Work

Design of a multivalent bifunctional chelator for diagnostic 64 Cu PET imaging in Alzheimer’s disease

Year: 2020

Type: article

Abstract: Herein, we report to the best of our knowledge the first 64 Cu 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 64 Cu PET imaging agent.

Source: Proceedings of the National Academy of Sciences

DOI: 10.1073/pnas.2014058117

Authors: Hong-Jun Cho, Truc T. Huynh, Buck E. Rogers, Liviu M. Mirica

Institutions: University of Illinois Urbana-Champaign, Washington University in St. Louis, Hope Center for Neurological Disorders

Language: English

Topic: Radiopharmaceutical Chemistry and Applications

Subfield: Radiology, Nuclear Medicine and Imaging

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: green

Funders: National Institutes of Health, Charles F. and Joanne Knight Alzheimer Disease Research Center, Washington University in St. Louis, National Institute on Aging, National Institute of General Medical Sciences