Comparison of two cross-bridged macrocyclic chelators for the evaluation of 64Cu-labeled-LLP2A, a peptidomimetic ligand targeting VLA-4-positive tumors
Integrin α4β1 (also called very late antigen-4 or VLA-4) plays an important role in tumor
growth, angiogenesis and metastasis, and there has been increasing interest in targeting
this receptor for cancer imaging and therapy. In this study, we conjugated a peptidomimetic
ligand known to have good binding affinity for α4β1 integrin to a cross-bridged macrocyclic
chelator with a methane phosphonic acid pendant arm, CB-TE1A1P. CB-TE1A1P-LLP2A
was labeled with 64Cu under mild conditions in high specific activity, in contrast to …
growth, angiogenesis and metastasis, and there has been increasing interest in targeting
this receptor for cancer imaging and therapy. In this study, we conjugated a peptidomimetic
ligand known to have good binding affinity for α4β1 integrin to a cross-bridged macrocyclic
chelator with a methane phosphonic acid pendant arm, CB-TE1A1P. CB-TE1A1P-LLP2A
was labeled with 64Cu under mild conditions in high specific activity, in contrast to …
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