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Combinatorial screening for specific drug solubilizers with switchable release profiles.

作者信息

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

机构信息

Laboratory for Organic Synthesis of Functional Systems, Department of Chemistry, Humboldt-Universität zu Berlin, Brook-Taylor-Str. 2, D-12489, Berlin, Germany.

出版信息

Macromol Biosci. 2015 Jan;15(1):82-9. doi: 10.1002/mabi.201400443. Epub 2014 Dec 29.

Abstract

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.

摘要

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