Coupling to Polymeric Scaffolds Stabilizes Biofunctional Peptides for Intracellular Applications

@article{Ruttekolk2011CouplingTP,
  title={Coupling to Polymeric Scaffolds Stabilizes Biofunctional Peptides for Intracellular Applications},
  author={Ivo R. Ruttekolk and A. Chakrabarti and Martin Richter and Falk Duchardt and Heike Glauner and W. P. Verdurmen and J. Rademann and R. Brock},
  journal={Molecular Pharmacology},
  year={2011},
  volume={79},
  pages={692 - 700}
}
Here, we demonstrate that coupling to N-hydroxypropyl methacrylamide (HPMA) copolymer greatly enhances the activity of apoptosis-inducing peptides inside cells. Peptides corresponding to the BH3 domain of Bid were coupled to a thioester-activated HPMA (28.5 kDa) via native chemical ligation in a simple one-pot synthesis. Peptides and polymer conjugates were introduced into cells either by electroporation or by conjugation to the cell-penetrating peptide nona-arginine. The molecular basis of the… Expand
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