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Keywords:

  • bioorganic chemistry;
  • dihydrofolate reductase;
  • fluorescent probes;
  • methotrexate;
  • proteins
Thumbnail image of graphical abstract

The labeling of proteins in living cells with fluorescent substituents is critical to the study of cell biology. A ligand–receptor approach based on the interaction between dihydrofolate reductase (DHFR) and methotrexate (Mtx) serves as a general method for labeling proteins with fluorescent or otherwise functional small molecules in vivo (see figure).