Molecular design of radiocopper-labelled Affibody molecules.

摘要: The use of long-lived positron emitters 64Cu or 61Cu for labelling Affibody molecules may improve breast cancer patients’ stratification HER-targeted therapy. Previous animal studies have shown that the triaza chelators synthetic is suboptimal. In this study, we tested a hypothesis cross-bridged chelator, CB-TE2A, in combination with Gly-Glu-Glu-Glu spacer radiocopper would imaging contrast. CB-TE2A was coupled to N-terminus extended either glycine (designation CB-TE2A-G-ZHER2:342) (CB-TE2A-GEEE-ZHER2:342). Biodistribution and targeting properties 64Cu-CB-TE2A-G-ZHER2:342 64Cu-CB-TE2A-GEEE-ZHER2:342 were compared tumor-bearing mice 64Cu-NODAGA-ZHER2:S1, which had best previous study. provided appreciably lower uptake normal tissues higher tumor-to-organ ratios than 64Cu-NODAGA-ZHER2:S1. most pronounced several-fold difference hepatic uptake. At optimal time point, 6 h after injection, tumor 16 ± 6%ID/g tumor-to-blood ratio 181 ± 52. conclusion, chelator preferable and, possibly, other scaffold proteins having high renal re-absorption.