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Author:   Andrew G. Stephen ,  Dominic Esposito
Publisher:   Springer-Verlag New York Inc.
Imprint:   Springer-Verlag New York Inc.
Edition:   1st ed. 2024
Volume:   2797
ISBN:  

9781071638217

ISBN 10:   1071638211
Pages:   365
Publication Date:   04 April 2024
Audience:   Professional and scholarly ,  Professional & Vocational
Format:   Hardback
Publisher's Status:   Active
Availability:   Not yet available  
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Table of Contents

KRAS as a therapeutic target.- The abundance of KRAS and RAS gene mutations in cancer.- Production of isotopically labeled KRAS4b.- Nucleotide Exchange on RAS Proteins using Hydrolysable and Non-Hydrolysable Nucleotides.- Crystallographic studies of KRAS in Complex with Small Molecules and RAS-binding Proteins.- Considerations around Structure-Based Drug Discovery for KRAS using DOCK.- Measurement of KRAS GTPase activity.- Affinity Measurement of Non-covalent Interactions of the covalent KRAS G12C GDP inhibitor MRTX849 to RAS Isoforms using Surface Plasmon Resonance.- 1D and 2D NMR for KRAS:ligand binding.- Luminescence based techniques for KRAS thermal stability monitoring.- MALDI-TOF mass spectrometry-based assay for measuring covalent target engagement of KRAS G12C inhibitors.- KRAS4b:RAF-1 Homogenous Time-Resolved Fluorescence Resonance Energy Transfer Assay for Drug Discovery.- Biophysical characterization of RAS-SOS Complexes by Native Mass Spectrometry.- Profiling complex RAS-effector interactions using NMR spectroscopy.- Probing RAS Function Using Monobody and NanoBiT Technologies.- Analysis of the guanine nucleotide-bound state of KRAS by ion-pair reversed-phase high-performance liquid chromatography.- Real-time monitoring of RAS activity using in vitro and in-cell NMR spectroscopy.- Studying RAS Interactions in live cells with BRET.- FLIM-FRET Protein-Protein Interaction Assay.- High-throughput cell-based screening of small molecule KRAS signaling inhibitors using a homogeneous time resolved fluorescence (HTRF) assay.- A method to conditionally measure target engagement at intracellular RAS and RAF complexes.- FLAG-KRAS4B as a model system for KRAS4B proteoform and PTM evaluation by mass spectrometry .- Creation of an isogenic H/N/KRAS-less mouse embryonic fibroblast cell line panel derived from a size sorted diploid clone.- Quality Control ofan Isogenic H/N/KRAS-less Mouse Embryonic Fibroblast Cell Line Panel.- A Facile Method to Append a Bio-ID Tag to Endogenous Mutant Kras Alleles.

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