Plettenburg Group
The Plettenburg group focusses on the development of new chemical probes with different modes of detection, targeted delivery and the design of novel inhibitors.
The Plettenburg group focusses on the development of new chemical probes with different modes of detection, targeted delivery and the design of novel inhibitors.
Research Topics
Medicinal Chemistry
A systemic exposure of bioactive substances can result in a variety of adverse effects. The specific delivery of drugs into specific cell types is therefore a powerful strategy to enhance biological activity, keeping the required drug amount low and to circumvent adverse effects resulting of uptake into different cells. Therefore, the Plettenburg group focusses on the development of cell specific ligands and the conjugation with drugs thereof.
The design of novel inhibitors for enzymes or protein-protein interactions is another core element in the research of the group. Besides classical medicinal chemistry approaches like hit optimization of hits from primary screens based on synthetic or natural product libraries also new fragment based approaches are investigated.
The optimization is done in a multi parametric fashion, taking biological activity as well as physicochemical (e.g. chemical stability, solubility) and eADME properties (e. g. cytotoxicity, plasma stability, plasma protein binding, off-target interactions) into account in order to create new lead structures.
Publications
Napolitano, V. ; Mroz, P. ; Marciniak, M. ; Kalel, V.C. ; Softley, C. ; Janna Olmos, J.D. ; Tippler, B.G. ; Schorpp, K.K. ; Rioton, S. ; Fröhlich, T. ; Plettenburg, O. ; Hadian, K. ; Erdmann, R. ; Sattler, M. ; Popowicz, G.M. ; Dawidowski, M. ; Dubin, G.
Structure-based design, synthesis and evaluation of a novel family of PEX5-PEX14 interaction inhibitors against Trypanosoma.Sekar, R. ; Motzler, K. ; Kwon, Y. ; Novikoff, A. ; Jülg, J. ; Najafi, B. ; Wang, S. ; Seitz, S. ; Hass, D, ; Gancheva, S. ; Kahl, S. ; Yang, B. ; Finan, B. ; Schwarz, K. ; Okun, J.G. ; Roden, M. ; Blüher, M. ; Müller, T.D. ; Krahmer, N. ; Behrends, C. ; Plettenburg, O. ; Miaczynska, M. ; Herzig, S. ; Zeigerer, A.
Vps37a regulates hepatic glucose production by controlling glucagon receptor localization to endosomes.Liu, N. ; O'Connor, P. ; Gujrati, V. ; Anzenhofer,P. ; Klemm, U. ; Kleigrewe, K. ; Sattler, M. ; Plettenburg, O. ; Ntziachristos, V.
Multifunctional croconaine nanoparticles for efficient optoacoustic imaging of deep tumors and photothermal therapy.Yin, H. ; Karayel, O. ; Chao, Y.Y. ; Seeholzer, T. ; Hamp, I. ; Plettenburg, O. ; Gehring, T. ; Zielinski, C. ; Mann, M. ; Krappmann, D.
A20 and ABIN-1 cooperate in balancing CBM complex-triggered NF-κB signaling in activated T cells.Napolitano, V. ; Dabrowska, A. ; Schorpp, K.K. ; Mourao, A. ; Barreto-Duran, E. ; Benedyk, M. ; Botwina, P. ; Brandner, S. ; Bostock, M.J. ; Chykunova, Y. ; Czarna, A. ; Dubin, G. ; Fröhlich, T. ; Hölscher, M. ; Jedrysik, M. ; Matsuda, A. ; Owczarek, K. ; Pachota, M. ; Plettenburg, O. ; Potempa, J.S. ; Rothenaigner, I. ; Schlauderer, F. ; Slysz, K. ; Szczepanski, A. ; Greve-Isdahl Mohn, K. ; Blomberg, B. ; Sattler, M. ; Hadian, K. ; Popowicz, G.M. ; Pyrc, K.
Acriflavine, a clinically approved drug, inhibits SARS-CoV-2 and other betacoronaviruses.Plettenburg, O.
Drug discovery in academia.Liu, N. ; O'Connor, P. ; Gujrati, V. ; Gorpas, D. ; Glasl, S. ; Blutke, A. ; Walch, A.K. ; Kleigrewe, K. ; Sattler, M. ; Plettenburg, O. ; Ntziachristos, V.
Facile synthesis of a croconaine-based nanoformulation for optoacoustic imaging and photothermal therapy.Gerckens, M. ; Schorpp, K.K. ; Pelizza, F. ; Wögrath, M. ; Reichau, K. ; Ma, H. ; Dworsky, A.-M. ; Sengupta, A. ; Stoleriu, M.-G. ; Heinzelmann, K. ; Merl-Pham, J. ; Irmler, M. ; Alsafadi, H.N. ; Trenkenschuh, E. ; Sarnova, L. ; Jirouskova, M. ; Frieß, W. ; Hauck, S.M. ; Beckers, J. ; Kneidinger, N. ; Behr, J. ; Hilgendorff, A. ; Hadian, K. ; Lindner, M. ; Königshoff, M. ; Eickelberg, O. ; Gregor, M. ; Plettenburg, O. ; Yildirim, A.Ö. ; Burgstaller, G.
