Radiotracer and Drug Development

Research of this group is devoted to the chemical and radiochemical development of novel radiotracers for extracellular and intracellular targets playing an important role for cancer, such as transglutaminase-2, cyclooxygenase-2 and cathepsin B. For this purpose, we hold expertise in the synthesis and in vitro evaluation of novel biologically active molecules to select the most promising compounds for further developments as well as the synthesis of precursor molecules suitable for radiolabeling. This comprises the application of the entire methodological repertoire of organic chemistry and radiochemistry. Furthermore, biochemical methods are used to study target binding and to obtain insight into the pharmacokinetic properties of potential tracer compounds. Our key competence and peculiar interest is the radiolabeling with the positron emitting nuclides fluorine-18, carbon-11 and other radionuclides including the optimization of radiosyntheses and upscaling to fully automated and remotely controlled procedures allowing for handling of high amounts of activity. In this regard we are interested in the development of novel radiotracers and innovative (radio)synthetic strategies to set the radiochemical basis for successful tracer development.

Key publications

• Laube M. et al., RSC Advances 10:38601-38611, 2020.
• Laube M. et al., Molecules 24:3807, 2019.
• Wodtke R. et al., J. Med. Chem. 61:4528-4560, 2018. (Front Cover, Volume 61, Issue 10)
• Kuchar M. et al., Front. Chem. 6:121, 2018.
• Löser R. et al., Amino Acids 51:219-244, 2019.

Projects (multicenter)

• Development of an Iodine-123-labeled radioligand for functional characterization of transglutaminase 2 in pancreatic cancer; European Regional Development Fund (ERDF, in German: EFRE) 

Research initiatives

• RIVAD: Radiation-Induced Vascular Dysfunction
• Theranostic Targeting of Cyclooxygenase-2 (COX-2): ⇒ open Special Issue in Molecules (MDPI)

Further literature on our hypotheses and approaches

• ref. targeting transglutaminase-2: [1]
• ref. targeting cyclooxygenase-2: [2], [3], [4], [5] 
• ref. targeting cathepsins: [6]
• ref. nitric oxide donors: [7] & Suppl. Cover