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Kinase Inhibitors

Overview of attention for book
Cover of 'Kinase Inhibitors'

Table of Contents

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    Book Overview
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    Chapter 1 Targeting Cancer with Small-Molecular-Weight Kinase Inhibitors.
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    Chapter 2 Small-Molecule Protein and Lipid Kinase Inhibitors in Inflammation and Specific Models for Their Evaluation
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    Chapter 3 Measuring the Activity of Leucine-Rich Repeat Kinase 2: A Kinase Involved in Parkinson’s Disease
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    Chapter 4 Measuring PI3K Lipid Kinase Activity
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    Chapter 5 A Fluorescence Polarization Assay for the Discovery of Inhibitors of the Polo-Box Domain of Polo-Like Kinase 1
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    Chapter 6 Assessment of Hepatotoxicity Potential of Drug Candidate Molecules Including Kinase Inhibitors by Hepatocyte Imaging Assay Technology and Bile Flux Imaging Assay Technology
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    Chapter 7 Kinase Inhibitors
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    Chapter 8 Chemoproteomic characterization of protein kinase inhibitors using immobilized ATP.
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    Chapter 9 Proteome-Wide Identification of Staurosporine-Binding Kinases Using Capture Compound Mass Spectrometry
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    Chapter 10 Affinity Purification of Proteins Binding to Kinase Inhibitors Immobilized on Self-Assembling Monolayers
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    Chapter 11 Kinase Inhibitor Profiling Using Chemoproteomics
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    Chapter 12 Covalent cross-linking of kinases with their corresponding peptide substrates.
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    Chapter 13 Receptor Tyrosine Kinase Inhibitor Profiling Using Bead-Based Multiplex Sandwich Immunoassays
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    Chapter 14 Monitoring Phosphoproteomic Response to Targeted Kinase Inhibitors Using Reverse-Phase Protein Microarrays
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    Chapter 15 Measuring Phosphorylation-Specific Changes in Response to Kinase Inhibitors in Mammalian Cells Using Quantitative Proteomics
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    Chapter 16 Investigation of Acquired Resistance to EGFR-Targeted Therapies in Lung Cancer Using cDNA Microarrays
Attention for Chapter 7: Kinase Inhibitors
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About this Attention Score

  • Above-average Attention Score compared to outputs of the same age (57th percentile)
  • Good Attention Score compared to outputs of the same age and source (71st percentile)

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Citations

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Readers on

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54 Mendeley
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1 CiteULike
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Chapter title
Kinase Inhibitors
Chapter number 7
Book title
Kinase Inhibitors
Published in
Methods in molecular biology, January 2012
DOI 10.1007/978-1-61779-337-0_7
Pubmed ID
Book ISBNs
978-1-61779-336-3, 978-1-61779-337-0
Authors

Oleg Fedorov, Frank H. Niesen, Stefan Knapp

Abstract

Fast, robust, and inexpensive screening methods are the heart of drug discovery processes. Moreover, it is useful to have access to several established assay formats, for validation purposes. If a targeted protein is an enzyme, the logical and widely used approach is the direct measurement of the effect of the added ligands on its activity. A variety of enzymatic assay formats have been successfully applied for inhibitor screening of protein kinases. However, enzymatic assays require an active enzyme with a known substrate and often time-consuming assay optimization. Several alternative approaches have been recently developed that detect binding of ligands to proteins. This chapter overviews and provides the experimental protocol of the successful application of differential scanning fluorimetry (DSF) in our laboratory for fast and robust screening of medium-sized (<10,000) inhibitor libraries. DSF monitors the thermal stabilization of the native protein structure upon ligand binding. It allows selectivity profiling of any protein kinase without prior knowledge of either substrate or activity of the kinase under investigation. Comparative studies revealed that generated data is highly reproducible and correlates well with the results from other ligand binding methodologies, direct binding constants as well as enzymatic assays.

Twitter Demographics

The data shown below were collected from the profile of 1 tweeter who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 54 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Canada 3 6%
Estonia 1 2%
Unknown 50 93%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 14 26%
Researcher 10 19%
Student > Bachelor 6 11%
Student > Master 5 9%
Professor > Associate Professor 3 6%
Other 9 17%
Unknown 7 13%
Readers by discipline Count As %
Agricultural and Biological Sciences 16 30%
Biochemistry, Genetics and Molecular Biology 14 26%
Chemistry 10 19%
Chemical Engineering 1 2%
Psychology 1 2%
Other 3 6%
Unknown 9 17%

Attention Score in Context

This research output has an Altmetric Attention Score of 2. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 20 March 2012.
All research outputs
#1,811,400
of 3,626,596 outputs
Outputs from Methods in molecular biology
#571
of 2,355 outputs
Outputs of similar age
#26,161
of 73,055 outputs
Outputs of similar age from Methods in molecular biology
#15
of 53 outputs
Altmetric has tracked 3,626,596 research outputs across all sources so far. This one is in the 45th percentile – i.e., 45% of other outputs scored the same or lower than it.
So far Altmetric has tracked 2,355 research outputs from this source. They receive a mean Attention Score of 1.4. This one has gotten more attention than average, scoring higher than 70% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 73,055 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 57% of its contemporaries.
We're also able to compare this research output to 53 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 71% of its contemporaries.