Combinatorial Screening for Specific Drug Solubilizers with Switchable Release Profiles
Sebastian Wieczorek
Laboratory for Organic Synthesis of Functional Systems, Department of Chemistry, Humboldt-Universität zu Berlin, Brook-Taylor-Str. 2, D-12489 Berlin, Germany
Search for more papers by this authorSara Vigne
École Polytechnique Fédérale de Lausanne (EPFL), Institute of Materials (IMX), EPFL – STI – IMX – LMOM, MXG 037, Station 12, CH-1015 Lausanne, Switzerland
Search for more papers by this authorTiziana Masini
Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, NL-9747 AG Groningen, The Netherlands
Search for more papers by this authorDaniela Ponader
Max Planck Institute of Colloids and Interfaces, MPI KGF Golm, D-14424 Potsdam, Germany
Search for more papers by this authorLaura Hartmann
Max Planck Institute of Colloids and Interfaces, MPI KGF Golm, D-14424 Potsdam, Germany
Search for more papers by this authorAnna K. H. Hirsch
Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, NL-9747 AG Groningen, The Netherlands
Search for more papers by this authorCorresponding Author
Hans G. Börner
- [email protected]
- | Fax: +49 (0)30 2093-7500
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
Search for more papers by this authorSebastian Wieczorek
Laboratory for Organic Synthesis of Functional Systems, Department of Chemistry, Humboldt-Universität zu Berlin, Brook-Taylor-Str. 2, D-12489 Berlin, Germany
Search for more papers by this authorSara Vigne
École Polytechnique Fédérale de Lausanne (EPFL), Institute of Materials (IMX), EPFL – STI – IMX – LMOM, MXG 037, Station 12, CH-1015 Lausanne, Switzerland
Search for more papers by this authorTiziana Masini
Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, NL-9747 AG Groningen, The Netherlands
Search for more papers by this authorDaniela Ponader
Max Planck Institute of Colloids and Interfaces, MPI KGF Golm, D-14424 Potsdam, Germany
Search for more papers by this authorLaura Hartmann
Max Planck Institute of Colloids and Interfaces, MPI KGF Golm, D-14424 Potsdam, Germany
Search for more papers by this authorAnna K. H. Hirsch
Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, NL-9747 AG Groningen, The Netherlands
Search for more papers by this authorCorresponding Author
Hans G. Börner
- [email protected]
- | Fax: +49 (0)30 2093-7500
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
Search for more papers by this authorAbstract
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.
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