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Design of a multivalent bifunctional chelator for diagnostic 64Cu PET imaging in Alzheimer's disease.
Cho, Hong-Jun; Huynh, Truc T; Rogers, Buck E; Mirica, Liviu M.
Afiliação
  • Cho HJ; Department of Chemistry, University of Illinois at Urbana-Champaign, Urbana, IL 61801.
  • Huynh TT; Department of Radiation Oncology, Washington University School of Medicine, St. Louis, MO 63108.
  • Rogers BE; Department of Chemistry, Washington University, St. Louis, MO 63130.
  • Mirica LM; Department of Radiation Oncology, Washington University School of Medicine, St. Louis, MO 63108.
Proc Natl Acad Sci U S A ; 117(49): 30928-30933, 2020 12 08.
Article em En | MEDLINE | ID: mdl-33234563
Herein, we report a 64Cu positron emission tomography (PET) imaging agent that shows appreciable in vivo brain uptake and exhibits high specific affinity for beta-amyloid (Aß) 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 Aß-interacting fragments that dramatically improves the Aß-binding affinity and lipophilicity for favorable blood-brain barrier penetration, while the use of optimized-length spacers between the Cu-chelating group and the Aß-interacting fragments further improves the in vivo Aß-binding specificity and brain uptake of the corresponding 64Cu PET imaging agent.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Radioisótopos de Cobre / Quelantes / Tomografia por Emissão de Pósitrons / Doença de Alzheimer Tipo de estudo: Diagnostic_studies Limite: Animals Idioma: En Ano de publicação: 2020 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Radioisótopos de Cobre / Quelantes / Tomografia por Emissão de Pósitrons / Doença de Alzheimer Tipo de estudo: Diagnostic_studies Limite: Animals Idioma: En Ano de publicação: 2020 Tipo de documento: Article