Combinatorial Screening for Specific Drug Solubilizers with Switchable Release Profiles

作者: Sebastian Wieczorek , Sara Vigne , Tiziana Masini , Daniela Ponader , Laura Hartmann

DOI: 10.1002/MABI.201400443

关键词: Combinatorial chemistryPeptideDrug deliveryLinkerBioconjugationPeptide bindingPhotosensitizerChemistrySmall moleculeMoiety

摘要: 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 a disulfide linker moiety into peptide-library design. While study focused on photosensitizer m-THPC reductive carrier cleavage, approach is generic might be expanded toward broad range poorly soluble small-molecule other selective cleavage mechanisms disassemble peptide binding domain bioconjugate-based solubilizer.

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