Sequence-defined oligo(ethanamino) amides

As delivery systems with high chemical precision and flexibility, we use sequence-defined cationic oligomers. Artificial oligoamino acids containing the PEI-like aminoethylene motif are assembled on solid-phase to sequence-defined oligo(ethanamino) amides.

Until now over 1400 different oligomers with different architectures have been generated and utilized for the delivery of nucleic acids, proteins, natural products, or drugs.

Selected publications

• Schaffert, D., Badgujar, N., Wagner, E. (2011) Novel Fmoc-Polyamino Acids for Solid-Phase Synthesis of Defined Polyamidoamines, Org Lett. 2011 Apr 1;13(7):1586-9
• Schaffert, D., Troiber, C., Salcher, E., Fröhlich, T., Martin,I., Badgujar, N., Dohmen, C., Edinger, D., Kläger, R., Maiwald, G., Farkasova, K., Seeber, S., Jahn-Hofmann, K., Hadwiger, P., Wagner, E. (2011) Solid-phase synthesis of sequence-defined T-, i-, and U-shape polymers for pDNA and siRNA delivery, Angew Chem Int Ed Engl. 2011 Sep 12;50(38):8986-9
• Dohmen, C., Edinger, D., Froehlich, T., Schreiner, L., Laechelt, U., Troiber, C., Rädler, J., Hadwiger, P., Vornlocher, H. P., Wagner, E. (2012) Nano Sized Multifunctional Polyplexes for Receptor Mediated SIRNA Delivery, ACS Nano. 2012 Jun 26;6(6):5198-208
• Zhang, P., He, D., Klein, P., Liu, X., Röder, R., Döblinger, M., Wagner, E.(2015) Enhanced Intracellular Protein Transduction by Sequence Defined Tetra-Oleoyl Oligoaminoamides Targeted for Cancer Therapy, Adv. Funct. Materials. 2015 Nov 11; 25:6627–6636
• Lee, D.J., Kessel, E., Edinger, D., He, D., Klein, P.M., Voith von Voithenberg, L., Lamb, D.C., Lächelt, U., Lehto, T., Wagner, E. (2016) Dual antitumoral potency of EG5 siRNA nanoplexes armed with cytotoxic bifunctional glutamyl-methotrexate targeting ligand, Biomaterials. 2016 Jan;77:98-110
• Lee, D.J., Kessel, E., Lehto, T., Liu, X., Yoshinaga, N., Padari, K., Chen, Y.-C., Kempter, S., Uchida, S., Rädler, J.O., Pooga, M., Sheu, M.-T., Kataoka, K., Wagner, E. (2017) Systemic Delivery of Folate-PEG siRNA Lipopolyplexes with Enhanced Intracellular Stability for In Vivo Gene Silencing in Leukemia, Bioconjug Chem. 2017 Sep 20;28(9):2393-2409
• Krhac Levacic, A., Morys, S., Kempter, S., Lächelt, U., Wagner, E. (2017) Minicircle Versus Plasmid DNA Delivery by Receptor-Targeted Polyplexes, Hum Gene Ther. 2017 Oct;28(10):862-874
• Röder, R., Helma, J., Preiß, T., Rädler, J.O., Leonhardt, H., Wagner, E. (2017) Intracellular Delivery of Nanobodies for Imaging of Target Proteins in Live Cells, Pharm Res. 2017 Jan;34(1):161-174
• Klein, P.M., Kern, S., Lee, D.J., Schmaus, J., Höhn, M., Gorges, J., Kazmaier, U., Wagner, E. (2018) Folate receptor-directed orthogonal click-functionalization of siRNA lipopolyplexes for tumor cell killing in vivo, Biomaterials. 2018 Sep;178:630-642
• Reinhard, S., Wang, Y., Dengler, S., Wagner, E. (2018) Precise enzymatic cleavage sites for improved bioactivity of siRNA lipo-polyplexes, Bioconjug Chem. 2018 Nov 21;29(11):3649-3657
• Truebenbach, I., Kern, S., Loy, D.M., Hoehn, M., Gorges, J., Kazmaier, U., Wagner E. (2019) Combination chemotherapy of L1210 tumors in mice with pretubulysin and methotrexate nanoparticles, Mol. Pharmaceutics 2019, 16, 2405−2417.
• Luo, J., Höhn, M., Reinhard, S., Loy, D.M., Klein, P.M., Wagner, E. (2019) IL4-receptor-targeted dual antitumoral apoptotic peptide - siRNA conjugate lipoplexes. Adv. Funct. Materials 25: 1900697. https://doi.org/10.1002/adfm.201900697
• Truebenbach, I., Zhang, W., Wang, Y., Kern, S., Höhn, M., Reinhard, S., Gorges, J., Kazmaier, U., Wagner, E. (2019) Co-delivery of pretubulysin and siEG5 to EGFR overexpressing carcinoma cells. Int J Pharm 2019, 569: 118570.