Publications Repository - Helmholtz-Zentrum Dresden-Rossendorf

1 Publication

Development of nuclear and optical dual-labelled agents for cancer imaging

Stephan, H.


For the past decade, nuclear and optical dual-labelled imaging agents have attracted enormous attention. Applied to cancer imaging, tumours can be tracked down by nuclear techniques such as single-photon emission tomography (SPECT) and positron emission tomography (PET), and subsequently resected using image-guided surgery with the appropriate fluorophores. Moreover, the high spatial resolution of fluorescence imaging permits the elucidation of cell-biological events and thereby gaining a deeper insight into in vitro and in vivo processes. The development of dual imaging probes can be achieved using sophisticated low-molecular compounds that combine moieties for the desired imaging modalities, e.g. dyes for fluorescence optical imaging, and appropriate bifunctional chelator agents (BFCAs) for radiometals enabling SPECT or PET. We have developed BFCAs based on bis(2-pyridylmethyl)-1,4,7-triazacyclononane (DMPTACN) and 3,7-diazabicyclo[3.3.1]nonane (bispidine) that rapidly form stable 64CuII complexes under mild conditions. These BFCAs are well-suited for in vivo application in cancer imaging. Since they are also relatively easy to functionalize with multiple modalities, they are ideal chelators for the design of targeted dual-labelled imaging agents (PET, fluorescence imaging). Moreover, these chelating agents can be easily grafted on the surface of nanomaterials that are equipped with a multitude of different functionalities, such as targeting units, solubility enhancer and fluorescent tags. Hence, higher sensitivity can be achieved compared to small molecules, and there is an almost infinite variability regarding the surface functionalization.
Examples of target-specific peptides and bio(nano)materials equipped with DMPTACN/bispidine ligands for labelling with 64Cu as an ideal positron emitter are discussed. This enables tumour imaging and the biodistribution of materials can be studied over a period of days via positron emission tomography (PET). The additional introduction of fluorescence labels allows for optical imaging with high spatial resolution, and offers the possibility to visualize cellular processes by fluorescence microscopy.

  • Lecture (Conference)
    Seventh International Conference on Radiation in Various Fields of Research, 10.-14.06.2019, Herceg Novi, Montenegro


Years: 2023 2022 2021 2020 2019 2018 2017 2016 2015