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Liver uptake of radiolabeled targeting proteins and peptides: considerations for targeting peptide conjugate design
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Radiology, Oncology and Radiation Science, Biomedical Radiation Sciences.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Radiology, Oncology and Radiation Science, Biomedical Radiation Sciences.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Preclinical PET Platform.ORCID iD: 0000-0001-6120-2683
2012 (English)In: Drug Discovery Today, ISSN 1359-6446, E-ISSN 1878-5832, Vol. 17, no 21-22, 1224-1232 p.Article in journal (Refereed) Published
Abstract [en]

Radionuclide imaging of molecular targets for cancer therapy is likely to be a powerful tool for patient stratification and response monitoring, allowing more personalized cancer treatment. Radiolabeled proteins and peptides are a promising class of imaging probes for visualization of molecular targets in vivo. However, hepatic uptake and hepatobiliary excretion of radioactivity can decrease imaging contrast, reducing the detection sensitivity of hepatic and extrahepatic abdominal metastases, respectively. In this article, we review factors that influence the hepatic uptake of radioactivity (e.g. the chemical nature of radiocatabolites and physicochemical properties of targeting peptides and linkers) to provide input for the rational design of peptide-based imaging probes.

Place, publisher, year, edition, pages
2012. Vol. 17, no 21-22, 1224-1232 p.
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-185395DOI: 10.1016/j.drudis.2012.07.002ISI: 000311133900010PubMedID: 22781499OAI: oai:DiVA.org:uu-185395DiVA: diva2:571589
Available from: 2012-11-23 Created: 2012-11-23 Last updated: 2017-12-07Bibliographically approved

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Hosseinimehr, Seyed JalalTolmachev, VladimirOrlova, Anna

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