Maria Larkina, Ruslan Varvashenya, Feruza Yuldasheva, Evgenii Plotnikov, Ekaterina Bezverkhniaia, Maria Tretyakova, Roman Zelchan, Alexey Schulga, Elena Konovalova, Anzhelika Vorobyeva, Mikhail Belousov, Anna Orlova, Vladimir Tolmachev, Sergey Deyev
HER2 status determination is a necessary step for the proper choice of therapy and selection of patients for the targeted treatment of cancer. Targeted radiotracers such as radiolabeled DARPins provide a noninvasive and effective way for the molecular imaging of HER2 expression. This study aimed to evaluate tumor-targeting properties of three 99m Tc-labeled DARPin G3 variants containing Gly-Gly-Gly-Cys (G3 C), (Gly-Gly-Gly-Ser)3 -Cys ((G3 S)3 C), or Glu-Glu-Glu-Cys (E3 C) amino acid linkers at the C-terminus and conjugated to the HYNIC chelating agent, as well as to compare them with the clinically evaluated DARPin G3 labeled with 99m Tc(CO)3 using the (HE)3 -tag at the N-terminus...
April 1, 2024: Molecular Pharmaceutics