Volume 15, Issue 1 pp. 82-89
Communication

Combinatorial Screening for Specific Drug Solubilizers with Switchable Release Profiles

Sebastian Wieczorek

Sebastian Wieczorek

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

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Sara Vigne

Sara Vigne

École Polytechnique Fédérale de Lausanne (EPFL), Institute of Materials (IMX), EPFL – STI – IMX – LMOM, MXG 037, Station 12, CH-1015 Lausanne, Switzerland

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Tiziana Masini

Tiziana Masini

Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, NL-9747 AG Groningen, The Netherlands

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Daniela Ponader

Daniela Ponader

Max Planck Institute of Colloids and Interfaces, MPI KGF Golm, D-14424 Potsdam, Germany

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Laura Hartmann

Laura Hartmann

Max Planck Institute of Colloids and Interfaces, MPI KGF Golm, D-14424 Potsdam, Germany

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Anna K. H. Hirsch

Anna K. H. Hirsch

Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, NL-9747 AG Groningen, The Netherlands

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Hans G. Börner

Corresponding Author

Hans G. Börner

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

Correspondence to: Prof. H. G. Börner

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First published: 29 December 2014
Citations: 11

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.mabi201400443-gra-0001

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