Selective Radical Trifluoromethylation of Native Residues in Proteins

J Am Chem Soc. 2018 Feb 7;140(5):1568-1571. doi: 10.1021/jacs.7b10230. Epub 2018 Jan 22.

Abstract

The incorporation of fluorine can not only significantly facilitate the study of proteins but also potentially modulate their function. Though some biosynthetic methods allow global residue-replacement, post-translational fluorine incorporation would constitute a fast and efficient alternative. Here, we reveal a mild method for direct protein radical trifluoromethylation at native residues as a strategy for symmetric-multifluorine incorporation on mg scales with high recoveries. High selectivity toward tryptophan residues enhanced the utility of this direct trifluoromethylation technique allowing ready study of fluorinated protein constructs using 19F-NMR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Free Radicals / chemical synthesis
  • Free Radicals / chemistry
  • Hemeproteins / chemistry*
  • Horses
  • Hydrocarbons, Fluorinated / chemical synthesis*
  • Hydrocarbons, Fluorinated / chemistry
  • Molecular Structure
  • Myoglobin / chemistry*
  • Tryptophan / chemistry*

Substances

  • Free Radicals
  • Hemeproteins
  • Hydrocarbons, Fluorinated
  • Myoglobin
  • Tryptophan