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Enhancing PET Signal at Target Tissue in Vivo: Dendritic and Multimeric Tris(hydroxypyridinone) Conjugates for Molecular Imaging of α v β 3 Integrin Expression with Gallium-68.

Bioconjugate Chemistry 2017 Februrary 16
Tris(hydroxypyridinone) chelators conjugated to peptides can rapidly complex the positron-emitting isotope gallium-68 (68 Ga) 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 αv β3 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 HP3 -RGD and HP3 -RGD3 that contain only a single metal binding site. PET scanning and biodistribution studies show that [68 Ga(HP9 -RGD3 )] demonstrates higher receptor-mediated tumor uptake in animals bearing U87MG tumors that overexpress αv β3 integrin than [68 Ga(HP3 -RGD)] and [68 Ga(HP3 -RGD3 )]. However, concomitant nontarget organ retention of [68 Ga(HP9 -RGD3 )] results in low tumor to nontarget organ contrast in PET images. On the other hand, the trimeric peptide homologue containing a single tris(hydroxypyridinone) chelator, [68 Ga(HP3 -RGD3 )], clears nontarget organs and exhibits receptor-mediated uptake in mice bearing tumors and in mice with induced rheumatoid arthritis. PET imaging with [68 Ga(HP3 -RGD3 )] enables clear delineation of αv β3 integrin receptor expression in vivo.

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