Data di Pubblicazione:
2018
Citazione:
MS methods to study macromolecule-ligand interaction : applications in drug discovery / F. Riccardi Sirtori, A. Altomare, M. Carini, G. Aldini, L. Regazzoni. - In: METHODS. - ISSN 1046-2023. - 144(2018), pp. 152-174.
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.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Drug discovery; Ligand; Macromolecule interaction; Mass spectrometry; Molecular Biology; Biochemistry, Genetics and Molecular Biology (all)
Elenco autori:
F. Riccardi Sirtori, A. Altomare, M. Carini, G. Aldini, L. Regazzoni
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