Enhancing PET Signal at Target Tissue in Vivo: Dendritic and Multimeric Tris(hydroxypyridinone) Conjugates for Molecular Imaging of α_vβ₃ Integrin Expression with Gallium-68.

ABSTRACT: Tris(hydroxypyridinone) chelators conjugated to peptides can rapidly complex the positron-emitting isotope gallium-68 (⁶⁸Ga) under mild conditions, and the resulting radiotracers can delineate peptide receptor expression at sites of diseased tissue in vivo. We have synthesized a dendritic bifunctional chelator containing nine 1,6-dimethyl-3-hydroxypyridin-4-one groups (SCN-HP₉) that can coordinate up to three Ga³⁺ ions. This derivative has been conjugated to a trimeric peptide (RGD₃) containing three peptide groups that target the α_vβ₃ integrin receptor. The resulting dendritic compound, HP₉-RGD₃, can be radiolabeled in 97% radiochemical yield at a 3-fold higher specific activity than its homologues HP<

SUBMITTER: Imberti C 

PROVIDER: S-EPMC5314429 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature