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Imaging of Insulinlike Growth Factor Type 1 Receptor in Prostate Cancer Xenografts Using the Affibody Molecule 111In-DOTA-ZIGF1R:4551
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Radiology, Oncology and Radiation Science, Biomedical Radiation Sciences. (Vladimir Tolmachev)
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Preclinical PET Platform. (Anna Orlova)
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2012 (English)In: Journal of Nuclear Medicine, ISSN 0161-5505, E-ISSN 1535-5667, Vol. 53, no 1, 90-97 p.Article in journal (Refereed) Published
Abstract [en]

One of the pathways leading to androgen independence in prostate cancer involves upregulation of insulinlike growth factor type 1 receptor (IGF-1R). Radionuclide imaging of IGF-1R in tumors might be used for selection of patients who would most likely benefit from IGF-1R–targeted therapy. The goal of this study was to evaluate the feasibility of in vivo radionuclide imaging of IGF-1R expression in prostate cancer xenografts using a small nonimmunoglobulin-derived binding protein called an Affibody molecule.


The IGF-1R-binding ZIGF1R:4551 Affibody molecule was site-specifically conjugated with a maleimido derivative of DOTA and labeled with 111In. The binding of radiolabeled ZIGF1R:4551 to IGF-1R–expressing cells was evaluated in vitro and in vivo.


DOTA-ZIGF1R:4551 can be stably labeled with 111In with preserved specific binding to IGF-1R–expressing cells in vitro. In mice, 111In-DOTA-ZIGF1R:4551 accumulated in IGF-1R–expressing organs (pancreas, stomach, lung, and salivary gland). Receptor saturation experiments demonstrated that targeting of DU-145 prostate cancer xenografts in NMRI nu/nu mice was IGF-1R–specific. The tumor uptake was 1.1 ± 0.3 percentage injected dose per gram, and the tumor-to-blood ratio was 3.2 ± 0.2 at 8 h after injection.


This study demonstrates the feasibility of in vivo targeting of IGF-1R–expressing prostate cancer xenografts using an Affibody molecule. Further development of radiolabeled Affibody molecules might provide a useful clinical tool for stratification of patients with prostate cancer for IGF-1R–targeting therapy.

Place, publisher, year, edition, pages
2012. Vol. 53, no 1, 90-97 p.
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Medical and Health Sciences
URN: urn:nbn:se:uu:diva-164418DOI: 10.2967/jnumed.111.090829ISI: 000298660900024PubMedID: 22173843OAI: oai:DiVA.org:uu-164418DiVA: diva2:473079
Available from: 2012-01-05 Created: 2011-12-20 Last updated: 2015-10-21Bibliographically approved

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Tolmachev, VladimirMalmberg, JennieSandström, MattiasOrlova, Anna
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