Proteome-wide drug and metabolite interaction mapping by thermal-stability profiling.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 26389571.
- Also identified by DOI 10.1038/nmeth.3590 and PMC identifier 4629415.
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Abstract
Thermal stabilization of proteins after ligand binding provides an efficient means to assess the binding of small molecules to proteins. We show here that in combination with quantitative mass spectrometry, the approach allows for the systematic survey of protein engagement by cellular metabolites and drugs. We profiled the targets of the drugs methotrexate and (S)-crizotinib and the metabolite 2'3'-cGAMP in intact cells and identified the 2'3'-cGAMP cognate transmembrane receptor STING, involved in immune signaling.
Medical subject headings
- Proteome
- Pyrazoles
- Pyridines