Site-Specific Polymer Conjugation Stabilizes Therapeutic Enzymes in the Gastrointestinal Tract

Adv Mater. 2016 Feb 17;28(7):1455-60. doi: 10.1002/adma.201504797. Epub 2015 Dec 7.

Abstract

The site-specific conjugation of polymers to multiple engineered cysteine residues of a prolyl endopeptidase leads to its stabilization in the gastrointestinal tract of rats, without compromising the activity relative to the native enzyme. The importance of polymer attachment sites is investigated, as well as the significance of polymer structure.

Keywords: gastrointestinal stability; poly(ethylene glycol); site-specific polymer conjugation, therapeutic enzymes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • Catalytic Domain
  • Endopeptidases / chemistry*
  • Endopeptidases / metabolism*
  • Endopeptidases / therapeutic use
  • Enzyme Stability
  • Gastrointestinal Tract / metabolism*
  • Models, Molecular
  • Myxococcus xanthus / enzymology
  • Polyethylene Glycols / chemistry*
  • Rats

Substances

  • Polyethylene Glycols
  • Endopeptidases