TY - JOUR
T1 - Liver uptake of radiolabeled targeting proteins and peptides
T2 - Considerations for targeting peptide conjugate design
AU - Hosseinimehr, Seyed Jalal
AU - Tolmachev, Vladimir
AU - Orlova, Anna
N1 - Funding Information:
The authors express their gratitude to the Swedish Cancer Society (Cancerfonden) and the Swedish Research Council (Vetenskapsrådent) for financial support.
Copyright:
Copyright 2013 Elsevier B.V., All rights reserved.
PY - 2012/11
Y1 - 2012/11
N2 - 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.
AB - 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.
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U2 - 10.1016/j.drudis.2012.07.002
DO - 10.1016/j.drudis.2012.07.002
M3 - Review article
C2 - 22781499
AN - SCOPUS:84868101162
VL - 17
SP - 1224
EP - 1232
JO - Drug Discovery Today
JF - Drug Discovery Today
SN - 1359-6446
IS - 21-22
ER -