Optimal composition and position of histidine-containing tags improves biodistribution of ^99mTc-labeled DARPin G3.

ABSTRACT: Radionuclide molecular imaging of HER2 expression in disseminated cancer enables stratification of patients for HER2-targeted therapies. DARPin G3, a small (14 kDa) engineered scaffold protein, is a promising probe for imaging of HER2. We hypothesized that position (C- or N-terminus) and composition (hexahistidine or (HE)₃) of histidine-containing tags would influence the biodistribution of [^99mTc]Tc(CO)₃-labeled DARPin G3. To test the hypothesis, G3 variants containing tags at N-terminus (H₆-G3 and (HE)₃-G3) or at C-terminus (G3-H₆ and G3-(HE)₃) were labeled with [^99mTc]Tc(CO)₃. Labeling yield, label stability, specificity and affinity of the binding to HER2, biodistribution and tumor target

SUBMITTER: Vorobyeva A 

PROVIDER: S-EPMC6599047 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature