Positioning of Tc-99m-chelators influences radiolabeling, stability and biodistribution of Affibody molecules

• Affibody molecules represent a novel class of affinity proteins with a high potential as tracers for radio-nuclide molecular imaging. In this comparative structure-property study, a series of Affibody molecules with the Tc-99m-chelators maGGG, maSSS, or maESE attached to the e-amine of the internally positioned K49 was prepared by peptide synthesis, for comparison to molecules with similar chelators positioned at the N-terminus. The conjugates were labeled with Tc-99m and evaluated in vitro and in vivo. It was found that both composition and position of the chelating moiety influence the label stability, biodistribution and targeting properties of HER2-binding Affibody molecules.

Nyckelord

Affibody molecule

Tc chelator

Molecular imaging

Peptide synthesis

malignant-tumors

binding-proteins

chelators

MEDICINE

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