Locally anchoring enzymes to tissues via extracellular glycan recognition

Nat Commun. 2018 Nov 22;9(1):4943. doi: 10.1038/s41467-018-07129-6.

Abstract

Success of enzymes as drugs requires that they persist within target tissues over therapeutically effective time frames. Here we report a general strategy to anchor enzymes at injection sites via fusion to galectin-3 (G3), a carbohydrate-binding protein. Fusing G3 to luciferase extended bioluminescence in subcutaneous tissue to ~7 days, whereas unmodified luciferase was undetectable within hours. Engineering G3-luciferase fusions to self-assemble into a trimeric architecture extended bioluminescence in subcutaneous tissue to 14 days, and intramuscularly to 3 days. The longer local half-life of the trimeric assembly was likely due to its higher carbohydrate-binding affinity compared to the monomeric fusion. G3 fusions and trimeric assemblies lacked extracellular signaling activity of wild-type G3 and did not accumulate in blood after subcutaneous injection, suggesting low potential for deleterious off-site effects. G3-mediated anchoring to common tissue glycans is expected to be broadly applicable for improving local pharmacokinetics of various existing and emerging enzyme drugs.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Extracellular Space / metabolism
  • Female
  • Galectin 3 / genetics
  • Galectin 3 / metabolism*
  • Humans
  • Injections, Subcutaneous
  • Jurkat Cells
  • Luciferases / genetics
  • Luciferases / metabolism*
  • Luminescent Measurements / methods
  • Mice, Inbred C57BL
  • Muscles / metabolism
  • Polysaccharides / metabolism*
  • Protein Binding
  • Recombinant Fusion Proteins / administration & dosage
  • Recombinant Fusion Proteins / metabolism*
  • Recombinant Fusion Proteins / pharmacokinetics
  • Subcutaneous Tissue / metabolism

Substances

  • Galectin 3
  • Polysaccharides
  • Recombinant Fusion Proteins
  • Luciferases