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Medicinal Chemistry and Drug Design

Oliver Plettenburg has been appointed Adjunct Faculty of the Institute for Lung Health, where he oversees the area of Medicinal Chemistry.

He studied chemistry at the University of Wuppertal and obtained his Ph.D. under the supervision of Prof. Hans-Josef Altenbach in 2000. He then moved to The Scripps Research Institute, La Jolla to work under the guidance of Prof. Chi-Huey Wong, where he focused on the synthesis of glycolipids. After this he joined the pharmaceutical industry at Aventis Pharma, working first in classical medicinal chemistry and developing projects from hit and lead optimization phase all the way to early clinical trials. Later he was more and more involved in establishing alternative concepts in pharmaceutical research, last he held positions as “Head of Chemical Biology” and “Head of Biosensors and Chemical Probes” at Sanofi-Aventis, Frankfurt, Germany.

From 2016, Prof. Plettenburg serves as founding director of the Institute of Medicinal Chemistry of the Helmholtz Zentrum München, he also is full professor for Medicinal Chemistry at Leibniz Universität Hannover. His research focuses on hit and lead optimization to open up new treatment options for severe diseases like diabetes, lung, inflammatory or infectious diseases. Furthermore, he develops innovative targeted and smart drug delivery methods and works on the synthesis of novel imaging agents for in-vivo monitoring of pathogenesis.

He is author of more than 85 publications in peer reviewed journals and inventor of 35 patents.

The Plettenburg lab is interested in providing contributions to the three main challenges of medicinal chemistry:

 

Finding new chemical matter for exciting new targets.

Availability of highly active, selective compounds is a key prerequisite for validating (or devalidating) conceptionally new target hypotheses. The design of novel inhibitors for enzymes or protein-protein interactions is a core element in the research of the group. Besides classical medicinal chemistry approaches like hit optimization of hits obtained from primary screens based on synthetic or natural product libraries, also fragment based approaches are investigated.

The optimization is performed in a multi parametric fashion, taking biological activity as well as physicochemical (e.g. chemical stability, solubility) and eADME properties (e. g. permeability, metabolic stability, cytotoxicity, plasma stability) into account in order to create new lead structures. We are striving to advance these leads to proof-of-concept compounds being effective in in vivo disease models, and ultimately to clinical development.

Development of targeted therapies.

Systemic exposure of bioactive substances can result in a variety of adverse effects, as only a fraction of the applied dose will ultimately end up in the target organ. The selective delivery of drugs into specific cell types is therefore a powerful strategy to enhance biological activity, keeping the required drug amount low and to minimize adverse effects resulting of uptake into different cells. Therefore, the Plettenburg group works on the development of cell specific ligands and their conjugation with drug molecules.

Probe Development

Lastly, we are convinced that more work needs to be invested in an improved understanding of the underlying causes of disease. In order to tackle these questions, we develop new probes to observe pathological changes in vitro, but also in in-vivo settings, using techniques like fluorescence, optoacoustics, MRI and PET. This will help us e.g. to determine the activity of selected enzymes in various disease states, to study the development of disease in longitudinal studies, to improve the knowledge on the translational value of certain animal models for the clinical situation and to possibly identify new, predictive biomarkers.

Contact

Prof. Dr. Oliver Plettenburg

Director, Institute of Medicinal Chemistry (IMC)

Helmholtz Zentrum München
German Research Center for Environmental Health (GmbH)

Institute of Organic Chemistry
Center for Biomolecular Drug Research (BMWZ)
Leibniz Universität

Schneiderberg 1b
D-30167 Hannover
Germany

Ph. +49 511 762 14297
e-mail: oliver.plettenburg@helmholtz-muenchen.de

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