1. Academic Validation
  2. Poly(Ethylene glycol)-based backbones with high peptide loading capacities

Poly(Ethylene glycol)-based backbones with high peptide loading capacities

  • Molecules. 2014 Oct 30;19(11):17559-77. doi: 10.3390/molecules191117559.
Aoife O'Connor 1 Jean-Noel Marsat 2 Annachiara Mitrugno 3 Tom Flahive 4 Niamh Moran 5 David Brayden 6 Marc Devocelle 7
Affiliations

Affiliations

  • 1 Department of Pharmaceutical and Medicinal Chemistry, Centre for Synthesis and Chemical Biology, Royal College of Surgeons in Ireland, 123 St Stephen's Green, Dublin 2, Ireland. [email protected].
  • 2 Department of Pharmaceutical and Medicinal Chemistry, Centre for Synthesis and Chemical Biology, Royal College of Surgeons in Ireland, 123 St Stephen's Green, Dublin 2, Ireland. [email protected].
  • 3 Department of Molecular and Cellular Therapeutics, Royal College of Surgeons in Ireland, 123 St Stephen's Green, Dublin 2, Ireland. [email protected].
  • 4 Department of Pharmaceutical and Medicinal Chemistry, Centre for Synthesis and Chemical Biology, Royal College of Surgeons in Ireland, 123 St Stephen's Green, Dublin 2, Ireland. [email protected].
  • 5 Department of Molecular and Cellular Therapeutics, Royal College of Surgeons in Ireland, 123 St Stephen's Green, Dublin 2, Ireland. [email protected].
  • 6 UCD School of Veterinary Medicine and UCD Conway Institute, University College Dublin, Belfield, Dublin 4, Ireland. [email protected].
  • 7 Department of Pharmaceutical and Medicinal Chemistry, Centre for Synthesis and Chemical Biology, Royal College of Surgeons in Ireland, 123 St Stephen's Green, Dublin 2, Ireland. [email protected].
Abstract

Polymer-peptide conjugates are a promising class of compounds, where Polymers can be used to overcome some of the limitations associated with Peptides intended for therapeutic and/or diagnostic applications. Linear Polymers such as poly(ethylene glycol) can be conjugated through terminal moieties and have therefore limited loading capacities. In this research, functionalised linear poly(ethylene glycol)s are utilised for peptide conjugation, to increase their potential loading capacities. These poly(ethylene glycol) derivatives are conjugated to peptide sequences containing representative side-chain functionalised Amino acids, using different conjugation chemistries, including copper-catalysed azide-alkyne cycloaddition, amide coupling and thiol-ene reactions. Conjugation of a sequence containing the RGD motif to poly(allyl glycidyl ether) by the thiol-ene reaction, provided a conjugate which could be used in platelet adhesion studies.

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