Oliver Plettenburg

Director

Career

Being always intrigued by bioorganic and medicinal chemistry and convinced that working at the interface of chemistry and biology had great chances for true innovation, I did start my scientific career in a major European pharmaceutical venture in 2001. I chose this career path, as I believed that this would open up a great environment to tackle pressing healthcare needs and actually bring new medications into the clinic, an assumption that turned out to be true. As a medicinal chemist I was responsible for progressing projects from very early phases (target discovery) through hit and lead optimization up to preclinical and ultimately clinical development. In this role I was deeply involved in target family approaches, particularly in the field of kinase research, also acting as local head of chemical biology kinases. As a project leader for various programs in the area of diabetes, oncology and cardiovascular diseases Fortunately, I was able to progress eight compounds to preclinical or clinical status. From 2010 I got more and more interested in exploring innovative approaches for improving success rates in drug discovery and exploration of potentially disruptive future medications, e.g. detoxifying compounds by specifically delivering compounds to the desired target organ or developing smart medicines being able to sense particular physiological conditions (like hypoglycemia) and then readily liberating compounds from a depot.

Albeit drug discovery in the pharmaceutical industry was a great experience, in 2016 I was offered the opportunity to return to academia and establish the newly founded Institute of Medicinal Chemistry at Helmholtz Munich. I realized that this would bring exiting opportunities to explore certain phenomena in greater detail than possible in an industrial setting and furthermore it would open up options to invest in highly innovative, with a chance to become game changers in treatment, which, however, may be regarded as too risky or too unconventional in a pharma setting. The institute is dedicated to the exploration mechanistic aspects of pathology and the discovery of new treatment options for different diseasessuch as diabetes (type 1 or type 2), immunological disorders or certain infectious diseases. I feel that being located in a competitive, highly interdisciplinary and interactive scientific infrastructure like being offered by Helmholtz Centre Munich provides an optimal environment to probe such innovative therapeutic concepts and to make significant contributions to public healthcare.

The aim of our research is to explore poorly understood biological processes and to make these accessible for therapeutic purposes. For this we optimize underexploited chemical substance classes according to modern medicinal chemistry criteria to create innovative chemical agents. We also aim at selectively delivering drug substances to the target organ and to develop smart systems that allow release of the free drug exactly at the time needed, thus effectively limiting drug side effects. Lastly, we want to develop tools to visualize the development of common diseases in tissues and living animals. This will on the one hand improve our understanding of disease pathogenesis and the value of individual disease models, on the other hand it will open up opportunities for a better characterization of defined early disease states and enable intervention at an early point in time, which is likely to improve therapeutic outcomes.

Fields of Work and Expertise

Medicinal ChemistryBiological ChemistryTargeted Delivery

CV

1997 - 2000

Ph.D. in Chemistry, University of Wuppertal, Germany

Topic: Synthesis of phosphorylated inositols and inositol derivatives

2000 – 2001

Postdoctoral stay with Prof. Wong Chi-Huey, Scripps Research Institute

Topic: Synthesis of a-galactosyl-ceramides to mediate a CD1 stimulated immune response

2001-2004

Research Scientist, Medicinial Chemistry, Aventis, Frankfurt

2005-2007

Research Scientist, TD Cardiovascular Diseases, Sanofi-Aventis, Frankfurt

2008-2010

Senior Research Scientist, TD Cardiovascular Diseases, Sanofi-Aventis, Frankfurt

2010-2012

Head of Chemical Biology, Sanofi, Frankfurt

2012-2016

Head of Biosensing und Chemical Probes, Sanofi, Frankfurt

2016 - today

Professor (W3) for Medicinal Chemistry at the Leibniz Universität Hannover; Director, Institute for Medicinal Chemistry, Helmholtz Munich

2008
Special Achievement Award, Sanofi-Aventis

2002
Milestone Award, Aventis

Publications

2022 Wissenschaftlicher Artikel in European Journal of Medicinal Chemistry

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.

2022 Wissenschaftlicher Artikel in Cell Metabolism

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.

2022 Wissenschaftlicher Artikel in Nanophotonics

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.

2022 Wissenschaftlicher Artikel in Cellular and Molecular Life Sciences - CMLS

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.

2022 Wissenschaftlicher Artikel in Cell Chemical Biology

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.

