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Kinase Inhibitors

Methods and Protocols

Series: Methods in Molecular Biology

by Bernhard Kuster

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Main description:

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 (TM) 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.

Contents:

1. Targeting Cancer with Small Molecular Weight Kinase Inhibitors

Doriano Fabbro, Sandra W. Cowan-Jacob, Henrik Moebitz, and Georg Martiny-Baron

2. Small Molecule Protein and Lipid Kinase Inhibitors in Inflammation and Specific Models for their Evaluation

Matthias Gaestel and Alexey Kotlyarov

3. Measuring the Activity of Leucine Rich Repeat Kinase 2 (LRRK2) - A Kinase Involved in Parkinson's Disease

Byoung Dae Lee, Xiaojie Li, Ted M. Dawson, and Valina L. Dawson

4. Measuring PI3K Lipid Kinase Activity

Elisa Ciraolo, Alessia Perino, and Emilio Hirsch

5. A Fluorescence Polarization Assay for the Discovery of Inhibitors of the Polo-box Domain of Polo-like Kinase 1

Wolfgang Reindl, Klaus Strebhardt, and Thorsten Berg

6. Assessment of Hepatotoxicity Potential of Drug Candidate Molecules Including Kinase Inhibitors by Hepatocyte Imaging Assay Technology and Bile Flux Imaging Assay Technology

Jinghai J. Xu, Margaret C. Dunn, Arthur R. Smith, and Eric S. Tien

7. Kinase Inhibitor Selectivity Profiling using Differential Scanning Fluorimetry

Oleg Fedorov, Frank H. Niesen, and Stefan Knapp

8. Chemoproteomic Characterization of Protein Kinase Inhibitors using Immobilized ATP

James S. Duncan, Timothy A.J. Haystead, and David W. Litchfield

9. Proteome-wide identification of staurosporine-binding kinases using Capture Compound Mass Spectrometry

Jenny J. Fischer, Olivia Y. Graebner nee Baessler, and Mathias Dreger

10. Affinity Purification of Proteins Binding to Kinase Inhibitors Immobilised on Self Assembling Monolayers

Marcus Bantscheff, Scott Hobson, and Bernhard Kuster

11. Kinase Inhibitor Profiling using Chemoproteomics

Markus Schirle, Eugene C. Petrella, Scott M. Brittain, David Schwalb, Edmund Harrington, Ivan Cornella-Taracido, and John A. Tallarico

12. Covalent Crosslinking of Kinases with Their Corresponding Peptide Substrates

Alexander V. Statsuk and Kevan M. Shokat

13. Receptor Tyrosine Kinase Inhibitor Profiling using Bead-based Multiplex Sandwich Immunoassays

Oliver Poetz, Nicole Schneiderhan-Marra, Tanja Henzler, Thomas Herget, and Thomas O. Joos

14. Monitoring Phosphoproteomic Response To Targeted Kinase Inhibitors Using Reverse-Phase Protein Microarrays

Gabriela Lavezzari and Mark R. Lackner

15. Measuring Phosphorylation Specific Changes in Response to Kinase Inhibitors in Mammalian Cells Using Quantitative Proteomics

Nurhan OEzlu , Marc Kirchner, and Judith Jebanathirajah Steen

16. Investigation of Acquired Resistance to EGFR-Targeted Therapies in Lung Cancer Using cDNA Microarrays

Kian Kani, Rafaella Sordella, and Parag Mallick

PRODUCT DETAILS

ISBN-13: 9781617793363
Publisher: Springer (Humana Press Inc.)
Publication date: September, 2011
Pages: 267
Weight: 707g
Availability: Available
Subcategories: Anatomy, Pharmacology

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