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.
New dyes and probes as chemical tolls for biological imaging are a specific focus of the Plettenburg group.
Besides molecules for novel detection methods like photoacoustic imaging, also molecules are developed for use as contrast agents, switchable dyes and biosensors for specific metabolites.
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.
New dyes and probes as chemical tolls for biological imaging are a specific focus of the Plettenburg group.
Besides molecules for novel detection methods like photoacoustic imaging, also molecules are developed for use as contrast agents, switchable dyes and biosensors for specific metabolites.
Team
Publications
Weiterlesen2022 Wissenschaftlicher Artikel in European Journal of Medicinal Chemistry
Structure-based design, synthesis and evaluation of a novel family of PEX5-PEX14 interaction inhibitors against Trypanosoma.
2022 Wissenschaftlicher Artikel in Cell Metabolism
Vps37a regulates hepatic glucose production by controlling glucagon receptor localization to endosomes.
2022 Wissenschaftlicher Artikel in Nanophotonics
Multifunctional croconaine nanoparticles for efficient optoacoustic imaging of deep tumors and photothermal therapy.
2022 Wissenschaftlicher Artikel in Cellular and Molecular Life Sciences - CMLS
A20 and ABIN-1 cooperate in balancing CBM complex-triggered NF-κB signaling in activated T cells.
2022 Wissenschaftlicher Artikel in Cell Chemical Biology
Acriflavine, a clinically approved drug, inhibits SARS-CoV-2 and other betacoronaviruses.
2021 Wissenschaftlicher Artikel in Science Advances
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
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
A patent review of MALT1 inhibitors (2013-present).
2021 Wissenschaftlicher Artikel in International Journal of Molecular Sciences
Structural and biochemical characterization of a dye-decolorizing peroxidase from Dictyostelium discoideum.
2021 Wissenschaftlicher Artikel in Journal of Medicinal Chemistry
Syntheses of morpholine-based nucleotide analogs for hepatic siRNA targeting and stabilization.
2021 Wissenschaftlicher Artikel in Advanced healthcare materials
Facile synthesis of a croconaine-based nanoformulation for optoacoustic imaging and photothermal therapy.
2021 Nature
Author Correction: Inceptor counteracts insulin signalling in β-cells to control glycaemia.
2021 Wissenschaftlicher Artikel in Diabetes
Drug occupancy assessment at the glucose-dependent insulinotropic polypeptide (GIP) receptor by positron emission tomography.
