Chemogenomics

This volume presents both theoretical guidance and protocols on chemogenomics including chemogenomics library assembly, compound profiling, and phenotypic assays. The chapters in this book cover topics such as the assembly and use of Kinase Chemogenomics; data mining for chemogenomic compound candidates; protocols for protein family-focused assay systems to profile chemogenomic compounds; functional and target engagement assays in cellular settings for broad characterization; and a discussion on phenotypic assays where chemogenomic sets may be applied. 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.
Cutting-edge and thorough, Chemogenomics: Methods and Protocols is a valuable resource for all researchers whoare interested in learning more about this diverse and developing field.

Includes cutting-edge methods and protocols Provides step-by-step detail essential for reproducible results Contains key notes and implementation advice from the experts

Contenu
An Introduction to Chemogenomics.- Developing a Kinase Chemogenomic Set: Facilitating Investigation into Kinase Biology by Linking Phenotypes to Targets.- Compilation of Custom Compound/Bioactivity Datasets from Public Repositories.- Quality Control of Chemogenomic Library using LC-MS.- Annotation of the Effect of Chemogenomic Compounds on Cell Health using High-Content Microscopy in Live-Cell Mode.- Characterization of Cellular Viability using Label-Free Brightfield Live-Cell Imaging.- Plate-Based Screening for DUB Inhibitors.- NanoBRET™ Live Cell Kinase Selectivity Profiling Adapted for High Throughput Screening.- A Fluorescence-Based Reporter Gene Assay to Characterize Nuclear Receptor Modulators.- Measuring Protein-Protein Interactions in Cells using NanoLuciferase Bioluminescence Resonance Energy Transfer (NanoBRET) Assay.- HiBiT Cellular Thermal Shift Assay (HiBiT CETSA).- Detection of Cellular Target Engagement for Small Molecule Modulators of Striatal-Enriched Protein Tyrosine Phosphatase (STEP).- Target Deconvolution by Limited Proteolysis Coupled to Mass Spectrometry.- Global Assessment of Drug Target Engagement and Selectivity of Covalent Cysteine-Reactive Inhibitors using Alkyne-Functionalized Probes.- 3D-Spheroid Invasion Assay for High-Throughput Screening of Small Molecule Libraries.- Live-Cell High-Throughput Screen for Monitoring Autophagy Flux.- Phenotypic Chemical Screening in CD4+ T Cells to Identify Epigenetic Inhibitors.