Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
8340011 | Methods | 2018 | 23 Pages |
Abstract
The interaction of small compounds (i.e. ligands) with macromolecules or macromolecule assemblies (i.e. targets) is the mechanism of action of most of the drugs available today. Mass spectrometry is a popular technique for the interrogation of macromolecule-ligand interactions and therefore is also widely used in drug discovery and development. Thanks to its versatility, mass spectrometry is used for multiple purposes such as biomarker screening, identification of the mechanism of action, ligand structure optimization or toxicity assessment. The evolution and automation of the instruments now allows the development of high throughput methods with high sensitivity and a minimized false discovery rate. Herein, all these approaches are described with a focus on the methods for studying macromolecule-ligand interaction aimed at defining the structure-activity relationships of drug candidates, along with their mechanism of action, metabolism and toxicity.
Keywords
HSADDSNSIMTSABPsITRAQHR-MSTOFMOAADCSCysHRFITCACEADMETDARTSESIHTSABPPSECIM-MSFTICRTPPdrug affinity responsive target stabilitynuclear magnetic resonanceCYPsMS/MSAdeninehuman serum albuminaffinity capillary electrophoresisCapillary electrophoresisHICisobaric tags for relative and absolute quantitationFourier transformNMRSurface plasmon resonanceSPRCollision activated dissociationthymineDissociation constantHIShydroxyl radical footprintingFourier transform ion cyclotron resonancecircular dichroismtime of flightcytosineCysteineDrug delivery systemSILACCADIon mobility mass spectrometryMass spectrometryHigh resolution mass spectrometryTandem mass spectrometryhigh throughput screeningactivity-based protein profilingLysineLYSligandmatrix assisted laser desorption ionizationMALDIMechanism of actionstable isotope labeling by amino acids in cell culturehistidineActivity-based probesIsothermal titration calorimetrySize exclusion chromatographyhydrophobic interaction chromatographyliquid chromatographyHigh pressure liquid chromatographyHPLCDrug discoveryantibody drug conjugatesGuanineelectrospray ionizationNanoelectrospray ionization
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Authors
Federico Riccardi Sirtori, Alessandra Altomare, Marina Carini, Giancarlo Aldini, Luca Regazzoni,