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Kinase Screening and Profiling

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Cover of 'Kinase Screening and Profiling'

Table of Contents

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    Book Overview
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    Chapter 1 HTRF Kinase Assay Development and Methods in Inhibitor Characterization
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    Chapter 2 Application of Eukaryotic Elongation Factor-2 Kinase (eEF-2K) for Cancer Therapy: Expression, Purification, and High-Throughput Inhibitor Screening
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    Chapter 3 Recombinant Kinase Production and Fragment Screening by NMR Spectroscopy.
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    Chapter 4 Bioluminescence Methods for Assaying Kinases in Quantitative High-Throughput Screening (qHTS) Format Applied to Yes1 Tyrosine Kinase, Glucokinase, and PI5P4Kα Lipid Kinase
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    Chapter 5 Using Bioluminescent Kinase Profiling Strips to Identify Kinase Inhibitor Selectivity and Promiscuity
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    Chapter 6 Measuring Activity of Phosphoinositide Lipid Kinases Using a Bioluminescent ADP-Detecting Assay.
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    Chapter 7 A High-Throughput Radiometric Kinase Assay
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    Chapter 8 A High-Content Assay to Screen for Modulators of EGFR Function
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    Chapter 9 Monitoring Protein Kinase Expression and Phosphorylation in Cell Lysates with Antibody Microarrays
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    Chapter 10 From Enzyme to Whole Blood: Sequential Screening Procedure for Identification and Evaluation of p38 MAPK Inhibitors.
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    Chapter 11 Genetically Encoded Fluorescent Indicators to Visualize Protein Phosphorylation in Living Cells
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    Chapter 12 Characterization of an Engineered Src Kinase to Study Src Signaling and Biology
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    Chapter 13 Screening One-Bead-One-Compound Peptide Libraries for Optimal Kinase Substrates
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    Chapter 14 Determination of the Substrate Specificity of Protein Kinases with Peptide Micro- and Macroarrays
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    Chapter 15 Rapid Identification of Protein Kinase Phosphorylation Site Motifs Using Combinatorial Peptide Libraries
Attention for Chapter 8: A High-Content Assay to Screen for Modulators of EGFR Function
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Chapter title
A High-Content Assay to Screen for Modulators of EGFR Function
Chapter number 8
Book title
Kinase Screening and Profiling
Published in
Methods in molecular biology, January 2016
DOI 10.1007/978-1-4939-3073-9_8
Pubmed ID
Book ISBNs
978-1-4939-3072-2, 978-1-4939-3073-9
Authors

Christophe Antczak, Hakim Djaballah

Abstract

Cell-based assays have the potential and advantage to identify cell-permeable modulators of kinase function, and hence provide an alternative to the conventional enzymatic activity-driven discovery approaches that rely on purified recombinant kinase catalytic domains. Here, we describe a domain-based high-content biosensor approach to study endogenous EGFR activity whereby EGF-induced receptor activation, subsequent trafficking, and internalization are imaged and quantified using time-dependent granule formation in cells. This method can readily be used to search for EGFR modulators in both chemical and RNAi screening; with potential applicability to other receptor tyrosine kinases.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 9 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United States 1 11%
Unknown 8 89%

Demographic breakdown

Readers by professional status Count As %
Researcher 3 33%
Professor > Associate Professor 2 22%
Student > Ph. D. Student 1 11%
Other 1 11%
Unknown 2 22%
Readers by discipline Count As %
Agricultural and Biological Sciences 3 33%
Biochemistry, Genetics and Molecular Biology 2 22%
Pharmacology, Toxicology and Pharmaceutical Science 1 11%
Unknown 3 33%