Solid-Phase Synthesis of Sequence-Defined T-, i-, and U-Shape Polymers for pDNA and siRNA Delivery

Authors

  • Dr. David Schaffert,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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    • These authors contributed equally to this work.

  • Christina Troiber,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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    • These authors contributed equally to this work.

  • Eveline E. Salcher,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • Thomas Fröhlich,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • Irene Martin,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • Dr. Naresh Badgujar,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • Christian Dohmen,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • Daniel Edinger,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • Raphaela Kläger,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • Dr. Gelja Maiwald,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • Katarina Farkasova,

    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • Dr. Silke Seeber,

    1. Roche Kulmbach GmbH, Fritz Hornschuch-Strasse 9, 95386 Kulmbach (Germany)
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  • Dr. Kerstin Jahn-Hofmann,

    1. Roche Kulmbach GmbH, Fritz Hornschuch-Strasse 9, 95386 Kulmbach (Germany)
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  • Dr. Philipp Hadwiger,

    1. Roche Kulmbach GmbH, Fritz Hornschuch-Strasse 9, 95386 Kulmbach (Germany)
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  • Prof. Ernst Wagner

    Corresponding author
    1. Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
    • Pharmaceutical Biotechnology, Center for Nanoscience, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, 81377 Munich (Germany)
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  • This work was supported by the Cluster “Nanosystems Initiative Munich” and the Biotech Cluster m4 T12. I.M. was a visiting PhD student from IRB Barcelona.

Abstract

original image

Artificial oligo(ethylene amino) acids, together with selected natural amino acids and fatty acid modifications, have been used for the solid-phase-assisted synthesis of polymers with precise sequence, topology, and modifications (see picture). First proof-of-concept studies demonstrate the high potential of such polymers in pDNA and siRNA delivery. K=lysine, A=alanine.

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