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Combinatorial Screening for Specific Drug Solubilizers with Switchable Release Profiles
Author(s) -
Wieczorek Sebastian,
Vigne Sara,
Masini Tiziana,
Ponader Daniela,
Hartmann Laura,
Hirsch Anna K. H.,
Börner Hans G.
Publication year - 2015
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201400443
Subject(s) - bioconjugation , linker , chemistry , moiety , combinatorial chemistry , peptide , cleavage (geology) , photosensitizer , small molecule , conjugate , biophysics , stereochemistry , biochemistry , organic chemistry , fracture (geology) , computer science , biology , operating system , mathematical analysis , geotechnical engineering , mathematics , engineering
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.