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Successful Design of a Multivalent Bifunctional Chelator for Diagnostic 64Cu PET Imaging in Alzheimer’s Disease

preprint
submitted on 04.06.2020 and posted on 05.06.2020 by Hong-Jun Cho, Truc T. Huynh, Buck E. Rogers, Liviu M. Mirica
Herein, we report to the best of our knowledge the first 64Cu PET imaging agent that shows appreciable in vivo brain uptake and exhibits high specific affinity for beta-amyloid (Aβ) aggregates, leading to the successful PET imaging of amyloid plaques in the brains of 5xFAD mice versus those of WT mice. The employed approach uses a bifunctional chelator with two Aβ-interacting fragments that dramatically improves the Aβ-binding affinity and lipophilicity for favorable BBB penetration, while the use of optimized-length spacers between the Cu-chelating group and the Aβ-interacting fragments further improves the in vivo Aβ-binding specificity and brain uptake of the corresponding 64Cu PET imaging agent.

Funding

NIH R01GM114588

History

Email Address of Submitting Author

mirica@illinois.edu

Institution

University of Illinois at Urbana-Champaign

Country

USA

ORCID For Submitting Author

0000-0003-0584-9508

Declaration of Conflict of Interest

No conflict of interest

Version Notes

version 1.0

Exports