Positioning of 99mTc-chelators influences radiolabeling, stability and biodistribution of Affibody molecules

Torun Ekblad, Anna Orlova, Joachim Feldwisch, Anders Wennborg, Amelie Eriksson Karlström, Vladimir Tolmachev

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)

Abstract

Affibody molecules represent a novel class of affinity proteins with a high potential as tracers for radionuclide molecular imaging. In this comparative structure-property study, a series of Affibody molecules with the 99mTc-chelators maGGG, maSSS, or maESE attached to the ε-amine of the internally positioned K49 was prepared by peptide synthesis, for comparison to molecules with similar chelators positioned at the N-terminus. The conjugates were labeled with 99mTc and evaluated in vitro and in vivo. It was found that both composition and position of the chelating moiety influence the label stability, biodistribution and targeting properties of HER2-binding Affibody molecules.

Original languageEnglish
Pages (from-to)3912-3914
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number14
DOIs
Publication statusPublished - 15 Jul 2009

Keywords

  • Affibody molecule
  • Molecular imaging
  • Peptide synthesis
  • Tc chelator

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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