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Affibody Molecules as Targeting Vectors for PET Imaging

by Vladimir Tolmachev 1,2,* and Anna Orlova 2,3,4
Department of Immunology, Genetics and Pathology, Uppsala University, 75185 Uppsala, Sweden
Research Centrum for Oncotheranostics, Research School of Chemistry and Applied Biomedical Sciences, Tomsk Polytechnic University, 634050 Tomsk, Russia
Department of Medicinal Chemistry, Uppsala University, 75183 Uppsala, Sweden
Science for Life Laboratory, Uppsala University, 75237 Uppsala, Sweden
Author to whom correspondence should be addressed.
Cancers 2020, 12(3), 651;
Received: 14 February 2020 / Revised: 6 March 2020 / Accepted: 9 March 2020 / Published: 11 March 2020
(This article belongs to the Special Issue Cancer Molecular Imaging)
Affibody molecules are small (58 amino acids) engineered scaffold proteins that can be selected to bind to a large variety of proteins with a high affinity. Their small size and high affinity make them attractive as targeting vectors for molecular imaging. High-affinity affibody binders have been selected for several cancer-associated molecular targets. Preclinical studies have shown that radiolabeled affibody molecules can provide highly specific and sensitive imaging on the day of injection; however, for a few targets, imaging on the next day further increased the imaging sensitivity. A phase I/II clinical trial showed that 68Ga-labeled affibody molecules permit an accurate and specific measurement of HER2 expression in breast cancer metastases. This paper provides an overview of the factors influencing the biodistribution and targeting properties of affibody molecules and the chemistry of their labeling using positron emitters. View Full-Text
Keywords: PET; affibody molecules; HER2; EGFR; molecular imaging; radiolabeling PET; affibody molecules; HER2; EGFR; molecular imaging; radiolabeling
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Tolmachev, V.; Orlova, A. Affibody Molecules as Targeting Vectors for PET Imaging. Cancers 2020, 12, 651.

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