide Libraries.