Kinase Screening and Profiling Methods and Protocols 1st Edition by Hicham Zegzouti ISBN 1493930737 9781493930739

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ISBN 10: 1493930737 
ISBN 13: 9781493930739
Author: Hicham Zegzouti

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.

Kinase Screening and Profiling Methods and Protocols 1st Table of contents:

1. Introduction to Kinases and Their Role in Disease

• 1.1 What Are Protein Kinases?

• 1.2 Kinases in Cell Signaling

• 1.3 Kinase Dysregulation in Disease

• 1.4 The Importance of Kinase Inhibitors in Drug Development

2. Kinase Assay Formats

• 2.1 In Vitro Kinase Assays

• 2.2 Radiometric Assays

• 2.3 Fluorescence-Based Assays

• 2.4 Enzyme-Linked Immunosorbent Assay (ELISA)

• 2.5 Homogeneous and Heterogeneous Assays

• 2.6 Selecting the Right Assay for Your Kinase

3. Kinase Screening and Profiling Techniques

• 3.1 High-Throughput Screening (HTS) of Kinase Inhibitors

• 3.2 Kinase Selectivity Profiling

• 3.3 Target Engagement Assays

• 3.4 Comparative Profiling Across Kinase Families

• 3.5 Challenges in Kinase Profiling: Specificity and Sensitivity

4. Small-Molecule Kinase Inhibitors and Their Mechanisms

• 4.1 Mechanisms of Kinase Inhibition

• 4.2 Reversible vs. Irreversible Inhibitors

• 4.3 Allosteric vs. ATP-Competitive Inhibitors

• 4.4 Chemical Libraries for Kinase Inhibition

• 4.5 Case Studies of Small-Molecule Kinase Inhibitors

5. Protein Kinase Profiling: Experimental Protocols

• 5.1 In Vitro Kinase Profiling Protocols

• 5.2 Cell-Based Kinase Profiling Methods

• 5.3 Phosphorylation Profiling in Cells

• 5.4 Kinase Substrate Profiling

• 5.5 Mass Spectrometry in Kinase Profiling

6. Screening Technologies for Kinase Activity

• 6.1 Fluorescence Polarization (FP) Assays

• 6.2 Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET)

• 6.3 Surface Plasmon Resonance (SPR) for Kinase Interaction Studies

• 6.4 Label-Free Screening Approaches

• 6.5 Microscale Thermophoresis (MST) and Kinase Screening

7. Kinase Inhibitor Discovery and Optimization

• 7.1 Hit Identification in Kinase Screening

• 7.2 Hit-to-Lead and Lead Optimization

• 7.3 Structure-Activity Relationship (SAR) Studies

• 7.4 In Silico Prediction and Modeling of Kinase Inhibitors

• 7.5 Kinase Inhibitor Development Pipeline

8. Kinase Assay Automation and Data Analysis

• 8.1 Automation in Kinase Assays

• 8.2 Data Management in High-Throughput Screening

• 8.3 Data Analysis Tools for Kinase Profiling

• 8.4 Statistical Methods for Kinase Screening

• 8.5 Quality Control and Validation in Kinase Assays

9. Kinase Profiling in Drug Development

• 9.1 Kinase Profiling in Early Drug Discovery

• 9.2 Assessing Kinase Inhibition in Clinical Trials

• 9.3 Kinase-Based Biomarkers in Drug Development

• 9.4 Kinase Inhibitors in Cancer Therapy

• 9.5 Future Directions in Kinase Targeted Therapy

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Tags: Hicham Zegzouti, Kinase Screening, Profiling Methods