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Bioactive Peptide Brush Polymers via Photoinduced Reversible-Deactivation Radical Polymerization.

Hao SunWonmin ChoiNanzhi ZangClaudia BattistellaMatthew P ThompsonWei CaoXuhao ZhouChristopher FormanNathan C Gianneschi
Published in: Angewandte Chemie (International ed. in English) (2019)
Harnessing metal-free photoinduced reversible-deactivation radical polymerization (photo-RDRP) in organic and aqueous phases, we report a synthetic approach to enzyme-responsive and pro-apoptotic peptide brush polymers. Thermolysin-responsive peptide-based polymeric amphiphiles assembled into spherical micellar nanoparticles that undergo a morphology transition to worm-like micelles upon enzyme-triggered cleavage of coronal peptide sidechains. Moreover, pro-apoptotic polypeptide brushes show enhanced cell uptake over individual peptide chains of the same sequence, resulting in a significant increase in cytotoxicity to cancer cells. Critically, increased grafting density of pro-apoptotic peptides on brush polymers correlates with increased uptake efficiency and concurrently, cytotoxicity. The mild synthetic conditions afforded by photo-RDRP, make it possible to access well-defined peptide-based polymer bioconjugate structures with tunable bioactivity.
Keyphrases
  • anti inflammatory
  • cell death
  • cancer therapy
  • drug delivery
  • electron transfer
  • single cell
  • ionic liquid
  • bone marrow
  • energy transfer