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Publication : Design of a multivalent bifunctional chelator for diagnostic <sup>64</sup>Cu PET imaging in Alzheimer's disease.

First Author  Cho HJ Year  2020
Journal  Proc Natl Acad Sci U S A Volume  117
Issue  49 Pages  30928-30933
PubMed ID  33234563 Mgi Jnum  J:299200
Mgi Id  MGI:6479927 Doi  10.1073/pnas.2014058117
Citation  Cho HJ, et al. (2020) Design of a multivalent bifunctional chelator for diagnostic (64)Cu PET imaging in Alzheimer's disease. Proc Natl Acad Sci U S A 117(49):30928-30933
abstractText  Herein, we report a (64)Cu positron emission tomography (PET) imaging agent that shows appreciable in vivo brain uptake and exhibits high specific affinity for beta-amyloid (Abeta) aggregates, leading to the successful PET imaging of amyloid plaques in the brains of 5xFAD mice versus those of wild-type mice. The employed approach uses a bifunctional chelator with two Abeta-interacting fragments that dramatically improves the Abeta-binding affinity and lipophilicity for favorable blood-brain barrier penetration, while the use of optimized-length spacers between the Cu-chelating group and the Abeta-interacting fragments further improves the in vivo Abeta-binding specificity and brain uptake of the corresponding (64)Cu PET imaging agent.
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