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PET Imaging of T Cells: Target Identification and Feasibility Assessment

Auberson, Yves, Briard, Emmanuelle, Rudolph, Bettina, Kaupmann, Klemens, Smith, Paul and Oberhauser, Berndt (2018) PET Imaging of T Cells: Target Identification and Feasibility Assessment. ChemMedChem. ISSN 18607187


Imaging Tcells using positron emission tomography (PET) would be highly useful for diagnosis and monitoring in immunology and oncology patients. There are, however, no obvious targets that can be used to develop imaging agents for this purpose. We evaluated several potential target proteins with selective expression in Tcells, and for which lead molecules were available: protein kinaseC isozymeθ (PKCθ), lymphocyte-specific protein tyrosine kinase (Lck), zeta-chain-associated protein kinase70 (ZAP70), and interleukin-2-inducible T-cell kinase (Itk). Ultimately, we focused on Itk and identified a tool molecule with properties suitable for in vivo imaging of Tcells: (5aR)-5,5-difluoro-5a-methyl-N-(1-((S)-3-(methylsulfonyl)phenyl)(tetrahydro-2H-pyran-4-yl)methyl)-1H-pyrazol-4-yl)-1,4,4a,5,5a,6-hexahydrocyclopropa[f]indazole-3-carboxamide (23). Although it does not have the optimal profile for clinical use, this molecule indicates that it might be possible to develop Itk-selective PET ligands for imaging the distribution of Tcells in patients.

Item Type: Article
Keywords: Imaging agents Immunology Kinases Ligand design Radiochemistry
Date Deposited: 22 Aug 2018 00:45
Last Modified: 22 Aug 2018 00:45


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