Phenotypic drug screening in a human fibrosis model identified a novel class of antifibrotic therapeutics.Fino, R. ; Lenhart, D. ; Kalel, V.C. ; Softley, C. ; Napolitano, V. ; Byrne, R. ; Schliebs, W. ; Dawidowski, M. ; Erdmann, R. ; Sattler, M. ; Schneider, G. ; Plettenburg, O. ; Popowicz, G.M.
Computer-aided design and synthesis of a new class of PEX14 inhibitors: substituted 2,3,4,5-tetrahydrobenzo[F][1,4]oxazepines as potential new trypanocidal agents.Hamp, I. ; O'Neill, T.J. ; Plettenburg, O. ; Krappmann, D.
A patent review of MALT1 inhibitors (2013-present).Rai, A. ; Klare, J.P. ; Reinke, P.Y.A. ; Englmaier, F. ; Fohrer, J. ; Fedorov, R. ; Taft, M.H. ; Chizhov, I. ; Curth, U. ; Plettenburg, O. ; Manstein, D.J.
Structural and biochemical characterization of a dye-decolorizing peroxidase from Dictyostelium discoideum.Hofmeister, A. ; Jahn-Hofmann, K. ; Brunner, B. ; Helms, M.W. ; Metz-Weidmann, C. ; Krack, A. ; Kurz, M. ; Li, Z. ; Weitzenberg, M.M. ; Pflimlin, E. ; Plettenburg, O. ; Scheidler, S.
Syntheses of morpholine-based nucleotide analogs for hepatic siRNA targeting and stabilization.Liu, N. ; O'Connor, P. ; Gujrati, V. ; Gorpas, D. ; Glasl, S. ; Blutke, A. ; Walch, A.K. ; Kleigrewe, K. ; Sattler, M. ; Plettenburg, O. ; Ntziachristos, V.
Facile synthesis of a croconaine-based nanoformulation for optoacoustic imaging and photothermal therapy.Ansarullah ; Jain, C. ; Far, F.F. ; Homberg, S. ; Wißmiller, K. ; von Hahn, F. ; Raducanu, A. ; Schirge, S. ; Sterr, M. ; Bilekova, S. ; Siehler, J. ; Wiener, J. ; Oppenländer, L. ; Morshedi, A. ; Bastidas-Ponce, A. ; Collden, G. ; Irmler, M. ; Beckers, J. ; Feuchtinger, A. ; Grzybek, M. ; Ahlbrecht, C. ; Feederle, R. ; Plettenburg, O. ; Müller, T.D. ; Meier, M. ; Tschöp, M.H. ; Coskun, Ü. ; Lickert, H.
Author Correction: Inceptor counteracts insulin signalling in β-cells to control glycaemia.Eriksson, O. ; Velikyan, I. ; Haack, T. ; Bossart, M. ; Evers, A. ; Lorenz, K. ; Laitinen, I. ; Larsen, P.J. ; Plettenburg, O. ; Johansson, L. ; Pierrou, S. ; Wagner, M.
Drug occupancy assessment at the glucose-dependent insulinotropic polypeptide (GIP) receptor by positron emission tomography.Ansarullah ; Jain, C. ; Far, F.F. ; Homberg, S. ; Wissmiller, K. ; Gräfin von Hahn, F. ; Raducanu, A. ; Schirge, S. ; Sterr, M. ; Bilekova, S. ; Siehler, J. ; Wiener, J. ; Oppenländer, L. ; Morshedi, A. ; Bastidas-Ponce, A. ; Collden, G. ; Irmler, M. ; Beckers, J. ; Feuchtinger, A. ; Grzybek, M. ; Ahlbrecht, C. ; Feederle, R. ; Plettenburg, O. ; Müller, T.D. ; Meier, M. ; Tschöp, M.H. ; Coskun, Ü. ; Lickert, H.
Inceptor counteracts insulin signalling in β-cells to control glycaemia.Hartleben, G. ; Schorpp, K.K. ; Kwon, Y. ; Betz, B. ; Tsokanos, F.-F. ; Dantes, Z. ; Schäfer, A. ; Rothenaigner, I. ; Monroy Kuhn, J.M. ; Morigny, P. ; Mehr, L. ; Lin, S. ; Seitz, S. ; Tokarz, J. ; Artati, A. ; Adamski, J. ; Plettenburg, O. ; Lutter, D. ; Irmler, M. ; Beckers, J. ; Reichert, M. ; Hadian, K. ; Zeigerer, A. ; Herzig, S. ; Berriel Diaz, M.
Combination therapies induce cancer cell death through the integrated stress response and disturbed pyrimidine metabolism.Contact
