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Combinatorial screening for specific drug solubilizers with switchable release profiles

Wieczorek, S., Vigne, S., Masini, T., Ponader, D., Hartmann, L., Hirsch, A. K. H. & Börner, H. G., Jan-2015, In : Macromolecular Bioscience. 15, 1, p. 82-89 8 p.

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  • Combinatorial screening for specific drug solubilizers with switchable release

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DOI

  • Sebastian Wieczorek
  • Sara Vigne
  • Tiziana Masini
  • Daniela Ponader
  • Laura Hartmann
  • Anna K H Hirsch
  • Hans G Börner

Polymer-block-peptide conjugates are tailored to render hydrophobic small molecule drugs water soluble. The combinatorial strategy selects for bioconjugates that exhibit sequence-specific solubilization and switchable release profiles of the cargo through incorporation of a disulfide linker moiety into the peptide-library design. While the study focused on the photosensitizer m-THPC and reductive carrier cleavage, the approach is generic and might be expanded toward a broad range of poorly soluble small-molecule drugs and other selective cleavage mechanisms to disassemble a peptide binding domain of the bioconjugate-based solubilizer.

Original languageEnglish
Pages (from-to)82-89
Number of pages8
JournalMacromolecular Bioscience
Volume15
Issue number1
Publication statusPublished - Jan-2015

ID: 22829706