期刊
ANNUAL REVIEW OF BIOCHEMISTRY, VOL 88
卷 88, 期 -, 页码 383-408出版社
ANNUAL REVIEWS
DOI: 10.1146/annurev-biochem-062917-012837
关键词
cellular thermal shift assay; quantitative proteomics; target engagement; mechanistic biomarkers; drug development; protein interaction state
The cellular thermal shift assay (CETSA) is a biophysical technique allowing direct studies of ligand binding to proteins in cells and tissues. The proteome-wide implementation of CETSA with mass spectrometry detection (MS-CETSA) has now been successfully applied to discover targets for orphan clinical drugs and hits from phenotypic screens, to identify offtargets, and to explain poly-pharmacology and drug toxicity. Highly sensitive multidimensional MS-CETSA implementations can now also access binding of physiological ligands to proteins, such as metabolites, nucleic acids, and other proteins. MS-CETSA can thereby provide comprehensive information on modulations of protein interaction states in cellular processes, including downstream effects of drugs and transitions between different physiological cell states. Such horizontal information on ligand modulation in cells is largely orthogonal to vertical information on the levels of different proteins and therefore opens novel opportunities to understand operational aspects of cellular proteomes.
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