2021 Wissenschaftlicher Artikel in Science Advances

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.

2021 Wissenschaftlicher Artikel in Journal of Chemical Information and Modeling

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.

2021 Review in Expert Opinion on Therapeutic Patents

Hamp, I. ; O'Neill, T.J. ; Plettenburg, O. ; Krappmann, D.

A patent review of MALT1 inhibitors (2013-present).

2021 Wissenschaftlicher Artikel in International Journal of Molecular Sciences

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.

2021 Wissenschaftlicher Artikel in Journal of Medicinal Chemistry

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.

2021 Wissenschaftlicher Artikel in Advanced healthcare materials

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.

2021 Nature

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.

2021 Wissenschaftlicher Artikel in Diabetes

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.

2021 Wissenschaftlicher Artikel in Nature

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.

2021 Wissenschaftlicher Artikel in EMBO Molecular Medicine

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.

2020 Wissenschaftlicher Artikel in Journal of Medicinal Chemistry

Dawidowski, M. ; Kalel, V.C. ; Napolitano, V. ; Fino, R. ; Schorpp, K.K. ; Emmanouilidis, L. ; Lenhart, D. ; Ostertag, M.S. ; Kaiser, M. ; Kolonko, M. ; Tippler, B. ; Schliebs, W. ; Dubin, G. ; Mäser, P. ; Tetko, I.V. ; Hadian, K. ; Plettenburg, O. ; Erdmann, R. ; Sattler, M. ; Popowicz, G.M.

Structure-activity relationship in pyrazolo[4,3-c]pyridines, first inhibitors of PEX14-PEX5 Protein-Protein Interaction (PPI) with trypanocidal activity.

Prof. Dr. Oliver Plettenburg

Career

Fields of Work and Expertise

CV

Ph.D. in Chemistry, University of Wuppertal, Germany

Postdoctoral stay with Prof. Wong Chi-Huey, Scripps Research Institute

Research Scientist, Medicinial Chemistry, Aventis, Frankfurt

Research Scientist, TD Cardiovascular Diseases, Sanofi-Aventis, Frankfurt

Senior Research Scientist, TD Cardiovascular Diseases, Sanofi-Aventis, Frankfurt

Head of Chemical Biology, Sanofi, Frankfurt

Head of Biosensing und Chemical Probes, Sanofi, Frankfurt

Professor (W3) for Medicinal Chemistry at the Leibniz Universität Hannover; Director, Institute for Medicinal Chemistry, Helmholtz Munich

Honors and Awards

Publications

Structure-based design, synthesis and evaluation of a novel family of PEX5-PEX14 interaction inhibitors against Trypanosoma.

Vps37a regulates hepatic glucose production by controlling glucagon receptor localization to endosomes.

Multifunctional croconaine nanoparticles for efficient optoacoustic imaging of deep tumors and photothermal therapy.

A20 and ABIN-1 cooperate in balancing CBM complex-triggered NF-κB signaling in activated T cells.

Acriflavine, a clinically approved drug, inhibits SARS-CoV-2 and other betacoronaviruses.

Drug discovery in academia.

Facile synthesis of a croconaine-based nanoformulation for optoacoustic imaging and photothermal therapy.

Phenotypic drug screening in a human fibrosis model identified a novel class of antifibrotic therapeutics.

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.

A patent review of MALT1 inhibitors (2013-present).

Structural and biochemical characterization of a dye-decolorizing peroxidase from Dictyostelium discoideum.

Syntheses of morpholine-based nucleotide analogs for hepatic siRNA targeting and stabilization.

Facile synthesis of a croconaine-based nanoformulation for optoacoustic imaging and photothermal therapy.

Author Correction: Inceptor counteracts insulin signalling in β-cells to control glycaemia.

Drug occupancy assessment at the glucose-dependent insulinotropic polypeptide (GIP) receptor by positron emission tomography.

Inceptor counteracts insulin signalling in β-cells to control glycaemia.

Combination therapies induce cancer cell death through the integrated stress response and disturbed pyrimidine metabolism.

Structure-activity relationship in pyrazolo[4,3-c]pyridines, first inhibitors of PEX14-PEX5 Protein-Protein Interaction (PPI) with trypanocidal activity.

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