Abstract:

Imaging probes for G-protein coupled receptors (GPCRs) would tremendously facilitate and push forward the understanding of the underlying mechanism of pathologies of the central and peripheral nervous system. Still, such imaging probes are highly underrepresented in biomedical applications due to their certain restrains caused by lack of specificity and selectivity. My group strives to develop and optimize affinity and subtype specificity of G-protein coupled receptor ligands. The main focus is on muscarinic acetylcholine receptors and the build-up of an extensive ligand library. The combination of conventional chemical screening methods with radiolabelling of the lead compounds enables significant insights into functional and molecular pathways. Following the 3R concept of animal testing and to reduce the time of the development process in preclinical research, I recently developed a dynamic column-based 3D cell culture method facilitating and fastening the screening process of ligand libraries. Besides the application as efficient diagnosis tool, we aim for highly selective imaging probes blazing the trail to personalized therapeutics for the steady increasing dementia pathologies. The transition of the hit compounds from bench to bedside is especially pillared by my strong involvement in clinical trials targeting GPCRs within the dopaminergic and serotonergic system.

This presentation will focus on development strategies including the design, synthesis and radiolabelling of new candidates/lead compounds. Furthermore, the talk will summarize the preclinical evaluation and establishment of new methods on the path into clinics of ligands targeting GPCRs for biomedical application.

• Dr. Verena Pichler, Medical University of Vienna, Department of Biomedical Imaging and Image-guided Therapy (Division of Nuclear Medicine)
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