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. |