Cysteine-functional polymers via thiol-ene conjugation

Macromol Rapid Commun. 2015 Mar;36(5):472-6. doi: 10.1002/marc.201400703. Epub 2015 Jan 21.

Abstract

A thiofunctional thiazolidine is introduced as a new low-molar-mass building block for the introduction of cysteine residues via a thiol-ene reaction. Allyl-functional polyglycidol (PG) is used as a model polymer to demonstrate polymer-analogue functionalization through reaction with the unsaturated side-chains. A modified trinitrobenzenesulfonic acid (TNBSA) assay is used for the redox-insensitive quantification and a precise final cysteine content can be predetermined at the polymerization stage. Native chemical ligation at cysteine-functional PG is performed as a model reaction for a chemoselective peptide modification of this polymer. The three-step synthesis of the thiofunctional thiazolidine reactant, together with the standard thiol-ene coupling and the robust quantification assay, broadens the toolbox for thiol-ene chemistry and offers a generic and straightforward approach to cysteine-functional materials.

Keywords: chemoselectivity; conjugated polymers; functionalization of polymers; protecting groups; thiol-ene chemistry.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allyl Compounds / chemistry
  • Cysteine / chemistry*
  • Oxidation-Reduction
  • Peptide Fragments / chemistry*
  • Polymerization
  • Polymers / chemistry*
  • Propylene Glycols / chemistry
  • Sulfhydryl Compounds / chemistry*
  • Surface Properties
  • Trinitrobenzenesulfonic Acid / chemistry

Substances

  • Allyl Compounds
  • Peptide Fragments
  • Polymers
  • Propylene Glycols
  • Sulfhydryl Compounds
  • polyglycidol
  • Trinitrobenzenesulfonic Acid
  • Cysteine