Radiometal-based bioconjugates

Our research focus is on the in-depth biological characterization and pharmacological evaluation of novel radiopharmaceuticals based on small molecules, peptides and antibody derivatives. Hereby, the individual building blocks (e.g. radiometals, chelators) as well as the conjugates as a whole are analyzed in depth regarding their in vitro stability, their effects on cell signaling and health as well as their multifaceted interactions with biomolecules and cells. Our fundamental aim is to understand the biology of such materials and to shed light on involved molecular mechanisms and use the knowledge gained for rationally improving their design in that respect. Building up on these studies, we are also working on precise engineering and tailoring of different kinds of bioconjugates for their application as diagnostic tools and therapeutic agents.

Range of methods (excerpt)

• Heterologous protein expression
• Protein purification (Affinity chromatography, Size exclusion chromatography)
• Protein characterization (SDS-PAGE, Western Blot, MALDI-TOF MS)
• Protein modification and functionalization (site-specific & classic)
• Radiolabeling of small molecules, peptides and protein derivatives (radio-thin layer chromatography, autoradiography, stability assessment, ligand challenge studies)
• Analysis of cell binding, uptake, localization, signaling, toxicity (flow cytometry, fluorescence microscopy, saturation and competitive binding, internalization, etc.)
• Matrix Assisted Laser Desorption Ionization - Time of Flight Mass Spectrometry (MALDI-TOF-MS)

Cover Gallery

Inside Back Cover

Falco Reissig, Kristof Zarschler, Zbynek Novy, Milos Petrik, Katerina Bendova, Daniela Kurfurstova, Jan Bouchal, Marie-Charlotte Ludik, Florian Brandt, Klaus Kopka, Marta Khoylou, Hans-Jürgen Pietzsch, Marian Hajduch, Constantin Mamat

Modulating the pharmacokinetic profile of Actinium-225-labeled macropa-derived radioconjugates by dual targeting of PSMA and albumin.

Theranostics 2022,12(17), 7203-7215

Cover Picture

Falco Reissig, Kristof Zarschler, René Hübner, Hans Jürgen Pietzsch, Klaus Kopka, Constantin Mamat

Sub 10 ‐ nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy.

ChemistryOpen 2020, 9 (8), 793-889.

Cover Picture

Kritee Pant, Christin Neuber, Kristof Zarschler, Johanna Wodtke, Sebastian Meister, Rainer Haag, Jens Pietzsch, Holger Stephan

Active Targeting of Dendritic Polyglycerols for Diagnostic Cancer Imaging.

Small 2020, 16 (7), 1905013.

Cover Feature

Garima Singh, Kristof Zarschler, Sebastian Hunoldt, Irma Ivette Santana Martínez, Carmen L. Ruehl, Madlen Matterna, Ralf Bergmann, Domokos Máthé, Nikolett Hegedüs, Michael Bachmann, Peter Comba, Holger Stephan

Versatile Bispidine Based Bifunctional Chelators for 64CuII‐Labelling of Biomolecules.

Chem. Eur. J. 2020, 26 (9), 1890-2001.

Inside Cover

Anne Nsubuga, Kristof Zarschler, Massimo Sgarzi, Bim Graham, Holger Stephan

Towards Utilising Photocrosslinking of Polydiacetylenes for the Preparation of “Stealth” Upconverting Nanoparticles.

Angew. Chem. Int. Ed. 2018, 57 (49), 16036-16040.

Back Cover

Anne Nsubuga, Massimo Sgarzi, Kristof Zarschler, Manja Kubeil, René Hübner, Robin Steudtner, Bim Graham, Tanmaya Joshi, Holger Stephan

Facile preparation of multifunctionalisable ‘stealth’ upconverting nanoparticles for biomedical applications.

Dalton Trans. 2018, 47 (26), 8595-8604.

Front Cover

Malay Patra, Kristof Zarschler, Hans-Jürgen Pietzsch, Holger Stephan, Gilles Gasser

New insights into the pretargeting approach to image and treat tumours.

Chem Soc Rev. 2016, 45 (23), 6415-6431.

Front Cover

Karina Pombo García, Kristof Zarschler, Lisa Barbaro, José A. Barreto, William O'Malley, Leone Spiccia, Holger Stephan, Bim Graham

Zwitterionic-Coated “Stealth” Nanoparticles for Biomedical Applications: Recent Advances in Countering Biomolecular Corona Formation and Uptake by the Mononuclear Phagocyte System.

Small 2014, 10(13), 2516-29.