Synthesis and Evaluation of New Bifunctional Chelators with Phosphonic Acid Arms for Gallium-68 Based PET Imaging in Melanoma.

ABSTRACT: Due to the increasing use of generator-produced radiometal Gallium-68 (⁶⁸Ga) in positron-emission tomography/computed tomography (PET/CT), reliable bifunctional chelators that can efficiently incorporate ⁶⁸Ga³⁺ into biomolecules are highly desirable. In this study, we synthesized two new bifunctional chelators bearing one or two phosphonic acid functional groups, named p-SCN-PhPr-NE2A1P and p-SCN-PhPr-NE2P1A, with the aim of enabling facile production of ⁶⁸Ga-based radiopharmaceuticals. Both chelators were successfully conjugated to LLP2A-PEG₄, a very late antigen-4 (VLA-4) targeting peptidomimetic ligand, to evaluate their application in ⁶⁸Ga-based PET imaging. NE2P1A-PEG₄-LLP2A exhibited the highest ⁶⁸

SUBMITTER: Gai Y 

PROVIDER: S-EPMC6333570 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature