P7 - Synthesis and evaluation of PSMA-targeted imaging reagents

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A major focus of our research is the development of PSMA-guided reagents for prostate cancer imaging. In a first line of research, we develop and synthesize ligands of low molecular weight for PSMA with improved pharmacokinetics for applications in MRI, PET, SPECT and fluorescence imaging (joint project with CURADEL, Prof. John V. Frangioni ). We focus on phosphinate and urea derivatives, which are evaluated with non-radioactive cell-assays (collaboration with Department of Physics, Prof. W. Parak ). An often neglected part of many imaging reagents is the tracer moiety. Particularly for targeting ligands of small molecular weight, the tracer contributes significantly to the overall pharmacokinetic properties of the whole imaging reagent. For metal-based imaging methods, the metal tracer is typically complexed by a chelator. In a second line of research, we develop novel chelators with improved pharmacokinetics for transition metal tracers such as Gd, Eu, Zr and others. In close cooperation with DESY and the Department of Physics, Prof. Florian Grüner tracers of low molecular weight for X-ray fluorescence imaging are developed.

  • Solution Structure and Relaxivity of Ln-DOTXAZA Derivatives. Holzapfel M., Baldau T., Kerpa S., Guadalupi, G. Qi B., Liu Y., Parak W. J., Maison W., Eur. J. Inorg. Chem. 2022. Published online, doi:10.1002/ejic.202200432

    Nonradioactive Cell Assay for the Evaluation of Modular Prostate-Specific Membrane Antigen Targeting Ligands via Inductively Coupled Plasma Mass Spectrometry. Holzapfel M, Mutas M, Chandralingam S, von Salisch C, Peric N, Segelke T, Fischer M, Chakraborty I, Parak WJ, Frangioni JV, Maison W.J Med Chem. 2019 Dec 12;62(23):10912-10918. doi: 10.1021/acs.jmedchem.9b01606. Epub 2019 Nov 26.PMID: 31714783

    X-ray Fluorescence Uptake Measurement of Functionalized Gold Nanoparticles in Tumor Cell Microsamples. Schmutzler O, Graf S, Behm N, Mansour WY, Blumendorf F, Staufer T, Körnig C, Salah D, Kang Y, Peters JN, Liu Y, Feliu N, Parak WJ, Burkhardt A, Gargioni E, Gennis S, Chandralingam S, Höeg F, Maison W, Rothkamm K, Schulz F, Grüner F.Int J Mol Sci. 2021 Apr 1;22(7):3691. doi: 10.3390/ijms22073691.PMID: 33916283